Search Result
Results for "
NSCLC cells
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
8
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-P99202
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Transmembrane Glycoprotein
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Cancer
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Vibostolimab is an anti-TIGIT (T cell immunoglobulin and ITIM domain) monoclonal antibody. Vibostolimab shows antitumor activity, and can be used in non-small cell lung cancer (NSCLC) and melanoma research .
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- HY-P99827
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TSR-022; GSK4069889
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Tim3
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Cancer
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Cobolimab (TSR-022) is an anti-TIM-3 monoclonal antibody. Cobolimab mediates the internalization of TIM3 with an IC50 value of 0.4464 nM. Cobolimab has potential application in solid tumors and non-small cell lung cancer (NSCLC) .
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- HY-153604
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MC4171
1 Publications Verification
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Histone Acetyltransferase
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Cancer
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MC4171 (compound 34) is a selective KAT8 inhibitor (IC50=8.1 µM). MC4171 has been shown to exhibit moderate micromolar antiproliferative activity in different cancer cell lines, including NSCLC and AML, with potential for studying cancer .
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- HY-P99223
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MEDI-575
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PDGFR
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Cancer
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Tovetumab (MEDI-575) is an anti-PDGFRα monoclonal antibody that selectively blocks the PDGFRα signal transduction. Tovetumab can be used in the research of glioblastoma and non-small cell lung cancer (NSCLC) .
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- HY-N11912
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Biochemical Assay Reagents
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Cancer
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Soladulcoside A is a steroidal glycoside and antineoplastic agent that can be obtained from the whole plant of Solanum nigrum. Soladulcoside A can inhibit A549 cells and has the potential to study cancers such as non-small cell lung cancer (NSCLC) .
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- HY-173501
-
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EGFR
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Cancer
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EGFR-IN-157 (compound IIB-5) is a potent EGFR inhibitor with an IC50 of 18.81 nM. EGFR-IN-157 can be used in the study of non-small cell lung cancer (NSCLC) .
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- HY-150571
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Topoisomerase
c-Myc
Apoptosis
ROS Kinase
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Cancer
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Anticancer agent 76 (Compound CT2-3) is an anticancer agent. Anticancer agent 76 significantly inhibits the proliferation of human NSCLC cells, induces cell cycle arrest, causes ROS generation and induces cell apoptosis .
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- HY-151905
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c-Met/HGFR
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Cancer
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D6808 is a highly selective and potent c‑Met inhibitor with an IC50 value of 2.9 nM. D6808 induces cell apoptosis and cell cycle arrest. D6808 can be used for the research of NSCLC and gastric cancers .
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- HY-173065
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CDK
Apoptosis
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Cancer
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CDK9-IN-36 (Compound T7) is a potent, selective and metabolically stable CDK9 inhibitor with an IC50 value of 1.2 nM. CDK9-IN-36 effectively suppresses cell proliferation, reduces colony formation, and induces apoptosis in Osimertinib (HY-15772)-resistant NSCLC cells by downregulating Mcl-1. CDK9-IN-36 also demonstrates antitumor efficacy in a tumor xenograft model .
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- HY-151377
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RET
EGFR
Aurora Kinase
c-Fms
MAP4K
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Cancer
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RET-IN-19 (compound 59) is a potent RET inhibitor, with IC50 values of 6.8 and 13.51 nM against RET-wt and RET V804M, respectively. RET-IN-19 shows anticancer activity. RET-IN-19 can be used for non-small cell lung cancer (NSCLC) research .
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- HY-153356
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Apoptosis
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Cancer
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MRT-2359 is a potent, orally active and selective GSPT1 depressant (IC50: >30 nM and <300 nM) that specifically induces apoptosis dependent on protein translation. MRT-2359 exhibits significant and preferred anti-proliferative activity in a variety of cancer cell lines, especially MYC-driven cell lines, such as non-small cell lung cancer (NSCLC) and small cell lung cancer (SCLC) with high expression of N-Myc or L-Myc. MRT-2359 inhibits the growth of drug-resistant NSCLC and SCLC cells, making it suitable for cancer research .
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- HY-137295
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PKC
Apoptosis
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Inflammation/Immunology
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Ingenol 3,20-dibenzoate is a potent protein kinase C (PKC) isoform-selective agonist. Ingenol 3,20-dibenzoate induces selective translocation of nPKC-delta, -epsilon, and -theta and PKC-mu from the cytosolic fraction to the particulate fraction and induces morphologically typical apoptosis through de novo synthesis of macromolecules. Ingenol 3,20-dibenzoate increases the IFN-γ production and degranulation by NK cells, especially when NK cells are stimulated by NSCLC cells .
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- HY-173403
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TrxR
Reactive Oxygen Species (ROS)
Apoptosis
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Cancer
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TrxR-IN-8 (Compound 6f) is a selective TrxR inhibitor (IC50: 10.2 μM). TrxR-IN-8 induces apoptosis through oxidative stress by stimulating the production of reactive oxygen species (ROS), reducing intracellular thiols, and lowering the glutathione/glutathione ratio. TrxR-IN-8 exhibits significant cytotoxicity against non-small cell lung cancer (NSCLC) cells .
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- HY-139047
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GLUT
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Cancer
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SW157765 is a selective non-canonical glucose transporter GLUT8 (SLC2A8) inhibitor. KRAS/KEAP1 double mutant NSCLC cells are selectively sensitive to the SW157765, due to the convergent consequences of dual KRAS and NRF2 modulation of metabolic and xenobiotic gene regulatory programs .
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- HY-144048
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EGFR
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Cancer
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EGFR-IN-31 is a potent inhibitor of EGFR. Overexpression and mutation of the epidermal growth factor receptor (EGFR) has been clearly demonstrated to lead to uncontrollable cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-31 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185298A1, compound 2) .
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- HY-144049
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EGFR
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Cancer
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EGFR-IN-32 is a potent inhibitor of EGFR. Overexpression and mutation of the epidermal growth factor receptor (EGFR) has been clearly demonstrated to lead to uncontrollable cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-32 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185297A1, compound 2) .
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- HY-145433
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17β-HSD
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Cancer
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17β-HSD1-IN-1 (Compound 1) is a highly selective 17β-HSD1 inhibitor with IC50s of 5.6 and 3155 nM for 17β-HSD1 and 17β-HSD2, respectively. 17β-HSD1-IN-1 can be used for the research of non-small cell lung cancer (NSCLC) .
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- HY-170665
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EGFR
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Cancer
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EGFR T790M/L858R-IN-9 (Compound 8) is an EGFR-L858R/T790M inhibitor that demonstrates potent inhibitory phosphorylation effects against the EGFR-L858R/T790M mutant kinase, with an IC50 value of 0.0064µM. EGFR T790M/L858R-IN-9 also inhibits the proliferation of non-small cell lung cancer (NSCLC) cells and can be utilized in cancer research .
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- HY-P991669
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Caspase
Apoptosis
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Cancer
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IGN523 is an anti-CD98 antibody (hCD98, KD = 0.55 nM). IGN523 induces antibody-dependent cell-mediated cytotoxicity (ADCC) activity, lysosomal membrane permeabilization, and inhibition of essential amino acid transport, ultimately leading to caspase-3 and caspase-7-mediated apoptosis of tumor cells. IGN523 inhibits tumor growth in multiple tumor xenograft models. IGN523 is useful in the research of non-small cell lung cancer (NSCLC), acute myeloid leukemia (AML), and other cancers. .
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- HY-147281
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Drug-Linker Conjugates for ADC
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Cancer
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BAY 1135626 is used to synthesize BAY 1129980, and use to anti-tumor research. BAY 1129980 is a Auristatin-based anti-C4.4A (LYPD3) antibody–agent conjugate (ADC), is used to non–small cell lung cancer (NSCLC) research .
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- HY-19642
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MGCD265
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TAM Receptor
c-Met/HGFR
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Cancer
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Glesatinib (MGCD265) is an orally active, potent MET/SMO dual inhibitor. Glesatinib, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC) .
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- HY-19642A
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MGCD265 hydrochloride
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TAM Receptor
c-Met/HGFR
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Cancer
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Glesatinib hydrochloride (MGCD265 hydrochloride) is an orally active, potent MET/SMO dual inhibitor. Glesatinib hydrochloride, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC) .
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- HY-110088
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MDM-2/p53
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Cancer
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SCH529074 is a potent and orally active p53 activator. SCH529074 binds specifically and conformation-dependently to p53 DBD ( DNA binding domain) with a Ki of 1-2 μM in a saturable manner. SCH529074 restores mutant p53 function and interrupts HDM2-mediated ubiquitination of wild Type p53. SCH529074 can be used for the study of non-small-cell lung carcinoma (NSCLC) .
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- HY-P11110
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PD-1/PD-L1
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Cancer
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RK-10 is a PD-L1 binding peptide. RK-10 conjugated with Cy5 (HY-D0821) or Biotin (HY-B0511) can used to detect PD-L1 expressing tumors with flow cytometry or immunohistochemistry. RK-10 can be used for cancers like NSCLC, breast cancer, squamous cell carcinoma and melanoma detection research .
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- HY-173493
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Anaplastic lymphoma kinase (ALK)
Apoptosis
Akt
mTOR
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Cancer
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ALK-IN-31 (Compound Ld-10) is an orally active ALK inhibitor (IC50: 1135 nM). ALK-IN-31 exhibits excellent antiproliferative activity against lung cancer H2228 cells with an IC50 value of 1.35 μM. ALK-IN-31 induces apoptosis and arrests cell proliferation in the G0/G1 phase by affecting mitochondrial function. ALK-IN-31 exerts its anti-tumor effect by downregulating the expression of p-AKT and p-mTOR in the PI3K-AKT-mTOR signaling pathway downstream of ALK. ALK-IN-31 can be used in the study of non-small cell lung cancer (NSCLC) .
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- HY-175749
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Wee1
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Cancer
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BMS-986463, a CRBN E3 ligase modulator (CELMoD), is a WEE1 kinase molecular glue degrader. BMS-986463 significantly inhibits tumor regression and reduces the level of phospho-CDK2. BMS-986463 can be used for advanced malignant solid tumors like non-small cell lung cancer (NSCLC) research .
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- HY-P99705
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RG-7599; DNIB-0600A; NaPi2b-ADC
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Antibody-Drug Conjugates (ADCs)
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Cancer
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Lifastuzumab vedotin (RG-7599; DNIB0600A) is an antibody-drug conjugate (ADC) that comprises a humanized IgG1 anti-NaPi2b monoclonal antibody (MNIB2126A) and a potent antimitotic agent, monomethyl auristatin E (MMAE), which inhibits cell division by blocking the polymerization of tubulin. Lifastuzumab vedotin has the potential for non-small cell lung cancer (NSCLC) and platinum-resistant ovarian cancer (PROC) research .
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- HY-150610
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EGFR
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Cancer
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EGFR-IN-69 (compound 17g) is a potent EGFR inhibitor, with IC50 values of 4.3, 6.6 and 25.6 nM against EGFR L858R/T790M/C797S, EGFR L858R/T790M, and EGFR 19del/T790M/C797S, respectively. EGFR-IN-69 can be used for non-small-cell-lung-cancer (NSCLC) research .
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- HY-147858
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PROTACs
EGFR
Apoptosis
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Cancer
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PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFR L858R/T790M degrader, with a DC50 of 13.2 nM. PROTAC EGFR degrader 7 inhibits NCI–H1975 cells proliferation, with an IC50 of 46.82 nM. PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI–H1975 cell. PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research . PROTAC EGFR degrader 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-P991620
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Transmembrane Glycoprotein
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Cancer
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JS006 is a humanized IgG4κ monoclonal antibody inhibitor targeting TIGIT/CD155. JS006 can be used to study advanced and/or metastatic cancers with resistance to PD-1/PD-L1 inhibitor such as non-small cell lung cancer (NSCLC), advanced lymphoma and advanced/metastatic triple negative breast cancer (TNBC) .
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- HY-N3764
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Akt
Dihydrofolate reductase (DHFR)
Endogenous Metabolite
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Others
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Diosbulbin C is a diterpene lactone component, which can be extracted from traditional Chinese medicine Dioscorea bulbifera L.. Diosbulbin C possesses high anticancer activity in non-small cell lung cancer (NSCLC). Diosbulbin C could induce cell cycle arrest at G0/G1 phase in NSCLC. Diosbulbin C also inhibits the proliferation of NSCLC cells, possibly by downregulating the expression/activation of AKT, DHFR, and TYMS .
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- HY-144050
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EGFR
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Cancer
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EGFR-IN-33 is a potent inhibitor of EGFR. EGFR-IN-33 is an anti-tumor agent with low toxic side effects. EGFR-IN-33 is an acrylamide derivative compound. Overexpression and mutation of the epidermal growth factor receptor (EGFR) has been clearly demonstrated to lead to uncontrollable cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-33 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185348A1, compound 13) .
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- HY-144052
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EGFR
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Cancer
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EGFR-IN-35 is a potent inhibitor of EGFR. EGFR-IN-35 is an anti-tumor agent with low toxic side effects. EGFR-IN-35 is an acrylamide derivative compound. Overexpression and mutation of the epidermal growth factor receptor (EGFR) has been clearly demonstrated to lead to uncontrollable cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-35 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185348A1, compound 11) .
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- HY-144051
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EGFR
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Cancer
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EGFR-IN-34 is a potent inhibitor of EGFR. EGFR-IN-34 is an anti-tumor agent with low toxic side effects. EGFR-IN-35 is an acrylamide derivative compound. Overexpression and mutation of the epidermal growth factor receptor (EGFR) has been clearly demonstrated to lead to uncontrollable cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-34 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185348A1, compound 12) .
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- HY-144056
-
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EGFR
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Cancer
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EGFR-IN-39 is a potent inhibitor of EGFR. EGFR-IN-39 is an anti-tumor agent with low toxic side effects. EGFR-IN-39 is an acrylamide derivative compound. Overexpression and mutation of the epidermal growth factor receptor (EGFR) has been clearly demonstrated to lead to uncontrollable cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-39 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185348A1, compound 2) .
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- HY-144054
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EGFR
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Cancer
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EGFR-IN-37 is a potent inhibitor of EGFR. EGFR-IN-37 is an anti-tumor agent with low toxic side effects. EGFR-IN-39 is an acrylamide derivative compound. Overexpression and mutation of the epidermal growth factor receptor (EGFR) has been clearly demonstrated to lead to uncontrollable cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-37 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185348A1, compound 7) .
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- HY-144055
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EGFR
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Cancer
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EGFR-IN-38 is a potent inhibitor of EGFR. EGFR-IN-38 is an anti-tumor agent with low toxic side effects. EGFR-IN-33 is an acrylamide derivative compound. Overexpression and mutation of the epidermal growth factor receptor (EGFR) has been clearly demonstrated to lead to uncontrollable cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-38 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185348A1, compound 4) .
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- HY-173218
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EGFR
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Cancer
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anti-NSCLC agent-1 (compound 8dc) is an inhibitor of tyrosine kinase inhibitors (TKIs) with IC50 values of 0.05 and 0.09 μM in A549 and NCI-H441 cells. anti-NSCLC agent-1 shows anti-NSCLC activities in colony formation, migration, and invasion .
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- HY-121537
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COX
Akt
Apoptosis
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Neurological Disease
Inflammation/Immunology
Cancer
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CAY10404 is a potent and selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 1 nM and a selectivity index (SI; COX-1 IC50/COX-2 IC50) of >500000. CAY10404 is a potent PKB/Akt and MAPK signaling pathways inhibitor and induces apoptosis in non-small cell lung cancer (NSCLC) cells. CAY10404, a diarylisoxazole, has good analgesic, anti-inflammatory, and anti-cancer activities .
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- HY-N6871
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Bacterial
IKK
Ferroptosis
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Infection
Metabolic Disease
Inflammation/Immunology
Cancer
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Abietic acid, an orally active diterpene isolated from Colophony, displays significant anti-proliferative, anti-inflammatory, anti-obesity effect, bacteriostatic, cell cycle arresting and pro-apoptotic activities. Abietic acid inhibits lipoxygenase activity for allergy. Abietic acid enhances cell migration and tube formation in HUVECs. Abietic acid induces significant angiogenic potential, which is associated with upregulation of extracellular signal-regulated kinase (ERK) and p38 expression. Abietic acid attenuates sepsis-induced lung injury by inhibiting nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) pathway to inhibit M1 macrophage polarization. Abietic acid exhibits a positive effect against liver injury by attenuating inflammation and ferroptosis. Abietic acid shows accelerated wound closure in a mouse model of cutaneous wounds. Abietic acid significantly reduces the proliferation and growth of NSCLC cells by IKKβ inhibition.Additionally, Abietic acid ameliorates psoriasis-like inflammation and modulates gut microbiota in mice. Abietic acid is promising for research in non-small-cell lung cancer (NSCLC), liver injury-related deseases and psoriasis .
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- HY-19637
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Topoisomerase
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Cancer
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SW044248 is a non-canonical topoisomerase I inhibitor, and selectively toxic for certain non-small cell lung cancer (NSCLC) cell lines.
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- HY-10261A
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BIBW 2992MA2
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EGFR
Autophagy
Apoptosis
c-Met/HGFR
Akt
p38 MAPK
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Cancer
|
Afatinib (BIBW 2992) dimaleate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib dimaleate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
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- HY-10261
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Afatinib
Maximum Cited Publications
87 Publications Verification
BIBW 2992
|
EGFR
Autophagy
Apoptosis
c-Met/HGFR
Akt
p38 MAPK
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Cancer
|
Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
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- HY-10261D
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BIBW 2992 oxalate
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EGFR
Autophagy
Apoptosis
c-Met/HGFR
Akt
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Cancer
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Afatinib (BIBW 2992) oxalate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib oxalate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
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- HY-169688
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MDM-2/p53
Apoptosis
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Cancer
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NA-17 is a naphthalimide compound with anti-tumor activity and lower toxicity to normal cells like HL-7702 and WI-38. NA-17 exhibits a p53-dependent selective inhibition in various NSCLC cells, inducing the accumulation of active p53 in the mitochondria and nuclei of NSCLC cells. NA-17 can cause cell cycle arrest in the G1 phase, leading to apoptosis and cell death .
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- HY-114358
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ONO-7475
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TAM Receptor
Trk Receptor
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Cancer
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Tamnorzatinib (ONO-7475) is a potent, selective, and orally active Axl/Mer inhibitor with IC50 values of 0.7 nM and 1.0 nM, respectively. Tamnorzatinib sensitizes AXL-overexpressing EGFR-mutant NSCLC cells to the EGFR-TKIs, suppresses the emergence and maintenance of tolerant cells. Tamnorzatinib combines with Osimertinib (HY-15772) provides a bright promise for the study of EGFR-mutated non-small cell lung cancer (NSCLC).
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- HY-175837
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EGFR
Apoptosis
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Cancer
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EGFR-IN-172 is a EGFR inhibitor. EGFR-IN-172 effectively inhibits the proliferation of non-small cell lung cancer (NSCLC) cells carrying the L858R, T790M and C797S drug-resistant mutations. EGFR-IN-172 inhibits EGFR phosphorylation, induces cell cycle arrest and apoptosis. EGFR-IN-172 can be used for the study of NSCLC .
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- HY-10261R
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BIBW 2992 (Standard)
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Reference Standards
EGFR
Autophagy
Apoptosis
c-Met/HGFR
Akt
p38 MAPK
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Cancer
|
Afatinib (Standard) is the analytical standard of Afatinib. This product is intended for research and analytical applications. Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
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- HY-121537R
-
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COX
Akt
Apoptosis
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Neurological Disease
Inflammation/Immunology
Cancer
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CAY10404 (Standard) is the analytical standard of CAY10404. This product is intended for research and analytical applications. CAY10404 is a potent and selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 1 nM and a selectivity index (SI; COX-1 IC50/COX-2 IC50) of >500000. CAY10404 is a potent PKB/Akt and MAPK signaling pathways inhibitor and induces apoptosis in non-small cell lung cancer (NSCLC) cells. CAY10404, a diarylisoxazole, has good analgesic, anti-inflammatory, and anti-cancer activities .
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- HY-173268
-
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TAM Receptor
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Cardiovascular Disease
Cancer
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UNC9426 is a potent and selective TYRO3 inhibitor (IC50 = 2.1 nM), demonstrating 276-fold and 90-fold selectivity over MERTK and AXL, respectively. UNC9426 reduces platelet aggregation without increasing bleeding time and blocks TYRO3-dependent functions in tumor cells and macrophages. UNC9426 demonstrates a favorable safety profile with no significant increase in bleeding risk in vivo. UNC9426 can be used for functional studies of TYRO3-dependent phenotypes such as non-small cell lung cancer (NSCLC) .
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- HY-147802
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EGFR
Apoptosis
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Cancer
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EGFR-IN-59 (Compound 8c) is a EGFR inhibitor (IC50=190 nM) and apoptosis inducer. EGFR-IN-59 exhibits cytotoxicity against non-small lung cancer cell lines (A549) and normal lung fibroblasts (WI38) with IC50s of 8.62 and 52.6 µM, respectively. EGFR-IN-59 can be used for the research of various cancers such as non-small cell lung cancer (NSCLC), head and neck cancer, breast cancer and colorectal cancer .
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- HY-10261AR
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BIBW 2992MA2 (Standard)
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Reference Standards
EGFR
Autophagy
Apoptosis
c-Met/HGFR
Akt
p38 MAPK
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Cancer
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Afatinib (dimaleate) (Standard) is the analytical standard of Afatinib (dimaleate). This product is intended for research and analytical applications. Afatinib (BIBW 2992) dimaleate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib dimaleate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
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- HY-174315
-
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PROTACs
Anaplastic lymphoma kinase (ALK)
Akt
ERK
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Cancer
|
WZH-17-002 is a WZH-15-125-based ALK PROTAC degrader with a DC50 of 25 nM. WZH-17-002 enhances activities against Lorlatinib (HY-12215)-resistant ALK compound mutations. WZH-17-002 significantly reduces drug resistance in ALK-fusion non-small cell lung cancer (NSCLC) and inhibits tumor growth in EML4-ALK G1202R/L1196 M xenograft mice model . Pink: ALK ligand (HY-174314); Blue: CRBN ligase ligand (HY-14658); Black: linker (HY-174316)
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- HY-175206
-
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P-glycoprotein
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Cancer
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P-gp-IN-30 (Compound 13) is a P-glycoprotein (P-gp) inhibitor by targeting YB-1. P-gp-IN-30 significantly enhances sensitivity to Paclitaxel by reducing total YB-1 and nucleus YB-1 protein expression, inhibiting the expression and function of downstream P-gp, further suppressing the efflux rate of Paclitaxel. P-gp-IN-30 potently inhibits tumor growth in A549/Taxol xenografts mice model with combination of Paclitaxel (HY-B0015). P-gp-IN-30 can be used for non-small cell lung cancer (NSCLC) research .
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- HY-Z3832
-
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Apoptosis
p38 MAPK
Autophagy
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Cancer
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N-Methylparoxetine is a derivative of Paroxetine that induces Apoptosis NSCLC cells by activating mitogen-activated protein kinase ( MAPK). N-Methylparoxetine has antitumor activity .
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-
- HY-151571
-
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Ras
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Cancer
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ZG1077 is a covalent KRAS G12C inhibitor. ZG1077 can be used in the research of non-small cell lung cancer (NSCLC) .
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- HY-118263
-
PF-00299804 hydrate; PF-299804 hydrate
|
EGFR
|
Cancer
|
Dacomitinib (PF-00299804) hydrate is an orally active, irreversible pan-ErbB inhibitor. Dacomitinib hydrate can be used in the research of cancers such as metastatic non-small cell lung cancer (NSCLC) .
|
-
- HY-106618
-
RA 233
|
Phosphodiesterase (PDE)
|
Cancer
|
Mopidamol (RA 233), a derivative of Dipyridamole (HY-B0312), is a phosphodiesterase inhibitor. Mopidamol can be used for non-small cell lung cancer (N-SCLC) research .
|
-
- HY-168875
-
|
TrxR
Reactive Oxygen Species (ROS)
|
Cancer
|
TrxR1 prodrug-1 (compound 5u) is a potent inhibitor of TrxR1. TrxR1 prodrug-1 exhibits significant antitumor efficiency in nude mice and NSCLC organoids .
|
-
- HY-110171
-
iMDK
3 Publications Verification
|
PI3K
|
Cancer
|
iMDK is a potent PI3K inhibitor and inhibits the growth factor MDK (also known as midkine or MK). iMDK suppresses non-small cell lung cancer (NSCLC) cooperatively with A MEK inhibitor without harming normal cells and mice .
|
-
- HY-148900
-
|
E1/E2/E3 Enzyme
|
Cancer
|
SCFSkp2-IN-2 (Compound AAA-237) is a Skp2 inhibitor with a KD of 28.77 μM. AAA-237 induces apoptosis of NSCLC cells and shows antitumor activities .
|
-
- HY-P99269
-
BIBH 1; Anti-Human FAP Recombinant Antibody
|
FAP
|
Cancer
|
Sibrotuzumab (BIBH 1) is a humanized IgG1 monoclonal antibody targets fibroblast activation protein (FAP). Sibrotuzumab can be used for the research of colorectal cancer and non-small cell lung cancer (NSCLC) .
|
-
- HY-N7459
-
|
AMPK
Autophagy
Fungal
|
Cancer
|
Sakurasosaponin is a saponin with potential anticancer activity that can be extracted from the root of Primula sieboldii. Sakurasosaponin can activate the AMPK pathway to induce cell autophagy and exert anti-NSCLC cell proliferation activity. Sakurasosaponin also has antifungal activity and significantly inhibits the growth of anthrax.
|
-
- HY-110171A
-
|
PI3K
|
Cancer
|
iMDK quarterhydrate is a potent PI3K inhibitor and inhibits the growth factor MDK (also known as midkine or MK). iMDK quarterhydrate suppresses non-small cell lung cancer (NSCLC) cooperatively with A MEK inhibitor without harming normal cells and mice .
|
-
- HY-N13164
-
|
PI3K
Akt
Apoptosis
|
Cancer
|
Polygalacin D3 is a triterpenoid saponin compound that can be extracted from the roots of the balloon flower. Polygalacin D3 can inhibit the proliferation of non-small cell lung cancer (NSCLC) cell lines by blocking the PI3K/Akt pathway, and it induces cell cycle arrest and cell apoptosis .
|
-
- HY-137433A
-
D-0316 mesylate
|
EGFR
|
Cancer
|
Befotertinib (D-0316) mesylate is an orally active EGFR tyrosine kinase inhibitor. Befotertinib mesylate can inhibit the proliferation of tumor cells. Befotertinib mesylate can be used in the research of EGFR T790M-positive non-small cell lung cancer (NSCLC) .
|
-
- HY-137433
-
D-0316
|
EGFR
|
Cancer
|
Befotertinib (D-0316) is an orally active EGFR tyrosine kinase inhibitor. Befotertinib can inhibit the proliferation of tumor cells. Befotertinib can be used in the research of EGFR T790M-positive non-small cell lung cancer (NSCLC) .
|
-
- HY-169269
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
PROTAC SMARCA2 degrader-18 (Example144) is a PROTAC SMARCA2 degrader. PROTAC SMARCA2 degrader-18 has the potential for the research of non-small cell lung cancer (NSCLC) .
|
-
- HY-117366
-
|
PKC
|
Cancer
|
PS432 is a PKC inhibitor with IC50s of 16.9 μM (PKCι) and 18.5 μM (PKCζ), respectively. PS432 effectively inhibits the proliferation of non-small cell lung cancer cells (NSCLCs) and tumor growth in mouse xenograft models .
|
-
- HY-146325
-
|
HSP
|
Cancer
|
HSP90-IN-11 (Compound 12c) is a potent inhibitor of HSP90. HSP90-IN-11 displays potent HSP90α inhibition comparable to AUY-922 (Luminespib). HSP90-IN-11 shows significant antiproliferative activity in CRC and NSCLC cells in a double digit nM range. HSP90-IN-11 leads to rapid degradation of client proteins EGFR and Akt in NSCLC cells. HSP90-IN-11 induces significant accumulation of a sub-G1 phase population .
|
-
- HY-159795
-
PF-07799933; ARRY-440
|
Raf
PERK
|
Cancer
|
Claturafenib ( PF-07799933) is an orally active inhibitor of pan-mutant BRAF. Claturafenib inhibits pERK in cells (IC50 value of 1.6 nM in HT29 cells). Claturafenib has anticancer activity against BRAF G469A mutant NSCLC and BRAF K601E mutant melanoma .
|
-
- HY-164513
-
|
Ras
Phosphodiesterase (PDE)
|
Cancer
|
NHTD is a KRAS-PDEδ inhibitor. NHTD targets the prenyl-binding pocket of PDEδ, altering the cellular localization of KRAS, thereby inhibiting the proliferation of KRAS-mutant cancer cells and inducing apoptosis. NHTD can be used for research on KRAS-driven non-small cell lung cancer (NSCLC) .
|
-
- HY-P991635
-
|
TNF Receptor
|
Cancer
|
PF-07329640 is a humanized monoclonal antibody inhibitor targeting TNFRSF3. PF-07329640 can be used for advanced/metastatic solid tumors like non-small cell lung cancer (NSCLC) and colorectal cancer (CRC) research .
|
-
- HY-126251
-
|
CDK
Apoptosis
|
Cancer
|
CDK9-IN-7 (compound 21e) is a selective, highly potent, and orally active CDK9/cyclin T inhibitor (IC50=11 nM), which exhibits more potent over other CDKs (CDK4/cyclinD=148 nM; CDK6/cyclinD=145 nM). CDK9-IN-7 shows antitumor activity without obvious toxicity. CDK9-IN-7 induces NSCLC cell apoptosis, arrests the cell cycle in the G2 phase, and suppresses the stemness properties of NSCLC .
|
-
- HY-126830
-
|
Antifolate
Apoptosis
|
Cancer
|
Antifolate C2 is an anti-folate compound that has inhibitory effects on the proliferation of non-squamous non-small cell lung cancer (NS-NSCLC). Antifolate C2 achieves tumor selectivity by targeting proton-coupled folate transporter (PCFT), which is more selective to PCFT than the commonly used anti-folate drug Pemetrexed (HY-10820). Antifolate C2 blocks the biosynthesis of deoxypurine nucleotides by inhibiting glycinamide ribonucleotide formyltransferase (GARFTase), ultimately inhibiting the proliferation of tumor cells. Antifolate C2 can be used in studies of NS-NSCLC, especially in patients who do not respond well to Pemetrexed .
|
-
- HY-123766
-
|
EGFR
|
Cancer
|
EGFR-IN-99 (compound 1a) is a potent EGFR and HER2 Exon 20 insertion mutant inhibitor. EGFR-IN-99 has excellent antiproliferative activity against DFCI127 cells, with an EC50 of 11.5 nM. EGFR-IN-99 can be used for the research of non-small cell lung cancer (NSCLC) .
|
-
- HY-P99921
-
HuMax-AXL-ADC
|
Antibody-Drug Conjugates (ADCs)
TAM Receptor
|
Cancer
|
Enapotamab vedotin is an AXL-targeted antibody-drug conjugate (ADC) with inhibitory potential against high AXL expressing non-small cell lung cancer (NSCLC). Enapotamab vedotin also exhibits resistant to EGFR inhibitor such as Osimertinib (HY-15772) .
|
-
- HY-167948
-
|
EGFR
|
Cancer
|
Dacomitinib metabolite M1/2 is a potent inhibitor of both wild-type (WT) EGFR and the T790M mutation, demonstrating significant activity against acquired resistance mechanisms in EGFR-mutant non-small-cell lung cancer (NSCLC).
|
-
- HY-173603
-
|
FAK
|
Cancer
|
FAK-IN-27 (compound 8A) is a potent and selective FAK inhibitor with an IC50 of 4.968 nM. FAK-IN-27 suppresses H1299 cells proliferation with an IC50 of 0.28 μM. FAK-IN-27 can be used in the study of NSCLC .
|
-
- HY-P991244
-
|
EGFR
|
Cancer
|
REGN-1400 is a humanized monoclonal antibody inhibitor targeting ErbB3. REGN-1400 reduces tumor cell proliferation by inhibiting ErbB3 and blocking related signaling pathways. REGN-1400 is promising for research of solid tumors such as non-small cell lung cancer (NSCLC), colorectal cancer (CRC), and squamous cell carcinoma of the head and neck (SCCHN) .
|
-
- HY-W423595
-
|
EGFR
|
Cancer
|
BEBT-109 is a potent pan-mutant-selective EGFR inhibitor. BEBT-109 has improved pharmacokinetic properties. BEBT-109 can be used for multiple mutant-EGFR-driven non-small cell lung cancer (NSCLC) research .
|
-
- HY-P991612
-
Sym024
|
CD73
|
Inflammation/Immunology
Cancer
|
S095024 is a humanized IgG1 monoclonal antibody inhibitor targeting CD73. S095024 can be used to study acute respiratory distress syndrome (ARDS), non-small cell lung cancer (NSCLC) and advanced solid tumor malignancies .
|
-
- HY-119182
-
NSC 300288
|
DNA/RNA Synthesis
|
Cancer
|
Mitonafide (NSC 300288) is a cytostatic agent. Mitonafide binds to double-stranded DNA through intercalation, and inhibits DNA and RNA synthesis. Mitonafide is an antitumor agent that can be used in the research of cancers, such as non-small cell lung cancer (NSCLC), leukemia .
|
-
- HY-107553
-
|
HSP
Apoptosis
|
Cancer
|
Chetomin, an active component of Chaetomium globosum, is a heat shock protein 90/hypoxia-inducible factor 1 alpha (Hsp90/HIF1α) pathway inhibitor. Chetomin is a potent, nontoxic non-small cell lung cancer cancer stem cells (NSCLC CSC)-targeting molecule .
|
-
- HY-P9986
-
MTIG-7192A; RG-6058
|
CD28
|
Cancer
|
Tiragolumab is an immune checkpoint inhibitor binding to the T-cell immunoglobulin and ITIM domain (TIGIT). Tiragolumab in combination with Atezolizumab (HY-P9904) and Bevacizumab (HY-P9906) has benefit in unresectable hepatocellular carcinoma. Tiragolumab can be used to study non-small cell lung cancer (NSCLC) and melanoma .
|
-
- HY-154960
-
|
Akt
Apoptosis
Microtubule/Tubulin
|
Cancer
|
Tubulin/AKT1-IN-1 (Compound D1-1) is an inhibitor of tubulin polymerization and AKT pathway activation. Tubulin/AKT1-IN-1 significantly inhibits the proliferation and metastasis of H1975 cells and slightly induced their apoptosis and can be used for non-small-cell lung cancer (NSCLC) research .
|
-
- HY-176205
-
AB801
|
TAM Receptor
|
Cancer
|
Ligritinib (AB801) is an orally active AXL receptor tyrosine kinase inhibitor. Ligritinib blocks the downstream signaling pathway by inhibiting the kinase activity of AXL. Ligritinib can be used in cancer research, especially in combination with chemotherapy for non-small cell lung cancer (NSCLC) .
|
-
- HY-P991628
-
|
PD-1/PD-L1
VEGFR
|
Cancer
|
SSGJ-707 is a bispecific, recombinant humanized IgG4 monoclonal antibody inhibitor targeting PD-1 and VEGF. SSGJ-707 can be used for cancers research, such as advanced non-small cell lung cancer (NSCLC) and recurrent endometrial cancer
|
-
- HY-157564
-
|
Apoptosis
|
Cancer
|
Antitumor agent-135 (Compound 13) is a potent antitumor agent. Antitumor agent-135 induces cell apoptosis, with IC50s of 3.79 , 10.55, 1.14, and 4.14 μM for NSCLC cell lines (A549, H460, PC-9, and PC-9/GR) .
|
-
- HY-158058
-
|
Toll-like Receptor (TLR)
Pyroptosis
|
Inflammation/Immunology
Cancer
|
WYJ-2 is a selective agonist for toll-like receptor 2/1 (TLR2/1) with EC50 of 18.57 nM in human TLR2 and TLR1 transient-cotransfected HEK 293T cells. WYJ-2 induces pyroptosis and exhibits anticancer activity against non-small cell lung cancer (NSCLC) .
|
-
- HY-143337
-
|
Apoptosis
EGFR
|
Cancer
|
EGFR-IN-47 is a potent and orally active EGFR L858R/T790M/C797S inhibitor with an IC50 of 0.01 μM. EGFR-IN-47 induces cell cycle attest and cell apoptosis. EGFR-IN-47 has the potential for the research of NSCLC .
|
-
- HY-77493
-
(rel)-ARQ 197; (rel)-(3R,4R)-ARQ 198
|
c-Met/HGFR
|
Cancer
|
(rel)-Tivantinib is a potent and highly selective inhibitor of the receptor tyrosine kinase c-MET. (rel)-Tivantinib has two novel targets, GSK3α and GSK3β, which play an important role in the cellular mechanism of non-small cell lung cancer (NSCLC) .
|
-
- HY-138751A
-
ASK120067 diTFA
|
EGFR
|
Cancer
|
limertinib (ASK120067) diTFA is a potent and orally active inhibitor of EGFR T790M (IC50: 0.3 nM) with selectivity over EGFR WT (IC50: 6.0 nM). limertinib diTFA is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC) .
|
-
- HY-163657
-
|
EGFR
|
Cancer
|
HER2-IN-20 (compound 32) is a potent and selective HER2 WT and HER2 YVMA inhibitor with IC50 values of 49, 42 nM, respectively. HER2-IN-20 has the potential for the research of non-small cell lung cancer (NSCLC) .
|
-
- HY-164426
-
|
P2X Receptor
Interleukin Related
IFNAR
|
Inflammation/Immunology
Cancer
|
HEI3090 is a P2X7R activator. HEI3090 stimulates dendritic cells expressing P2X7R to produce IL-18, which subsequently promotes Natural Killer cells and CD4 T cells within tumors to produce IFN-γ, leading to a sustained antitumor response. HEI3090 can be used to enhance the efficacy of αPD-1 therapy in non-small cell lung cancer (NSCLC) .
|
-
- HY-170809
-
|
RET
|
Cancer
|
RET-IN-29 (Compound 8W) is a selective RET kinase inhibitor. RET-IN-29 exhibits inhibitory potency against the BaF3 cells harboring CCDC6-RET V804M mutation with an IC50 value of 0.715 μM. RET-IN-29 is promising for research of non-small cell lung cancer (NSCLC) .
|
-
- HY-163418
-
|
EGFR
|
Cancer
|
HER2-IN-17 (Compound 2) is an inhibitor for HER2, which inhibits the Her YVMA exon 20 insertion mutation (HER2 YVMA) with an IC50 <200 nM. HER2-IN-17 inhibits proliferation of HER2 YVMA mutated BaF3 cells with an IC50 <200 nM and amliorates non-small-cell lung cancer (NSCLC) .
|
-
- HY-163417
-
|
EGFR
|
Cancer
|
HER2-IN-15 (Compound 1) is an inhibitor for HER2, which inhibits the Her YVMA exon 20 insertion mutation (HER2 YVMA) with an IC50 <200 nM. HER2-IN-15 inhibits proliferation of HER2 YVMA mutated BaF3 cells with an IC50 <200 nM and amliorates non-small-cell lung cancer (NSCLC) .
|
-
- HY-163420
-
|
EGFR
|
Cancer
|
HER2-IN-16 (Compound 14) is an inhibitor for HER2, which inhibits the Her YVMA exon 20 insertion mutation (HER2 YVMA) with an IC50 <200 nM. HER2-IN-16 inhibits proliferation of HER2 YVMA mutated BaF3 cells with an IC50 <200 nM and amliorates non-small-cell lung cancer (NSCLC) .
|
-
- HY-168926
-
|
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
NQO2-IN-1 (Compound 20b) is the inhibitor for quinone oxidoreductase (NQO) that inhibits NQO2 with an IC50 of 95 nM. NQO2-IN-1 overcomes the resistance of NSCLC cells to tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) by induction of ROS and apoptosis .
|
-
- HY-P991058
-
BMS-986315
|
Checkpoint Kinase (Chk)
|
Cancer
|
Zimistobart (BMS-986315) is a fully human IgG1 antibody that targets NKG2A. Zimistobart can be used for the study of non-small cell lung cancer (NSCLC). The isotype control for Zimistobart can refer to Human IgG1 kappa, Isotype Control (HY-P99001) .
|
-
- HY-147259
-
|
c-Met/HGFR
|
Cancer
|
Dalmelitinib is an orally active selective c-Met kinase inhibitor (IC50: 2.9 nM) that binds to the ATP-binding region of c-Met. Dalmelitinib induces the phosphorylation of MET, partially or completely inhibits the phosphorylation of AKT and ERK. Dalmelitinib potently inhibits cancer cell (c-Met oncogene amplification) proliferation, and is used for the research of cancers like human non-small cell lung cancer (NSCLC) .
|
-
- HY-138751
-
ASK120067
|
EGFR
|
Cancer
|
limertinib (ASK120067) is a potent and orally active inhibitor of EGFR T790M (IC50:0.3 nM) with selectivity over EGFR WT (IC50:6.0 nM). limertinib is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC) .
|
-
- HY-N2199
-
|
Apoptosis
Autophagy
|
Cancer
|
Sotetsuflavone is a flavonoid that can be isolated from Cycas revolute. Sotetsuflavone inhibits migration and invasion of A549 cells by reversing EMT, and induces cell apoptosis and autophagy. Sotetsuflavone inhibits HIF-1α, VEGF, angiostatin, MMP-9, and MMP-13 expression in A549 cells. Sotetsuflavone also protects mice against Crohn's disease (CD)-like colitis. Sotetsuflavone can be used for research of NSCLC .
|
-
- HY-P5005
-
|
CMV
PD-1/PD-L1
|
Infection
Inflammation/Immunology
Cancer
|
VIPhyb is a vasoactive intestinal polypeptide (VIP) receptor antagonist. VIPhyb can inhibit VIP signaling, increase T-cell immunity and downregulate PD1. VIPhyb can inhibit cancer cell proliferation. VIPhyb can reduce inflammatory cytokine expression. VIPhyb can enhance viral clearance. VIPhyb can be used for the researches of cancer, infection and inflammation and immunology, such as non-small cell lung cancer (NSCLC), cytomegalovirus infection and colitis .
|
-
- HY-157526
-
|
EGFR
Apoptosis
|
Cancer
|
EGFR-TK-IN-1 (compound 7o) is a potent mutant EGFR inhibitor with IC50 of 8.5 nM an 9.3 nM against EGFR L858R/T790M and EGFR Del19.EGFR-TK-IN-1 showes strong antiproliferative effects against EGFR mutant-driven non-small cell lung cancer (NSCLC) cells and induces cell apoptosis .
|
-
- HY-151606
-
|
Akt
|
Cancer
|
Akt3 degrader 1 (compound 12l) is a selective Akt3 degrader that overcomesOsimertinib (HY-15772)-induced resistance in H1975OR NSCLC cells. Akt3 degrader 1 also has anti-proliferative activity and significantly inhibits tumour growth in mice. Akt3 degrader 1 can be used in the study of drug-resistant non-small cell lung cancer .
|
-
- HY-161030
-
|
EGFR
|
Cancer
|
EGFR-IN-92 (compound 15) is an allosteric T790M/L858R double mutant EGFR inhibitor. EGFR-IN-92 shows antiproliferative activity against H1975 non-small lung cancer (NSCLC) cancer cells expressing double mutant EGFR .
|
-
- HY-P99961
-
JS004; Icatolimab
|
CD28
|
Cancer
|
Tifcemalimab (JS004) is a humanized anti-BTLA (B and T lymphocyte attenuation factor) monoclonal antibody. Tifcemalimab blocks the interaction of HVEM-BTLA by binding to BTLA, and thus blocks the inhibitory signaling pathway mediated by BTLA. Tifcemalimab can be used in research of cancer, such as lymphoma and non-small cell lung cancer (NSCLC) .
|
-
- HY-114842
-
|
DNA/RNA Synthesis
|
Cancer
|
TDRL-551 is a potent replication protein A (RPA) inhibitor (IC50 = 18 µM). TDRL-551 inhibits RPA-DNA interaction and increases the anti-cancer efficacy of Platinum (Pt)-based chemotherapy. TDRL-551 can be used for the research of cancer, such as non-small cell lung cancer (NSCLC) .
|
-
- HY-143466
-
|
FAK
ULK
AMPK
Apoptosis
Autophagy
|
Cancer
|
ULK1-IN-2 (compound 3s) is a potent ULK1 inhibitor. ULK1-IN-2 shows highest cytotoxic effect against cancer cell lines, with IC50 of 1.94 μM in A549. ULK1-IN-2 can induce apoptosis and simultaneously block autophagy, and can be used to study NSCLC (Non-small cell lung cancer) .
|
-
- HY-119182R
-
|
DNA/RNA Synthesis
|
Cancer
|
Mitonafide (Standard) is the analytical standard of Mitonafide. This product is intended for research and analytical applications. Mitonafide (NSC 300288) is a cytostatic agent. Mitonafide binds to double-stranded DNA through intercalation, and inhibits DNA and RNA synthesis. Mitonafide is an antitumor agent that can be used in the research of cancers, such as non-small cell lung cancer (NSCLC), leukemia .
|
-
- HY-172943
-
|
Polo-like Kinase (PLK)
|
Cancer
|
PLK1/PRC1-IN-1 (compound B4) is a PLK1/PRC1 protein complex formation inhibitor. PLK1/PRC1-IN-1 can be used in the study of non-small cell lung cancer (NSCLC) .
|
-
- HY-172449
-
|
Hedgehog
|
Cancer
|
GLI1-IN-3 (Compound 11a), a triterpenoid analogue, can inhibit Hedgehog signaling in GLI1 overexpression cancer cells. GLI1-IN-3 inhibits the proliferation in NSCLC and prostate cancer cell lines exhibiting hyper-activated Hh signaling. GLI1-IN-3 can also decrease the expression of endogenous GLI1 protein and its target genes associated with tumor progression and proliferation in A549 and DU-145 cancer cells .
|
-
- HY-175634
-
|
Lipoxygenase
β-catenin
STAT
Apoptosis
|
Cancer
|
ALOX5 stabilizer-1 is an arachidonate 5-lipoxygenase (ALOX5) stabilizer with a Kd of 7.26 μM. ALOX5 stabilizer-1 inhibits β-catenin protein levels and then suppresses STAT3 signal pathway. ALOX5 stabilizer-1 induces lung cancer cells apoptosis, inhibited cell migration and proliferation. ALOX5 stabilizer-1 can used for the study of non-small cell lung cancer (NSCLC) .
|
-
- HY-161470
-
|
Histone Demethylase
E1/E2/E3 Enzyme
DNA/RNA Synthesis
Caspase
Apoptosis
|
Cancer
|
WS-384 is a dual LSD1 and DCN1-UBC12 protein-protein interaction inhibitor with oral activity, with IC50 values of 338.79 nM and 14.81 nM, respectively. WS-384 possesses anticancer activity and can cause cell cycle arrest, DNA damage, and induce apoptosis. WS-384 can be used in the research of non-small cell lung cancer (NSCLC) .
|
-
- HY-162896
-
|
DNA/RNA Synthesis
|
Cancer
|
And1 degrader 1 (Compound A15) is a degrader of the acidic nucleoplasmic DNA-binding protein 1 (And1), which can significantly induce the degradation of And1 in NSCLC cells. And1 degrader 1 (5 μM) combined with Olaparib (HY-10162) (1 μM) effectively inhibits the proliferation of A549 and H460 cells. And1 degrader 1 can be used in cancer research .
|
-
- HY-N4139R
-
|
Drug Intermediate
|
Cancer
|
Protohypericin is a compound that can be extracted from Hypericum perforatum. Protohypericin has low photocytotoxicity but can be efficiently photoconverted into Hypericin (HY-N0453) with high phototoxicity under visible light. Protohypericin can be used in cancer research .
|
-
- HY-N4139
-
|
Drug Intermediate
|
Cancer
|
Protohypericin is a compound that can be extracted from Hypericum perforatum. Protohypericin has low photocytotoxicity but can be efficiently photoconverted into Hypericin (HY-N0453) with high phototoxicity under visible light. Protohypericin can be used in cancer research .
|
-
- HY-W110138
-
|
DNA/RNA Synthesis
Cytochrome P450
ROCK
|
Cancer
|
Chloroxoquinoline is an anticancer agent. Chloroxoquinoline damages the DNA templates of cancer cells, inducing DNA breaks and cell death, and inhibits cell invasion via down-regulating Rho/Rho kinase signaling pathway. Chloroxoquinoline enhances the radiation sensitivity of Lewis lung cancer cells and xenograft tumors in tumor-bearing mouse models but decreases efficacy after long term exposure in rat models by auto-induction effects on CYP1A and CYP3A. Chloroxoquinoline has a broad-spectrum anticancer activity, such as non-small-cell lung carcinoma (NSCLC), breast cancer and gastric cancer .
|
-
- HY-116504
-
|
EGFR
Akt
ERK
Apoptosis
|
Cancer
|
WB-308 is a novel small molecule that was identified as an inhibitor of EGFR by an in vitro EGFR kinase activity system. WB-308 was able to reduce the proliferation and clonogenicity of NSCLC cells, causing G2/M phase arrest and apoptosis. In addition, WB-308 inhibited tumor growth in two in vivo animal models (lung orthotopic transplantation model and patient-derived clonal mouse model). WB-308 impaired the phosphorylation of EGFR, AKT, and ERK1/2 proteins. Compared with Gefitinib, WB-308 had lower cytotoxicity. This study showed that WB-308 is a new EGFR-TKI that may be considered as an alternative to Gefitinib in the clinical treatment of NSCLC.
|
-
- HY-112870
-
Alflutinib; Furmonertinib; AST2818
|
EGFR
|
Cancer
|
Firmonertinib (Alflutinib; Furmonertinib) is an orally active, mutant-selective, and highly brain penetrant EGFR inhibitor. Firmonertinib inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Firmonertinib has the potential for the research of cancer diseases, especially advanced non-small cell lung cancer (NSCLC) with EGFR ex20ins mutation .
|
-
- HY-142283AS
-
|
EGFR
|
Cancer
|
Dosimertinib-d5 (mesylate) is a potent and orally active EGFR inhibitor. Dosimertinib-d5 (mesylate) decreases the expression of p-EGFR and p-ERK protein levels. Dosimertinib-d5 (mesylate) shows antiproliferative and anti-tumor activity. Dosimertinib-d5 (mesylate) has the potential for the research of non-small-cell lung cancer (NSCLC) .
|
-
- HY-13299
-
MK-8033
2 Publications Verification
|
c-Met/HGFR
|
Cancer
|
MK-8033 is an orally active ATP competitive c-Met/Ron dual inhibitor (IC50s: 1 nM (c-Met),7 nM (Ron)), with preferential binding to the activated kinase conformation. MK-8033 can be used in the research of cancers, such as breast and bladder cancers, non-small cell lung cancers (NSCLCs) .
|
-
- HY-149352
-
|
Thymidylate Synthase
|
Cancer
|
DG1 (Compound 8Nc) is a Thymidylate Synthase (TS) inhibitor that affects cancer angiogenesis and metabolic reprogramming in NSCLC cells. DG1 can effectively inhibit the expression of CD26, ET-1, FGF-1 and EGF. DG1 also effectively inhibits the proliferation of cancer tissue in the A549 xenograft mouse model .
|
-
- HY-112870A
-
Alflutinib mesylate; Furmonertinib mesylate; AST2818 mesylate
|
EGFR
|
Cancer
|
Firmonertinib (Alflutinib; Furmonertinib) mesylate is is an orally active, mutant-selective, and highly brain penetrant EGFR inhibitor. Firmonertinib mesylate inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Firmonertinib mesylate has the potential for the research of cancer diseases, especially advanced non-small cell lung cancer (NSCLC) with EGFR ex20ins mutation .
|
-
- HY-13299A
-
|
c-Met/HGFR
|
Cancer
|
MK-8033 hydrochloride is an orally active ATP competitive c-Met/Ron dual inhibitor (IC50s: 1 nM (c-Met),7 nM (Ron)), with preferential binding to the activated kinase conformation. MK-8033 hydrochloride can be used in the research of cancers, such as breast and bladder cancers, non-small cell lung cancers (NSCLCs) .
|
-
- HY-P99157
-
|
CD276/B7-H3
|
Cancer
|
Omburtamab is a humanized monoclonal antibody targeting B7-H3 (CD276). Omburtamab selectively binds to B7-H3 highly expressed on the surface of tumor cells and activates anti-tumor immune responses mediated by T cells and natural killer (NK) cells. Omburtamab can promote the specific infiltration of CAR-T cells into tumors, enhance the killing function of NK cells through the CD16 signaling pathway, and regulate tumor cell glucose metabolism (such as inhibiting the Warburg effect). Omburtamab has the potential to inhibit solid tumors such as non-small cell lung cancer (NSCLC) .
|
-
- HY-155227
-
|
Anaplastic lymphoma kinase (ALK)
EGFR
Apoptosis
|
Cancer
|
ALK/EGFR-IN-1 (Compound 8l) is an ALK/EGFR dual inhibitor that blocks the phosphorylation of EGFR and ALK. ALK/EGFR-IN-1 inhibits ALK/EGFR mutants respectively, with IC50 of 4.3 nM for EGFR L858R T790M in H1975 cells and EML4-ALK in BaF3 cells, respectively. and 3.6 nM. ALK/EGFR-IN-1 may be used in NSCLC research .
|
-
- HY-153901
-
|
EGFR
PROTACs
|
Cancer
|
PROTAC EGFR degrader 8 (T-184) is a PROTAC EGFR degrader. PROTAC EGFR degrader 8 degrades EGFR in HCC827 cell with a DC50 of 15.56 nM. PROTAC EGFR degrader 8 inhibits H1975, PC-9, HCC827 cell growth with IC50s of 7.72 nM, 121.9 nM, 14.21 nM. PROTAC EGFR degrader 8 can be used for research of cancer, especially NSCLC .
|
-
- HY-161857
-
|
Akt
mTOR
Caspase
CDK
|
Cancer
|
Akt/mTOR-IN-1 (Compound 8r) is an AKT/mTOR signaling pathway inhibitor exhibiting an IC50 value of 0.8 µM with anticancer activity. Akt/mTOR-IN-1 can decrease the expression of Caspase 3 and increase the expression of the autophagic protein Cyclin B1, thereby inducing cell autophagy and apoptosis. Akt/mTOR-IN-1 can be used in research related to non-small cell lung cancer (NSCLC) .
|
-
- HY-N0429
-
|
Apoptosis
MDM-2/p53
Bcl-2 Family
CDK
|
Cancer
|
Diosbulbin B, a diterpene lactone, is an anticancer agent. Diosbulbin B is an orally active component of Dioscorea. bulbifera L. Diosbulbin B can inhibit cell proliferation, induce G0/G1 phase arrest and apoptosis. Diosbulbin B can induce autophagy and mitochondrial dysfunction. Diosbulbin B can induce liver injury. Diosbulbin B can be used for the research of cancer, such as non-small cell lung cancer (NSCLC) .
|
-
- HY-147942
-
|
PROTACs
EGFR
|
Cancer
|
MS9449 is a potent PROTAC EGFR degrader with Kds of 17 nM and 10 nM for EGFR WT and EGFR L858R, respectively. MS9449 effectively induces degradation of mutant EGFRs through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9449 potently inhibits the proliferation of NSCLC cells. MS9449 can be used for researching anticancer .
|
-
- HY-120436
-
|
Drug Derivative
|
Cancer
|
RM 49 is the derivative of Mitomycin C (HY-13316). RM 49 exhibits cytotoxicity in SCLC and NSCLC lung cancer cells with IC50 of 0.01-0.5 μg/mL. RM 49 exhibits high relative antitumor activity in compared with Mitomycin C, Cisplatin (HY-17394), Carboplatin (HY-17393) and Doxorubicin (HY-15142) .
|
-
- HY-147340
-
|
Drug-Linker Conjugates for ADC
|
Cancer
|
TL033 is a drug-Linker conjugates for ADC. TL033 contains a linker and bioactive small molecule toxins. TL033 can conjugate with Sacituzumab antibody (anti Trop-2) for synthesizing BT001021. BT001021 has anti-cancer activities against various cancers, such as breast cancer, non-small cell lung cancer (NSCLC), gastric cancer .
|
-
- HY-168112
-
|
EGFR
|
Cancer
|
EGFR-IN-127 is an ATP-competitive EGFR inhibitor with IC50s of 136.3 nM and 161. 2 nM for EGFR del19 and EGFR del19/T790M/C797S, respectively. EGFR-IN-127 has the potential for the study of non-small-cell lung cancer (NSCLC) .
|
-
- HY-P99379
-
CAN04; Anti-IL-1RAP/IL-1R3 Reference Antibody (nidanilimab)
|
Interleukin Related
|
Cancer
|
Nidanilimab (CAN04) is a fully humanized monoclonal anti-IL1RAP antibody with a Kd value of 1.10 pM. Nidanilimab blocks IL1α and IL1β signaling and stimulates the immune system to destroy tumour cells. Nidanilimab can be used in research of non-small lung cancer (NSCLC) and pancreatic ductal adenocarcinoma (PDAC) .
|
-
- HY-P10944
-
NNS309
|
FAP
|
Cancer
|
Unlabeled FXX489 (NNS309) is a fibroblast activation protein (FAP)-targeting ligand. Unlabeled FXX489 can be labeled with 68Ga and 177Lu and shows anticancer effects. Unlabeled FXX489 can be used for the study of pancreatic ductal adenocarcinoma (PDAC), non-small cell lung cancer (NSCLC), breast cancer (BC), and colorectal cancer (CRC) .
|
-
- HY-148510
-
|
Phosphatase
Apoptosis
Akt
ERK
Reactive Oxygen Species (ROS)
|
Cancer
|
HKB99 is an allosteric inhibitor of phosphoglycerate mutase 1 (PGAM1). HKB99 induces apoptosis. HKB99 inhibits the formation of invasive pseudopodia and inhibits migration. HKB99 increases the oxidative stress, activates JNK/c-Jun and suppresses AKT and ERK. HKB99 can be used for the research of non-small-cell lung cancer (NSCLC) .
|
-
- HY-157229
-
|
EGFR
ERK
|
Cancer
|
STX-721 is an orally active, irreversible, covalent EGFR exon 20 insertion (ex20ins) inhibitor that selectively targets ex20ins-mutant dynamic protein states. STX-721 potently inhibits the kinase activity of EGFR ex20ins mutants (NPG, ASV, SVD). STX-721 inhibits phosphorylation of EGFR (pEGFR Y1068) and downstream ERK (pERK Thr202/Tyr204), and suppresses proliferation of ex20ins-mutant Ba/F3 cells and human NSCLC cell lines (NCI-H2073 ASV KI, CUTO-14 ASV). STX-721 induces tumor regression in EGFR ex20ins-mutant PDX/CDX models. STX-721 can be used for the study of non-small cell lung cancer (NSCLC) harboring EGFR or HER2 ex20ins mutations .
|
-
- HY-14783
-
-
- HY-N2993R
-
|
Apoptosis
Caspase
PARP
Akt
PTEN
MDM-2/p53
JNK
|
Cancer
|
Polyporenic acid C (Standard) is an analytical standard of Polyporenic acid C (HY-N2993). This product is intended for research and analytical applications. Polyporenic acid C is a lanostane-type triterpenoid. Polyporenic acid C can be isolated from Poria cocos. Polyporenic acid C causes the cleavage of caspase-8 and caspase-3, as well as the cleavage of PARP. Polyporenic acid C reduces the phosphorylation level of Akt (Ser473), increases the phosphorylation of PTEN and p53 (Ser15), and activates JNK. Polyporenic acid C induces Apoptosis. Polyporenic acid C shows anticancer activity against non-small cell lung cancer .
|
-
- HY-N2993
-
|
Apoptosis
Caspase
PARP
Akt
PTEN
MDM-2/p53
JNK
|
Cancer
|
Polyporenic acid C is a lanostane-type triterpenoid. Polyporenic acid C can be isolated from Poria cocos. Polyporenic acid C causes the cleavage of caspase-8 and caspase-3, as well as the cleavage of PARP. Polyporenic acid C reduces the phosphorylation level of Akt (Ser473), increases the phosphorylation of PTEN and p53 (Ser15), and activates JNK. Polyporenic acid C induces Apoptosis. Polyporenic acid C shows anticancer activity against non-small cell lung cancer .
|
-
- HY-12965B
-
|
TAM Receptor
|
Cancer
|
(Z)-S49076 hydrochloride is an orally active inhibitor of MET and AXL that blocks the downstream signaling of these receptors both in vitro and in vivo, inhibiting the proliferation and migration of tumor cells and suppressing tumor growth in xenograft models. (Z)-S49076 hydrochloride is capable of overcoming the resistance to epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) due to MET amplification in Erlotinib (HY-50896)-resistant cell lines both in vitro and in vivo. (Z)-S49076 hydrochloride can be used for research in non-small cell lung cancer (NSCLC) .
|
-
- HY-137497
-
|
Ras
Apoptosis
|
Cancer
|
KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells .
|
-
- HY-173500
-
|
MMP
Apoptosis
EGFR
STAT
|
Cancer
|
MG-3C is a potent matrix metalloproteinase 9 (MMP-9) inhibitor. MG-3C can selectively kill non-small-cell lung cancer (NSCLC) cells harboring the EGFR T790M mutation. MG-3C blocks the EGFR/STAT3 signaling pathway, inducing G2/M phase arrest, growth inhibition, and apoptosis of cancer cells. MG-3C is promising for research of lung cancer .
|
-
- HY-147941
-
|
PROTACs
EGFR
|
Cancer
|
MS9427 is a potent PROTAC EGFR degrader with Kds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 potently inhibits the proliferation of NSCLC cells. MS9427 can be used for researching anticancer .
|
-
- HY-161284
-
|
MMP
|
Cancer
|
MMP-9/10-IN-1 (Compound 6b) is a potent dual MMP-9/10 Inhibotor with IC50s of 0.076 and 0.139 μM against NSCLC and A549 cells, respectively. MMP-9/10-IN-1 has anti-invasive and anti-angiogenic activities when in combination with Sorafenib (HY-10201) .
|
-
- HY-19815
-
CK-101; RX518
|
EGFR
|
Cancer
|
Olafertinib (CK-101) is an orally available, third generation and irreversible epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI). Olafertinib selectively inhibits both EGFR-TKI-sensitizing and resistance mutations with minimal activity on wild-type EGFR. Olafertinib can be used in research for non-small cell lung cancer (NSCLC) with EGFR mutations and other advanced malignancies .
|
-
- HY-119694
-
|
Others
|
Cancer
|
Rotenolone is an antiproliferative agent. Rotenolone shows antiproliferative activity against the ovarian cancer A2780, breast cancer BT-549, prostate cancer DU 145, NSCLC NCI-H460, and colon cancer HCC-2998 cell lines, with IC50s of 0.95, 1.6, 2.7, 2.0, and 2.9 μM, respectively .
|
-
- HY-50687
-
(3S,4S)-ARQ 197; ARQ 198
|
c-Met/HGFR
|
Cancer
|
(3S,4S)-Tivantinib is a potent and highly selective inhibitor of the receptor tyrosine kinase c-MET. (3S,4S)-Tivantinib has two novel targets, GSK3α and GSK3β, which play an important role in the cellular mechanism of non-small cell lung cancer (NSCLC) .
|
-
- HY-18750A
-
AZD3759 hydrochloride
|
EGFR
Apoptosis
|
Cancer
|
Zorifertinib (AZD3759) hydrochloride is a potent, orally active, central nervous system-penetrant, EGFR inhibitor (IC50s: 0.3, 0.2, and 0.2 nM for EGFR wt, EGFR L858R, and EGFR exon 19Del, respectively). Zorifertinib hydrochloride induces cancer cell apoptosis. Zorifertinib hydrochloride has antitumor activity, and can be used for NSCLC, HCC etc. research .
|
-
- HY-172881
-
|
Pyruvate Kinase
|
Cancer
|
PKM2-IN-10 (Compound 16) is a PKM2 inhibitor. PKM2-IN-10 inhibits the proliferation of A549 and HCC1833 cell lines with IC50 of 3.36 μM and 9.20 μM, respectively. PKM2-IN-10 exhibits antitumor activity in human non-small cell lung cancer (NSCLC) and mouse lung adenocarcinoma models. PKM2-IN-10 can be used in lung cancer research .
|
-
- HY-173520
-
|
EGFR
HDAC
|
Cancer
|
EGFR/HDAC-IN-1 (Compound 22c2) is a potent dual inhibitor of epidermal growth factor receptor (EGFR) and histone deacetylase (HDAC) with IC50 values of 4.81 nM, 119.4 nM and 354.8 nM for EGFR, HDAC1 and HDAC3, respectively. EGFR/HDAC-IN-1 blocks the EGFR signaling pathway and affects the histone acetylation status, thereby inhibiting tumor cell proliferation. EGFR/HDAC-IN-1 is promising for research of non-small cell lung cancer (NSCLC) .
|
-
- HY-172958
-
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
F6524-1593 is an ALK inhibitor. F6524-1593 has inhibitory activity against A549 and HepG-2 cells with IC50 values of 161.1 μM and 91.03 μM, respectively. F6524-1593 can be used in the research of ALK-related cancers (such as non-small cell lung cancer, lymphoma and neuroblastoma) .
|
-
- HY-119307
-
TMI-005
|
MMP
TNF Receptor
|
Cancer
|
Apratastat (TMI-005) is an orally active, non-selective and reversible TACE/MMPs inhibitor, can inhibit inhibit the release of TNF-α. Apratastat has the potential to overcome radiotherapy-resistance in non-small cell lung cancer (NSCLC) . Apratastat is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-E70713
-
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
EML4-ALK is a fusion-type protein tyrosine kinase produced through gene rearrangement. EML4-ALK is a potential molecular target in non-small cell lung carcinoma (NSCLC). EML4 ALK Recombinant Human Active Protein Kinase is a recombinant EML4 ALK protein that can be used to study EML4 ALK-related functions .
|
-
- HY-18750
-
AZD3759
|
EGFR
Apoptosis
|
Cancer
|
Zorifertinib (AZD3759) is a potent, orally active, central nervous system-penetrant, EGFR inhibitor. At Km ATP concentrations, the IC50s are 0.3, 0.2, and 0.2 nM for EGFR wt, EGFR L858R, and EGFR exon 19Del, respectively. Zorifertinib induces cancer cell apoptosis. Zorifertinib has antitumor activity, and can be used for NSCLC, HCC etc. research .
|
-
- HY-E70646
-
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase in the insulin receptor superfamily. ALK can be used for the study of non-small cell lung carcinoma (NSCLC). ALK has multiple mutants. ALK L1196M Recombinant Human Active Protein Kinase is a recombinant ALK L1196M protein that can be used to study ALK L1196M-related functions .
|
-
- HY-E70644
-
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase in the insulin receptor superfamily. ALK can be used for the study of non-small cell lung carcinoma (NSCLC). ALK has multiple mutants. ALK F1174S Recombinant Human Active Protein Kinase is a recombinant ALK F1174S protein that can be used to study ALK F1174S-related functions .
|
-
- HY-19939S
-
VX-984
4 Publications Verification
M9831
|
DNA-PK
|
Cancer
|
VX-984 is an orally active, potent, selective and BBB-penetrated DNA-PK inhibitor. VX-984 efficiently inhibits NHEJ (non-homologous end joining) and increases DSBs (DNA double-strand breaks). VX-984 can be used for glioblastomas (GBM) and non-small cell lung cancer (NSCLC) research. VX-984 is a de novo deuterium .
|
-
- HY-E70642
-
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase in the insulin receptor superfamily. ALK can be used for the study of non-small cell lung carcinoma (NSCLC). ALK has multiple mutants. ALK C1156Y Recombinant Human Active Protein Kinase is a recombinant ALK C1156Y protein that can be used to study ALK C1156Y-related functions .
|
-
- HY-E70645
-
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase in the insulin receptor superfamily. ALK can be used for the study of non-small cell lung carcinoma (NSCLC). ALK has multiple mutants. ALK G1202R Recombinant Human Active Protein Kinase is a recombinant ALK G1202R protein that can be used to study ALK G1202R-related functions .
|
-
- HY-147340A
-
|
Drug-Linker Conjugates for ADC
|
Cancer
|
TL033 TFA is a drug-Linker conjugates for ADC. TL033 TFA contains a linker and bioactive small molecule toxins. TL033 TFA can conjugate with Sacituzumab antibody (anti Trop-2) for synthesizing BT001021. BT001021 has anti-cancer activities against various cancers, such as breast cancer, non-small cell lung cancer (NSCLC), gastric cancer .
|
-
- HY-148572
-
|
Indoleamine 2,3-Dioxygenase (IDO)
NAMPT
|
Cancer
|
NAMPT/IDO1-IN-1 is an orally active dual inhibitor of NAMPT and IDO1 with IC50s of 57.7 nM and 233 nM, respectively. NAMPT/IDO1-IN-1 blocks NAD+ biosynthesis, inhibits proliferation and migration of Paclitaxel (HY-B0015)- and FK866 (HY-50876)-resistant NSCLC cell lines (A549/R cells). NAMPT/IDO1-IN-1 has shown antitumor effects in mice and enhanced A549/R cell sensitivity to paclitaxel .
|
-
- HY-103702
-
|
Proton Pump
|
Cancer
|
TIP48/49-IN-1 (Compound B) is an orally active and specific inhibitor of RUVBL1/2 ATPase, with an IC50 of 59 nM for purified RUVBL1/2. TIP48/49-IN-1 affects DNA replication process, and leads to S-phase arrest. TIP48/49-IN-1 induces apoptosis. TIP48/49-IN-1 inhibits tumor growth and radiosensitizes non-small cell lung cancer cells (NSCLC) .
|
-
- HY-147941A
-
|
PROTACs
EGFR
|
Cancer
|
MS9427 TFA is a potent PROTAC EGFR degrader with Kds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 TFA selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 TFA potently inhibits the proliferation of NSCLC cells. MS9427 TFA can be used for researching anticancer .
|
-
- HY-138072
-
|
EGFR
|
Cancer
|
EMI1 is an EGFR ex19del/T790M/C797S and EGFR L858R/T790M/C797S inhibitor. EMI1 can be used for the research of mutant EGFR-associated, drug-resistant non-small-cell lung cancer (NSCLC) .
|
-
- HY-114277
-
AMG-510
|
Ras
|
Cancer
|
Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C‑mutated locally advanced or metastatic non‑small cell lung cancer (NSCLC) .
|
-
- HY-153361
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
YD23 is a selective SMARCA2 PROTAC degrader with DC50 values of 64 nM and 297 nM in H1792 cells and H1975 cells. YD23 induces degradation of SMARCA2, which is synthetic lethal to SMARCA4. YD23 reduces chromatin accessibility only in SMARCA4 deficient cells, including cell cycle and cell growth regulatory genes. YD23 selectively inhibits growth of SMARCA4 mutant lung cancer cells. YD23 has potent tumor growth inhibitory activity in SMARCA4-mutant xenografts. YD23 can be used for the study of non-small cell lung cancer (NSCLC) (Pink: SMARCA2 ligand (HY-44012); Blue: CRBN ligand (HY-41547); Black: Linker (HY-175566)) .
|
-
- HY-170968
-
|
EGFR
Apoptosis
|
Cancer
|
EGFR-IN-150 is an EGFR inhibitor that effectively suppresses the phosphorylation of mutant epidermal growth factor receptor (EGFR) and its downstream AKT signaling pathway, thereby exerting antitumor effects and inducing HMOX1 expression to trigger ferroptosis. EGFR-IN-150 exhibits an IC50 of 0.386 μM against the non-small cell lung cancer (NSCLC) cell line H1975, and significantly inhibits colony formation and migration of both H1975 and A549 cells while inducing apoptosis. In addition, EGFR-IN-150 markedly suppresses tumor growth in the H1975 cell-derived xenograft (CDX) mouse model. EGFR-IN-150 holds promise for research related to non-small cell lung cancer .
|
-
- HY-159966
-
|
Topoisomerase
HDAC
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
Top/HDAC-IN-3 (Compound 31) is an orally active dual inhibitor of Topoisomerase and HDAC. Top/HDAC-IN-3 increases reactive oxygen species (ROS) levels, leading to DNA damage, thereby inhibiting cancer cell colony formation and migration, inducing cancer cell Apoptosis, and causing cell cycle arrest. In the NSCLC model, Top/HDAC-IN-3 exhibited significant antitumor effects, with a tumor growth inhibition (TGI) of 77.5% at 100 mg/kg, surpassing the efficacy of the HDAC inhibitor SAHA (HY-10221) and the combination of SAHA (HY-10221) with the topoisomerase inhibitor Irinotecan (HY-16562) .
|
-
- HY-171191
-
|
Antibody-Drug Conjugates (ADCs)
Microtubule/Tubulin
c-Met/HGFR
|
Cancer
|
REGN5093-M114 is a bispecific antibody-drug conjugate (ADC) that targets two epitopes of the MET receptor tyrosine kinase inhibits the proliferation of NSCLC cells, exhibits antitumor efficacy in mouse models. REGN5093-M114 is composed of the human monoclonal anti-MET antibody Davutamig (HY-P990073) and the tubulin-inhibiting linker-payload (HY-148528) .
|
-
- HY-12972
-
PF-06747775
|
EGFR
|
Cancer
|
Mavelertinib is a selective, orally available and irreversible EGFR tyrosine kinase inhibitor (EGFR TKI), with IC50s of 5, 4, 12 and 3 nM for Del, L858R, and double mutants T790M/L858R and T790M/Del, respectively. Mavelertinib can be used for the research of non-small-cell lung cancer (NSCLC) .
|
-
- HY-17654
-
|
EGFR
mTOR
|
Cancer
|
BIEGi-1 is an EGFR inhibitor. BIEGi-1 effectively disrupts the EGFR-Rheb interaction in cells. BIEGi-1 robustly inhibits EGFR kinase activity (reduces p-Y1068-EGFR) as well as mTORC1 activation (reduces p-T389-S6K1) in EGFR-mutant cells. BIEGi-1 shows strong antiproliferative effects on EGFR-mutant PC9 and HCC827 cells with IC50 values of 17 nM and 20 nM, respectively. BIEGi-1 can be used for the study of cancers harboring EGFR mutations, such as non-small cell lung cancer (NSCLC) .
|
-
- HY-137191
-
|
EGFR
|
Cancer
|
CH7233163 is a noncovalent ATP-competitive inhibitor for EGFR-Del19/T790M/C797S. CH7233163 can overcome Osimertinib (HY-15772)-Resistant EGFR-Del19/T790M/C797S mutation. CH7233163 blocks the EGFR phosphorylation in the Del19/T790M/C797S_NIH3T3 cells. CH7233163 has antitumor activities .
|
-
- HY-156698
-
|
PROTACs
EGFR
|
Cancer
|
HJM-561 is a selective and effective orally active EGFR PROTAC degrader. HJM-561 is able to overcome the triple EGFR mutations that are resistant to Osimertinib (HY-15772). HJM-561 exhibits potent degradation of EGFR Del19/T790M/C797S (DC50: 9.2 nM) and L858R/T790M/C797S (DC50: 5.8 nM), and has anti-tumor activity (pink: EGFR ligand (HY-12857); blue: CRBN ligand (HY-A0003); black: linker) .
|
-
- HY-P10386
-
|
Bcl-2 Family
|
Cancer
|
155H1 (Compound 11) is a stapled peptide, that covalently binds hMcl1 (172-323) with IC50 of 18 nM .
|
-
- HY-145928
-
GDC-6036
|
Ras
|
Cancer
|
Divarasib (GDC-6036) is an orally bioavailable, highly potent, and selective KRAS G12C inhibitor with an IC50 of <0.01 μM. Divarasib covalently binds to the switch II (SW-II) pocket of KRAS G12C and irreversibly locks it in the inactive GDP-bound state.
|
-
- HY-108230
-
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
ALK-IN-12 is a potent and orally active ALK inhibitor with an IC50 of 0.18 nM. ALK-IN-12 also inhibits IGF1R and InsR (IC50=20.3 and 90.6 nM). Antitumor activities .
|
-
- HY-145928B
-
GDC-6036 adipate
|
Ras
|
Cancer
|
Divarasib (GDC-6036) adipate is an orally bioavailable, highly potent, and selective KRAS G12C inhibitor with an IC50 of <0.01 μM. Divarasib covalently binds to the switch II (SW-II) pocket of KRAS G12C and irreversibly locks it in the inactive GDP-bound state .
|
-
- HY-W403933R
-
|
Autophagy
Reference Standards
|
Metabolic Disease
|
Afatinib (Standard) is the analytical standard of Afatinib. This product is intended for research and analytical applications. Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
|
-
- HY-155005
-
|
EGFR
|
Cancer
|
EGFR mutant-IN-2 (Compound D51) is an EGFR mutant inhibitor. EGFR mutant-IN-2 inhibits the EGFR L858R/T790M/C797S mutant with an IC50 value of 14 nM. EGFR mutant-IN-2 inhibits the EGFR del19/T790M/C797S mutant with an IC50 value of 62 nM. EGFR mutant-IN-2 has favorable PK parameters, safety properties, in vivo stability, and antitumor activity .
|
-
- HY-144680
-
ZL-2313
|
EGFR
|
Cancer
|
BLU-945 is a potent, highly selective, reversible and orally active epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKIs). BLU-945 can effectively inhibit EGFR with L858R and/or exon 19 deletion mutation, T790M mutation and C797S mutation. BLU-945 can be used for the research of lung cancer including non-small cell lung cancer (NSCLC) .
|
-
- HY-116749
-
BBSKE
|
TrxR
|
Cancer
|
Ethaselen (BBSKE) is an orally active, selective thioredoxin reductase (TrxR) inhibitor with IC50s of 0.5 and 0.35 μM for the wild-type human TrxR1 and rat TrxR1, respectively. Ethaselen specifically binds to the unique selenocysteine-cysteine redox pair in the C-terminal active site of mammalian TrxR1. Ethaselen, an organoselenium compound, is a potent antitumor candidate that exerts potent inhibition on non-small cell lung cancer (NSCLC) by targeting TrxR .
|
-
- HY-149275
-
|
Pyruvate Kinase
PDK-1
Akt
EGFR
Apoptosis
|
Cancer
|
PKM2/PDK1-IN-1, one of shikonin thioether derivatives, is a dual inhibitor of PKM2/PDK1. PKM2/PDK1-IN-1 inhibits the proliferation of NSCLC cells, and induces apoptosis. PKM2/PDK1-IN-1 induces intercellular ROS production, and regulates the apoptotic proteins, to involves in mitochondrial and death receptor pathway .
|
-
- HY-147858A
-
|
PROTACs
|
Cancer
|
PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFRL858R/T790M degrader, with a DC50 of 13 .2 nM.PROTAC EGFR degrader 7 inhibits NCI-H1975 cells proliferation, with an IC50 of 46 .82 nM.PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI-H1975 cell.PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research .
|
-
- HY-159607
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
PRT3789 is a SMARCA2 PROTAC degrader (DC50 in HeLa cell: 0.72 nM for SMARCA2, 14 nM for SMARCA4). PRT3789 shows synergistic anti-proliferation effects with Adagrasib (HY-130149) in cancer cells. PRT3789 inhibits SMARCA4-mutated lung cancer proliferation. PRT3789 inhibits tumor growth in SMARCA4-deleted NSCLC models. Pink: SMARCA4 ligand (HY-44824) ; Blue: VHL ligand (HY-159465) ; Black: linker; VHL ligand+linker (HY-172738) .
|
-
- HY-P99117
-
AK104
|
PD-1/PD-L1
CTLA-4
|
Inflammation/Immunology
Cancer
|
Cadonilimab (AK104) is a humanized tetravalent IgG1 bispecific antibody targeting PD1/CTLA4. Cadonilimab blocks both PD-1 and CTLA-4 pathways, thereby relieving their corresponding immunosuppressive effects and reversing tumor specific T cell exhaustion. Cadonilimab significantly downregulates Fc-mediated effector functions, including antibody-dependent cell-mediated cytotoxicity (ADCC), antibody-dependent cellular phagocytosis (ADCP), complement dependent cytotoxicity (CDC). Cadonilimab can be used for research of metastatic cervical cancer, as well as other malignancies such as gastric cancer, GEJ adenocarcinoma and non-small cell lung cancer (NSCLC) .
|
-
- HY-101522
-
|
EGFR
BMX Kinase
Btk
MEK
|
Cancer
|
CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. CHMFL-EGFR-202 exhibits ~10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 adopts a covalent “DFG-in-C-helix-out” inactive binding conformation with EGFR, with strong antiproliferative effects against EGFR mutant-driven nonsmall-cell lung cancer (NSCLC) cell lines .
|
-
- HY-146194
-
|
Reactive Oxygen Species (ROS)
|
Cancer
|
NHEJ inhibitor-1 (Compound C2) is a trifunctional Pt(II) complex, alleviates the non-homologous end connection (NHEJ)/homologous recombination (HR)-related double strand breaks (DSBs) repairs to evade Cisplatin-resistance in non-small cell lung cancer (NSCLC). NHEJ inhibitor-1 inhibits the damage repair proteins Ku70 and Rad51 to make tumors re-sensitive to Cisplatin. NHEJ inhibitor-1 also induces ROS generation and MMP deduction .
|
-
- HY-142283
-
|
Isotope-Labeled Compounds
EGFR
|
Cancer
|
Dosimertinib-d3-d3 is a potent and orally active EGFR inhibitor. Dosimertinib-d3-d3 decreases the expression of p-EGFR and p-ERK protein levels. Dosimertinib-d3-d3 shows antiproliferative and anti-tumor activity. Dosimertinib-d3-d3 has the potential for the research of non-small-cell lung cancer (NSCLC) .
|
-
- HY-149695
-
|
EGFR
|
Cancer
|
EGFR-IN-91 (compound 9) is an orally available EGFR inhibitor with blood-brain barrier penetrability. EGFR-IN-91 inhibits EGFR L858R/C797S and EGFR exon 19del/C797S, inducing tumor regression in xenograft (PDX) mouse models. EGFR-IN-91 has the potential to inhibit localized and metastatic non-small cell lung cancer (NSCLC) driven by EGFR mutants .
|
-
- HY-119307R
-
|
MMP
TNF Receptor
|
Cancer
|
Apratastat (Standard) is the analytical standard of Apratastat. This product is intended for research and analytical applications. Apratastat (TMI-005) is an orally active, non-selective and reversible TACE/MMPs inhibitor, can inhibit inhibit the release of TNF-α. Apratastat has the potential to overcome radiotherapy-resistance in non-small cell lung cancer (NSCLC) . Apratastat is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-153863
-
|
PROTACs
MEK
Raf
|
Cancer
|
MS934 is a novel improved VHL-recruiting MEK 1/2 PROTAC degrader. MS934 also degrades CRAF. MS934 can be used for the research of variety of human cancers, such as melanoma, nonsmall cell lung cancer (NSCLC), colorectal cancer, primary brain tumors, and hepatocellular carcinoma (Pink: Target protein ligand (HY-168288); Black: linker (HY-168289); Blue: E3 ligase ligand (HY-112078)) .
|
-
- HY-114277R
-
|
Ras
|
Cancer
|
Sotorasib (Standard) is the analytical standard of Sotorasib. This product is intended for research and analytical applications. Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C‑mutated locally advanced or metastatic non‑small cell lung cancer (NSCLC) .
|
-
- HY-14463
-
AT13387
|
HSP
|
Cancer
|
Onalespib (AT13387) is a potent and cross the blood-brain barrier heat-shock-protein-90 (Hsp90) inhibitor. Onalespib inhibits the proliferation, survival and migration. Onalespib decreases the expression of EGFR, p-EGFR, AKT, P-AKT, ERK1/2, P-ERK1/2, S6, P-S6 protein. Onalespib shows antitumor activity. Onalespib has the potential for the research of non-small cell lung cancer (NSCLC) .
|
-
- HY-176556
-
|
EGFR
|
Cancer
|
EGFR-IN-1671 is a selective EGFR inhibitor with an IC50 of 0.19 nM. EGFR-IN-167 exhibits good potency against various EGFR mutants (IC50 = 0.109 nM, 0.75 nM and <0.05 nM against EGFR (L858R), EGFR (C797S) and EGFR (del19), respectively). EGFR-IN-1671 covalently engages the catalytically conserved lysine of EGFR in live mammalian cells. EGFR-IN-1671 demonstrates excellent anti-proliferative activity by inhibiting EGFR autophosphorylation. EGFR-IN-1671 can be used for the study of non-small-cell lung carcinomas (NSCLC), glioblastoma and many solid tumors .
|
-
- HY-10261E
-
(R)-BIBW 2992
|
EGFR
c-Met/HGFR
p38 MAPK
|
Cancer
|
(R)-Afatinib ((R)-BIBW 2992) is the Afatinib isomer. Afatinib (HY-10261) is an orally active, potent and irreversible dual specificity inhibitor of?ErbB?family (EGFR?and?HER2), with?IC50?values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for?EGFR wt, EGFR L858R,?EGFR L858R/T790M?and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung?cancer?(NSCLC) and gastric?cancer .
|
-
- HY-156671A
-
|
Ras
PI3K
ERK
mTOR
Apoptosis
|
Cancer
|
RMC-4998 formic is an orally active inhibitor targeting the active or GTP-bound state of the KRAS G12C mutant. RMC-4998 formic can form a ternary complex with intracellular CYPA and the activated KRAS G12C mutant, with an IC50 value of 28 nM. RMC-4998 formic can inhibit ERK signaling in KRAS G12C mutant cancer cells and induce apoptosis. RMC-4998 formic can be used for tumor research .
|
-
- HY-158006
-
|
MetAP
|
Cancer
|
SDX-7539 is a selective inhibitor for Methionine aminopeptidase type 2 (MetAP2). SDX-7539 inhibits proliferarion of HUVECs with an IC50 of 120 μM. SDX-7539 exhibits antitumor activity in NSCLC xenograft athymic nude mice .
|
-
- HY-50895G
-
ZD1839
|
EGFR
Autophagy
Apoptosis
|
Cancer
|
Gefitinib (ZD1839) (GMP) is Gefitinib (HY-50895) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Gefitinib is a potent, selective and orally active EGFR tyrosine kinase inhibitor .
|
-
- HY-164307
-
BLU 451; LNG-451
|
EGFR
|
Cancer
|
Pebezertinib (BLU 451) is an orally active inhibitor for EGFR. Pebezertinib exhibits the ability to penetrate the central nervous system (CNS). Pebezertinib can be used for research about non-small cell lung cancer carrying EGFR exon 20 insertion .
|
-
- HY-10224A
-
LBH589 lactate; NVP-LBH589 lactate
|
HDAC
HIV
Autophagy
Apoptosis
|
Infection
Cancer
|
Panobinostat lactate is a potent and orally active non-selective HDAC inhibitor. Panobinostat lactate has antineoplastic activities. Panobinostat lactate effectively disrupts HIV latency. Panobinostat lactate induces cell apoptosis and autophagy. Panobinostat lactate can be used for the study of refractory or relapsed multiple myeloma .
|
-
- HY-156671
-
|
Ras
PI3K
ERK
mTOR
Apoptosis
|
Cancer
|
RMC-4998 is an orally active inhibitor targeting the active or GTP-bound state of the KRAS G12C mutant. RMC-4998 can form a ternary complex with intracellular CYPA and the activated KRAS G12C mutant, with an IC50 value of 28 nM. RMC-4998 can inhibit ERK signaling in KRAS G12C mutant cancer cells and induce apoptosis. RMC-4998 can be used for tumor research .
|
-
- HY-169982
-
|
EGFR
|
Cancer
|
EGFR-IN-136 (compound 21v) is a potent EGFR inhibitor with IC50 values of 20.2, 1.2, 2.3, 12.5 nM for EGFR WT, EGFR LR/TM, EGFR 19D/TM/CS, EGFR LR/TM/CS, respectively. EGFR-IN-136 shows antiproliferative activity. EGFR-IN-136 shows antitumor activity and has the potential for the research of NSCLC .
|
-
- HY-161923
-
|
EGFR
Apoptosis
Akt
ERK
|
Cancer
|
EGFR-IN-120 (Compound 11eg) is an orally active EGFR inhibitor. EGFR-IN-120 inhibits EGFR L858R/T790M/C797S with an IC50 value of 0.053 μM, and has a relatively weak effect on EGFR WT (IC50: 1.05 μM). EGFR-IN-120 inhibits the phosphorylation of EGFR and main downstream effectors (STAT3, AKT, and Erk). EGFR-IN-120 induces cell cycle arrest and cell apoptosis in EGFR mutant cells. EGFR-IN-120 inhibits the proliferation of the NSCLC cells harboring EGFR L858R/T790M/C797S with an IC50 of 0.052 μM .
|
-
- HY-170438
-
|
EGFR
|
Cancer
|
EGFR-IN-139 (compound PD 18) is an epidermal growth factor receptor (EGFR) inhibitor, with IC50s of 12.88 (wild type), 10.84 (L858R/T790M), 42.68 (L858R/T790M/C797S) nM, respectively. EGFR-IN-139 displays strong anticancer activity against A549 and H1975 cancer cell lines, which are highly expressed EGFR. EGFR-IN-139 has a strong selectivity to cancer cells. EGFR-IN-139 can be used for nonsmall cell lung cancer (NSCLC) research[1].
|
-
- HY-125847
-
|
Ras
PI3K
Akt
Caspase
Apoptosis
Bcl-2 Family
NF-κB
MMP
|
Cancer
|
Salvianolic acid F is a KRAS inhibitor, especially for KRAS G12D. Salvianolic acid F inhibits NF-kB, MMP-9, and NO simultaneously. Salvianolic acid F inhibits cancer cell growth, invasion, and migration and induces apoptosis via the EP300/PI3K/AKT pathway in vitro. Salvianolic acid F inhibits the growth of KRAS-dependent lung cancer cells via the PI3K/AKT signaling pathway in vivo. Salvianolic acid F can be used in the research of various cancers, including KRAS G12D-driven non-small cell lung cancer (NSCLC) and ovarian cancer .
|
-
- HY-164476
-
|
EGFR
GSK-3
PD-1/PD-L1
|
Cancer
|
ES-072 is an orally effective selective EGFR mutant (EGFR-T790M) inhibitor. ES-072 activates GSK3α by inhibiting EGFR-T790M activity, which promotes phosphorylation of PD-L1 at Ser279 and Ser283. The phosphorylated PD-L1 recruits the E3 ubiquitin ligase ARIH1, leading to ubiquitination and proteasomal degradation of PD-L1. This mechanism not only reduces cancer cell growth but also enhances anti-tumor immune response by lowering PD-L1 levels. ES-072 can be used to inhibit proliferation in non-small cell lung cancer (NSCLC) cells .
|
-
- HY-114277S
-
AMG-510-d7
|
Isotope-Labeled Compounds
Ras
|
Cancer
|
Sotorasib-d7 (AMG-510-d7) is a deuterium-labeled Sotorasib (HY-114277). Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C‑mutated locally advanced or metastatic non‑small cell lung cancer (NSCLC) .
|
-
- HY-172392
-
|
MNK
Ribosomal S6 Kinase (RSK)
|
Cancer
|
HSND80 (Compound 1) is an orally active inhibitor of MNK/p70S6K, with Kd values of 44 nM against MNK1 and 4 nM against MNK2. HSND80 has a longer target residence time of 45 mins and 58 mins against MNK1 and MNK2 respectively. HSND80 can suppress non-small cell lung cancer (NSCLC) both in vitro and in vivo, and suppress Triple-Negative Breast Cancer (TNBC) in vitro .
|
-
- HY-114277S2
-
AMG-510-d3
|
Isotope-Labeled Compounds
Ras
|
Cancer
|
Sotorasib-d3 (AMG-510-d3) is deuterium labeled Sotorasib. Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C?mutated locally advanced or metastatic non?small cell lung cancer (NSCLC) .
|
-
- HY-148260
-
|
Ras
|
Cancer
|
KRAS G12D inhibitor 16 is a KRAS G12D inhibitor. KRAS G12D inhibitor 16 has inhibitory activity against KRAS G12D and KRAS G12D mutation with IC50 value of 0.7 nM and 0.35 μM, respectively. KRAS G12D inhibitor 16 can be used for the research of many malignant tumor, such as pancreatic ductal adenocarcinomas (PDAC), colon and rectal carcinomas (CRC), non-small cell lung carcinomas (NSCLC) .
|
-
- HY-134877
-
|
EGFR
ERK
Akt
|
Cancer
|
BAY 2476568 is a potent and mutant-selective inhibitor targeting EGFR exon20 insertion variants. BAY 2476568 potently inhibits the kinase activity of EGFR exon20 insertion mutants (insASV, insSVD, insNPG) with IC50 values of 0.09 nM, 0.21 nM, and 0.11 nM, respectively. BAY 2476568 inhibits EGFR (Y1068) phosphorylation and reduces the phosphorylation of ERK1/2 and Akt (S473) in Ba/F3 cells expressing EGFR exon20 insertion mutants (insASV, insSVD). BAY 2476568 can be used for the study of non-small cell lung cancer (NSCLC) driven by EGFR exon20 insertion mutations .
|
-
- HY-173237
-
|
CDK
Epigenetic Reader Domain
|
Cancer
|
CDK4/6/BRD4-IN-1 (B15) is an inhibitor of CDK4, CDK6 and BRD4, with IC50 values of 220 nM, 146 nM, 106 nM and 85 nM for BRD4-BD2, BRD4-BD1, CDK6 and CDK4, respectively. CDK4/6/BRD4-IN-1 (B15) can be used in the study of NSCLC (Non-Small Cell Lung Cancer). CDK4/6/BRD4-IN-1 (B15) induces cell cycle arrest and apoptosis .
|
-
- HY-P99284
-
MK-0646; h7C10
|
IGF-1R
Apoptosis
|
Cancer
|
Dalotuzumab (MK-0646) is a recombinant humanized monoclonal antibody (IgG1 type) targeting IGF-1R. Dalotuzumab acts by inhibiting IGF-1- and IGF-2-mediated tumor cell proliferation, IGF-1R autophosphorylation, and Akt phosphorylation. Dalotuzumab also induces apoptosis and cycle arrest. Dalotuzumab in combination with other anticancer agents such as statins can enhance the antitumor activity of Dalotuzumab in vitro and in vivo .
|
-
- HY-124295
-
ABT-301; MPT0E028; TMU-C-0012
|
HDAC
Akt
Apoptosis
|
Inflammation/Immunology
Cancer
|
Imofinostat (ABT-301; MPT0E028) is an orally active and selective HDAC inhibitor with IC50s of 53.0 nM, 106.2 nM, 29.5 nM for HDAC1, HDAC2 and HDAC6, respectively. Imofinostat has a weak inhibitory effect on HDAC8 (IC50 of 2.5 μM), but no inhibitory effect on HDAC4 (IC50>10 μM). Imofinostat reduces the viability of B-cell lymphomas by inducing apoptosis and possesses potent direct Akt targeting ability and reduces Akt phosphorylation in B-cell lymphoma. Imofinostat has a broad-spectrum antitumor activity, including colorectal cancer, B-cell lymphoma, non-small cell lung carcinoma (NSCLC), and pancreatic cancer, while also showing therapeutic potential in non-tumor diseases like emphysema and pulmonary fibrosis .
|
-
- HY-155721
-
22-(4′-Pyridinecarbonyl) jorunnamycin A
|
Akt
mTOR
|
Cancer
|
22-(4′-py)-JA is a semisynthetic derivative of junamycin A (JA) that can be isolated from the Thai blue sponge (Xestospongia sp.). 22-(4′-py)-JA has antimetastatic activity and can inhibit AKT/mTOR/p70S6K signaling. 22-(4′-py)-JA inhibits tumor cell invasion and tube formation in human umbilical vein endothelial cells (HUVEC), downregulates metalloproteinases (MMP-2 and MMP-9), hypoxia-inducible factor 1α (HIF-1α) and vascular endothelial growth factor (VEGF). 22-(4′-py)-JA has potent anticancer activity against non-small cell lung cancer (NSCLC) .
|
-
- HY-113916
-
AT13387 lactate
|
HSP
|
Cancer
|
Onalespib lactate is a potent and cross the blood-brain barrier heat-shock-protein-90 (Hsp90) inhibitor with an Kd value of 0.71 nM. Onalespib lactate inhibits the proliferation, survival and migration. Onalespib lactate decreases the expression of EGFR, p-EGFR, AKT, P-AKT, ERK1/2, P-ERK1/2, S6, P-S6 protein. Onalespib lactate shows antitumor activity. Onalespib lactate has the potential for the research of non-small cell lung cancer (NSCLC) .
|
-
- HY-170995
-
|
PROTACs
ROR
Apoptosis
|
Cancer
|
PROTAC ROR1 degrader-1 (Compound 11d) is a PROTAC degrader for pseudokinase ROR1 that degrades ROR1 in NSCLC cells with a DC50s of 40-80 nM. PROTAC ROR1 degrader-1 causes the cleavage of PARP and induces apoptosis in NCI-H23 . (Pink: ligand for target protein ROR1 ligand-1 (HY-170996); Black: linker (HY-W014787); Blue: ligand for VHL E3 ligase (S,R,S)-AHPC (HY-125845))
|
-
- HY-E70714
-
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
EML4-ALK is a fusion-type protein tyrosine kinase produced through gene rearrangement. EML4-ALK can be used for the study of non-small cell lung carcinoma (NSCLC) and neuroblastoma (NB). EML4-ALK has multiple mutants. EML4 ALK F1174L Recombinant Human Active Protein Kinase is a recombinant EML4 ALK F1174L protein that can be used to study EML4 ALK F1174L-related functions .
|
-
- HY-142870
-
|
Pyruvate Carboxylase (PC)
Apoptosis
β-catenin
ERK
Wnt
|
Cancer
|
ZY-444 is an anti-cancer agent, targeting pyruvate carboxylase (PC). ZY-444 suppresses the Wnt/β-catenin/Snail signaling pathway by blocking nuclear translocation of β-catenin. ZY-444 selectively inhibits proliferation, migration, and invasion and induces apoptosis in cancer cells. ZY-444 exhibits potent anti-tumor in cancer mouse models. ZY-444 can be used for the study of breast cancer, lung cancer (NSCLC), prostate cancer and iodine-refractory thyroid cancer .
|
-
- HY-159006
-
|
Cytochrome P450
|
Cancer
|
CYP1B1 ligand 3 (Compound A1) is a selective inhibitor for cytochrome P450 enzyme CYP1B1 with an IC50 of 11.9 nM. CYP1B1 ligand 3 can be utilized for the synthesis of PROTAC CYP1B1 degrader-2 (HY-158429) .
|
-
- HY-158429
-
|
PROTACs
Cytochrome P450
|
Cancer
|
PROTAC CYP1B1 degrader-2 (compound PV2) is a von Hippel-Landau (VHL) E3 ligase-based CYP1B1 degrader with the DC50 of 1.0 nM at 24 h in A549/Taxol cells. PROTAC CYP1B1 degrader-2 inhibits growth, migration, and invasion of A549/Taxol cell(Sturcture Note:(Blue: VHL ligand (HY-112078), Black: linker (HY-W007700), Pink: CYP1B1 ligand (HY-159006) .
|
-
- HY-114277A
-
AMG-510 racemate
|
Ras
p38 MAPK
|
Cancer
|
Sotorasib racemate (Compound A) is an orally active racemate of Sotorasib (HY-114277), a covalent inhibitor of KRAS G12C mutant which induces adaptive feedback activation of MAPK pathway. Sotorasib racemate also exerts inhibitor activity against KRAS G12C induced cancer and can be applied to cancer research .
|
-
- HY-N7694
-
|
TGF-β Receptor
JAK
STAT
Apoptosis
|
Inflammation/Immunology
Cancer
|
Isotoosendanin is an orally active TGFβR1 inhibitor and abrogating its kinase activity (IC50 = 6732 nM). Isotoosendanin inhibits the JAK/STAT3 signaling pathway by directly targeting SHP-2, enhancing its stability, and reducing its ubiquitination. Isotoosendanin inhibits TGF-β-induced reduces the migration, invasion, and metastasis in triple-negative breast cancer (TNBC) cells. Isotoosendanin exhibits anti-tumor efficacy in TNBC xenograft models and A549 xenograft tumors. Isotoosendanin exhibits significant anti-inflammatory effects in acetic acid-induced vascular permeability and λ-carrageenan-induced hind paw edema tests. Isotoosendanin can be used for the study of non-small cell lung cancer (NSCLC), TNBC and inflammation .
|
-
- HY-161269
-
|
EGFR
|
Cancer
|
EGFR-IN-101 (I-10) is a 2-phenylamino pyrimidine derivative. EGFR-IN-101 is a EGFR inhibitor. The IC50 values for EGFR L858R/T790M/C797S and Ba/F3-EGFR L858R/T790M/C797S are 33.26 and 106.4 nM, respectively. EGFR-IN-101 can be used IN the study of non-small cell lung cancer (NSCLC) .
|
-
- HY-N3610
-
|
nAChR
|
Cancer
|
Coclaurine is a class of tetrahydroisoquinoline alkaloids that can be isolated from Sarcopetalum harveyanum with anticancer activity. Coclaurine is a nicotinic acetylcholine receptor (nAChRs) antagonist. Coclaurine is a key molecule in S. tetrandra responsible for EFHD2 inhibition. Coclaurine can downregulate EFHD2-related NOX4-ABCC1 signaling and enhanced Cisplatin (HY-17394) sensitivity. Coclaurine suppresses the stemness and metastatic properties of NSCLC cells. Coclaurine disrupts the interaction between the transcription factor FOXG1 and the EFHD2 promoter, leading to a reduction in EFHD2 transcription .
|
-
- HY-175527
-
|
PROTACs
Anaplastic lymphoma kinase (ALK)
Apoptosis
|
Cancer
|
ALK degrader 2 is an orally active ALK degrader that degrades EML4-ALK levels (DC50 = 8 nM) and nucleophosmin (NPM)-ALK protein levels (DC50 = 102 nM). ALK degrader 2 mediates ALK degradation via the Hsp70 chaperone system and ubiquitin-proteasome pathway. ALK degrader 2 induces significant S-phase cell cycle arrest and apoptosis in H3122 cells. ALK degrader 2 shows anti-tumor activity in mice bearing H3122 xenografts. ALK degrader 2 can be used for the study of non-small cell lung cancer (NSCLC). (Pink: ALK ligand (HY-W754809), Blue: Hyt (HY-W013021), Black: Linker (HY-Y1760), ALK ligand-linker conjugate (HY-175528)) .
|
-
- HY-159190
-
|
MAPKAPK2 (MK2)
|
Cancer
|
HRX-0233 is a small-molecule MAP2K4 inhibitor. HRX-0233 results in strong tumor shrinkage without any apparent toxicity in H358 KRASG12C-mutant non-small cell lung cancers (NSCLC) in vivo. HRX-0233 efficiently prevents feedback activation of receptor tyrosine kinases (RTKs) upon monotherapy KRAS inhibitor Sotorasib (HY-114277) and causes a more sustained and complete inhibition of MAPK signaling. HRX-0233 is promising for research of AR-negative prostate cancer, lung and colon cancers .
|
-
- HY-N0373
-
|
Amyloid-β
Apoptosis
NOD-like Receptor (NLR)
|
Neurological Disease
|
Licochalcone B is an extract from the root of Glycyrrhiza uralensis. Licochalcone B inhibits amyloid β (42) self-aggregation (IC50=2.16 μM) and disaggregate pre-formed Aβ42 fibrils, reduce metal-induced Aβ42 aggregation through chelating metal ionsLicochalcone B inhibits phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone B inhibits growth and induces apoptosis of NSCLC cells. Licochalcone B specifically inhibits the NLRP3 inflammasome by disrupting NEK7‐NLRP3 interaction .
|
-
- HY-P99109
-
GLS-010; AB-122; WBP-3055
|
PD-1/PD-L1
|
Cancer
|
Zimberelimab (GLS-010) is a fully human IgG4 anti-PD-1 monoclonal antibody with an EC50 of 210 pM for human PD-1. Zimberelimab effectively blocks the binding of PD-L1 and PD-L2 to cell-surface PD-1 in CHO-S cells, with IC50 values of 580 pM and 670 pM, respectively. Zimberelimab shows antitumor activities, and can be used for various cancers research, including cervical cancer, non-small cell lung cancer and classical Hodgkin’s lymphoma .
|
-
- HY-144686
-
|
ATM/ATR
PI3K
mTOR
|
Cancer
|
ATM Inhibitor-3 (compound 34) is a potent and selective ATM inhibitor, with an IC50 of 0.71 nM. ATM Inhibitor-3 shows inhibition of PI3K kinases family. ATM Inhibitor-3 exhibits favorable metabolic stability .
|
-
- HY-116000
-
Gumarontinib; SCC244
|
c-Met/HGFR
|
Cancer
|
Glumetinib (SCC244) is a highly selective, orally bioavailable, ATP-competitive c-Met inhibitor with an IC50 of 0.42 nM. Glumetinib has greater than 2400-fold selectivity for c-Met over those 312 kinases evaluated, including the c-Met family member RON and highly homologous kinases Axl, Mer, TyrO3. Antitumor activity .
|
-
- HY-144687
-
|
ATM/ATR
PI3K
mTOR
|
Cancer
|
ATM Inhibitor-4 (compound 39) is a potent and selective ATM inhibitor, with an IC50 of 0.32 nM. ATM Inhibitor-4 shows stronger inhibition of PI3K kinases family. ATM Inhibitor-4 shows a full inhibition of mTOR at 1 μM. ATM Inhibitor-4 exhibits favorable metabolic stability .
|
-
- HY-123502
-
AZD-6738 formate
|
ATM/ATR
|
Cancer
|
Ceralasertib formate is a potent, selective and orally active ATR inhibitor with an IC50 value of 1 nM. Ceralasertib formate inhibits cell viability and induces DNA damage. Ceralasertib formate induces cell senescence. Ceralasertib formate shows antitumor activity .
|
-
- HY-144685
-
|
ATM/ATR
|
Cancer
|
ATM Inhibitor-2 (compound 7) is a potent and selective ATM inhibitor, with an IC50 of <1 nM .
|
-
- HY-129336
-
LSN3106726
|
CDK
|
Cancer
|
Abemaciclib metabolite M20 (LSN3106726), the active metabolite of Abemaciclib, is a selective CDK4/6 inhibitor for the treatment of cancer .
|
-
- HY-155358
-
|
EGFR
Apoptosis
|
Cancer
|
Os30, a potent fourth-generation EGFR inhibitor, is a potent EGFRC797S-TK inhibitor with IC50 values of 18 nM and 113 nM for EGFRDel19/T790M/C797S TK and EGFRL858R/T790M/C797S TK, respectively. Os30 can suppress EGFR phosphorylation, arrest at G1 phase and induce the apoptosis of KC-0116 (BaF3-EGFRDel19/T790M/C797S) cells. Os30 shows potent antitumor efficacy on non-small cell lung cancer (NSCLC) with EGFmRC797S mutation .
|
-
- HY-171509
-
|
Drug-Linker Conjugates for ADC
Apoptosis
|
Cancer
|
Mal-N(Me)-C6-N(Me)-PNU-159682 (Compound 27), an agent-linker conjugate for ADC, consists the ADC linker Mal-N(Me)-C6-N(Me) and a potent ADC cytotoxin PNU-159682. Mal-N(Me)-C6-N(Me)-PNU-159682 (Compound 27) selectively delivers the payload to CD46-expressing cells, where the linker is cleaved by cathepsin B to release PNU-159682, inducing DNA damage and apoptosis. Mal-N(Me)-C6-N(Me)-PNU-159682 shows durable tumor regression in xenograft (PDX) models of non-small cell lung cancer (NSCLC) and colorectal cancer (CRC) .
|
-
- HY-162098
-
|
PROTACs
Microtubule/Tubulin
Apoptosis
|
Cancer
|
PROTAC tubulin-Degrader-1 is a α/β/β3-tubulin PROTAC degrader. PROTAC tubulin-Degrader-1 exhibits potent anti-proliferative activity against multiple human tumor cell lines. PROTAC tubulin-Degrader-1 induces G2/M phase arrest and apoptosis and inhibits colony formation in A549 and A549/Taxol cells. PROTAC tubulin-Degrader-1demonstrates potent anti-tumor efficacy in A549 and A549/Taxol (Taxol-resistant) xenograft model. PROTAC tubulin-Degrader-1 can be used for the study of non-small cell lung cancer (NSCLC). (Pink: Tubulin ligand (HY-N2146), Blue: CRBN Ligand (HY-10984), Black: Linker (HY-N6056)) .
|
-
- HY-139612
-
JDQ-443; NVP-JDQ443
|
Ras
PERK
|
Cancer
|
Opnurasib (JDQ-443) (NVP-JDQ443) is an orally active, potent, selective, and covalent KRAS G12C inhibitor (extracted from patent WO2021120890A1). Opnurasib shows antitumor activity .
|
-
- HY-107513
-
|
mGluR
|
Neurological Disease
Cancer
|
BAY 36-7620 is a potent and noncompetitive antagonist of mGlu1 Receptor (IC50=0.16 μM) with inverse agonist activity. BAY 36-7620 inhibits tumor growth and prolongs the survival of mice with tumors by inhibiting mGlu1 receptor. BAY 36-7620 suppresses AKT phosphorylation in A549 tumors. BAY 36-762 has neuroprotective effect in acute subdural hematoma rat model.BAY 36-7620 is used in non-small cell lung cancer and breast cancer research .
|
-
- HY-139612A
-
(S)-NVP-JDQ443
|
Ras
PERK
|
Cancer
|
(S)-JDQ-443 is an isomer of JDQ-443 (HY-139612). JDQ-443 is an orally active, potent, selective, and covalent KRAS G12C inhibitor (extracted from patent WO2021120890A1). JDQ-443 shows antitumor activity .
|
-
- HY-E70717
-
|
FGFR
|
Cancer
|
FGFR1 has been implicated in numerous cancer types including non-small cell lung cancer (NSCLC). FGFR1 is activated upon FGF binding to its extracellular domain, resulting in protein dimerization and transautophosphorylation of the intracellular tyrosine kinase domains. FGFR1 V561M gatekeeper mutation drives Fexagratinib (AZD4547) (HY-13330) resistance through STAT3 Activation and EMT. FGFR1 V561M Recombinant Human Active Protein Kinase is a recombinant FGFR1 V561M protein that can be used to study FGFR1 V561M-related functions .
|
-
- HY-121246
-
AKF-PD
|
NF-κB
ERK
TGF-beta/Smad
|
Inflammation/Immunology
Cancer
|
Fluorofenidone (AKF-PD) is an orally active compound with anti-fibrotic, antioxidant, and anti-inflammatory pharmacological effects. Fluorofenidone downregulates the expression of ACSL4, upregulates GPX4 expression and inhibits the NF-κB signaling pathway to alleviate inflammation and fibrosis. Fluorofenidone ameliorates cholestasis and fibrosis by inhibiting hepatic Erk/-Egr-1 signaling and Tgfβ1/Smad pathway in mice. Fluorofenidone demonstrates protective effects against chronic lung injury in mice. Fluorofenidone can be used for the study of chronic obstructive pulmonary disease (COPD), pulmonary interstitial fibrosis (PIF) and non-small cell lung cancer (NSCLC) .
|
-
- HY-172733S
-
|
Isotope-Labeled Compounds
Histone Methyltransferase
|
Cancer
|
PRMT5-MTA-IN-3-d3 (compound P22) is the deuterium labeled PRMT5-MTA-IN-3 (HY-172733). PRMT5-MTA-IN-3-d3 is an orally active PRMT5-MTA inhibitor. PRMT5-MTA-IN-3-d3 has antiproliferative effects on HTC116-MTAP del and wild type colorectal cancer HCT-116 cell lines, with IC50 values of 6 nM and 961 nM, respectively. PRMT5-MTA-IN-3-d3 has anticancer effects, especially for MTAP-deficient tumors, such as non-small cell lung cancer (NSCLC), pancreatic cancer .
|
-
- HY-175252
-
|
PROTACs
EGFR
Apoptosis
|
Cancer
|
PROTAC EGFR degrader 14 is a potent and selective EGFR PROTACdegrader with a DC50 of about 2.9 nM and a Dmax of 93.1% for EGFR L858R/T790M/C797S. PROTAC EGFR degrader 14 selectively induces EGFR C797S degradation through a VHL and proteasome-dependent manner and downregulated EGFR-associated transcriptome and exhibits good selectivity over EGFR WT. PROTAC EGFR degrader 14 induces cell cycle arrest and apoptosis and significantly inhibits tumor growth. PROTAC EGFR degrader 14 can be used for the study of nonsmall cell lung cancer (NSCLC) (Pink: Target protein ligand: (HY-143337); Blue: E3 ligand (HY-125845); Black: Linker (HY-W004688)) .
|
-
- HY-175836
-
|
Cytochrome P450
Apoptosis
|
Cancer
|
CYP1B1-IN-12 is a selective cytochrome P450 1B1 (CYP1B1) inhibitor with an IC50 of 6.05 nM. CYP1B1-IN-12 demonstrates remarkable selectivity, exceeding 1600-fold and 16,000-fold over CYP1A1 and CYP1A2, respectively. CYP1B1-IN-12 can enhance Paclitaxel (HY-B0015)-mediated apoptosis and restore Paclitaxel sensitivity in A549/Taxol-resistant cells. CYP1B1-IN-12 can inhibit the epithelial-mesenchymal transition process and reduce cells migration and invasion. CYP1B1-IN-12 can be used for the research of cancer, such as non-small cell lung cancer (NSCLC) .
|
-
- HY-113471
-
|
Apoptosis
HSV
|
Infection
Inflammation/Immunology
Cancer
|
Perillic acid is the metabolite of Perillyl alcohol (HY-N7000). Perillic acid induces lung cancer cell cycle arrest and apoptosis. Perillic acid shows anti-HSV-1 and immunomodulatory activities .
|
-
- HY-136174
-
|
PARP
|
Cancer
|
RBN-2397 is a potent, accross species and orally active NAD + competitive inhibitor of PARP7 (IC50<3 nM). RBN-2397 selectively binds to PARP7 (Kd=0.001 μM) and restores IFN signaling. RBN-2397 has the potential for the study of advanced or metastatic solid tumors .
|
-
- HY-168893
-
|
Src
Apoptosis
IAP
Survivin
Akt
mTOR
JAK
STAT
Ras
p38 MAPK
|
Cancer
|
K882 (Compound 4e) is a Src inhibitor, with KD of 0.315 μM. K882 induces Apoptosis. K882 inhibits XIAP and Survivin. K882 inhibits the activation of PI3K/Akt/mTOR, Jak1/Stat3, Ras/MAPK signaling pathways. K882 shows anti-tumor activity against non-small cell lung cancer .
|
-
- HY-19617A
-
|
EGFR
|
Cancer
|
EGFR-IN-1 hydrochloride is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 hydrochloride potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 hydrochloride displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity .
|
-
- HY-19617B
-
|
EGFR
|
Cancer
|
EGFR-IN-1 TFA is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity .
|
-
- HY-19617
-
|
EGFR
|
Cancer
|
EGFR-IN-1 (compound 24) is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity .
|
-
- HY-135890
-
-
- HY-121246R
-
|
Reference Standards
NF-κB
ERK
TGF-beta/Smad
|
Inflammation/Immunology
|
Fluorofenidone (Standard) is the analytical standard of Fluorofenidone (AKF-PD) (HY-121246). This product is intended for research and analytical applications. Fluorofenidone is an orally active compound with anti-fibrotic, antioxidant, and anti-inflammatory pharmacological effects. Fluorofenidone downregulates the expression of ACSL4, upregulates GPX4 expression and inhibits the NF-κB signaling pathway to alleviate inflammation and fibrosis. Fluorofenidone ameliorates cholestasis and fibrosis by inhibiting hepatic Erk/-Egr-1 signaling and Tgfβ1/Smad pathway in mice. Fluorofenidone demonstrates protective effects against chronic lung injury in mice. Fluorofenidone can be used for the study of chronic obstructive pulmonary disease (COPD), pulmonary interstitial fibrosis (PIF) and non-small cell lung cancer (NSCLC) .
|
-
- HY-N0373R
-
|
Reference Standards
Amyloid-β
Apoptosis
NOD-like Receptor (NLR)
|
Neurological Disease
|
Licochalcone B (Standard) is the analytical standard of Licochalcone B. This product is intended for research and analytical applications. Licochalcone B is an extract from the root of Glycyrrhiza uralensis. Licochalcone B inhibits amyloid β (42) self-aggregation (IC50=2.16 μM) and disaggregate pre-formed Aβ42 fibrils, reduce metal-induced Aβ42 aggregation through chelating metal ionsLicochalcone B inhibits phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone B inhibits growth and induces apoptosis of NSCLC cells. Licochalcone B specifically inhibits the NLRP3 inflammasome by disrupting NEK7‐NLRP3 interaction .
|
-
- HY-151563A
-
|
Deubiquitinase
|
Cancer
|
OTUB1/USP8-IN-1 TFA is the TFA salt form of OTUB1/USP8-IN-1 (HY-151563). OTUB1/USP8-IN-1 TFA is a dual inhibitor for OTUB1/USP8, IC50 for OTUB1 and USP8 is 0.17 and 0.28 nM, respectively. OTUB1/USP8-IN-1 TFA inhibits proliferation of NSCLC cells. OTUB1/USP8-IN-1 TFA exhibits good pharmacokinetic characters in ICR mouse, and exhibits antitumor activity in H1975 xenograft mouse model .
|
-
- HY-161275
-
|
EGFR
Akt
ERK
Ribosomal S6 Kinase (RSK)
|
Cancer
|
BI-4732 is an orally active, reversible, ATP-competitive EGFR inhibitor with blood-brain barrier penetration. BI-4732 inhibits the kinase activity of EGFR L858R, T790M and C797S with IC50 values of 1 nM while sparing EGFR wild-type. BI-4732 inhibits EGFR and reduces the phosphorylation of AKT, ERK, and S6K. BI-4732 demonstrates excellent intracranial anti-tumor efficacy in YU-1097 xenograft model harboring EGFR_E19del/T790M/C797S. BI-4732 can be used for the study of non-small cell lung cancer (NSCLC) .
|
-
- HY-W018324
-
5hmC
|
Endogenous Metabolite
|
Neurological Disease
Metabolic Disease
Cancer
|
5-Hydroxymethylcytosine (5hmC) is an oxidized forms of 5-methylcytosine (5mC) in mammalian DNA. 5-Hydroxymethylcytosine is produced from 5mC in an enzymatic pathway involving three 5mC oxidases, Ten-eleven translocation (TET)1, TET2, and TET3. The conversion of 5mC into 5hmC can be the first step in a pathway leading towards DNA demethylation. 5-Hydroxymethylcytosine is associated with gene transcription and frequently used as a mark to investigate dynamic DNA methylation conversion during mammalian development. 5-Hydroxymethylcytosine can be used for the study of non-small cell lung cancer (NSCLC), neurodegenerative diseases (Alzheimer’s, Parkinson’s) and hematological malignancies (acute myeloid leukemia, myelodysplastic syndromes) .
|
-
- HY-175839
-
|
PROTACs
EGFR
ATP Synthase
|
Cancer
|
PROTAC EGFR degrader 15 is a Pomalidomide (HY-10984)-based Gefitinib (HY-50895) EGFR PROTAC degrader. PROTAC EGFR degrader 15 triggers EGFR degradation via ubiquitin-proteasome-dependent proteolysis and autophagy-lysosome activation pathways. PROTAC EGFR degrader 15 targets ETFA to enhance ATP production. PROTAC EGFR degrader 15 significantly suppresses tumor growth in a Gefitinib-acquired resistant HCC-827 xenograft model. PROTAC EGFR degrader 15 can be used for the study of non-small cell lung cancer (NSCLC) (Pink: EGFR ligand (HY-W109039); Blue: CRBN ligand (HY-10984); Black: Linker (HY-W679737)) .
|
-
- HY-P99114
-
|
PD-1/PD-L1
|
Cancer
|
Sugemalimab is a fully human, full length, anti-programmed death ligand 1 (PD-L1) immunoglobulin G4 (IgG4) monoclonal antibody (mAb). Sugemalimab shows anticancer activities and can be used for non-small cell lung cancer research .
|
-
- HY-149040
-
(S)-OBI-3424; (S)-TH-3424; AST-3424
|
17β-HSD
|
Cancer
|
Odafosfamide ((S)-OBI-3424) is a highly selective prodrug bis-alkylating agent activated by aldehyde-keto reductase 1C3 (AKR1C3(). Odafosfamide is highly cytotoxic to cell lines with high AKR1C3 expression. Odafosfamide exhibits antitumor activity in a variety of tumors with high AKR1C3 expression (such as liver cancer, non-small cell lung cancer, and leukemia). Odafosfamide can be used in cancer research .
|
-
- HY-N1930
-
Hinesol
|
Apoptosis
|
Cancer
|
(-)-Hinesol (Hinesol) is a potent anticancer agent. (-)-Hinesol induces apoptosis and cell cycle arrest at G0/G1 phase. (-)-Hinesol downregulates MEK/ERK pathway and NF-κB pathway and mediates theexpression of cyclin D1, Bax and Bcl-2. (-)-Hinesol has the potential for the research of non–small cell lung cancer .
|
-
- HY-121246S
-
AKF-PD-d3
|
Isotope-Labeled Compounds
NF-κB
ERK
TGF-beta/Smad
|
Inflammation/Immunology
Cancer
|
Fluorofenidone-d3 (AKF-PD-d3) is deuterium labeled Fluorofenidone (AKF-PD) (HY-121246). Fluorofenidone is an orally active compound with anti-fibrotic, antioxidant, and anti-inflammatory pharmacological effects. Fluorofenidone downregulates the expression of ACSL4, upregulates GPX4 expression and inhibits the NF-κB signaling pathway to alleviate inflammation and fibrosis. Fluorofenidone ameliorates cholestasis and fibrosis by inhibiting hepatic Erk/-Egr-1 signaling and Tgfβ1/Smad pathway in mice. Fluorofenidone demonstrates protective effects against chronic lung injury in mice. Fluorofenidone can be used for the study of chronic obstructive pulmonary disease (COPD), pulmonary interstitial fibrosis (PIF) and non-small cell lung cancer (NSCLC) .
|
-
- HY-176854
-
|
PI3K
mTOR
|
Cancer
|
PI3K/mTOR-IN-18 (Compound 12) is a highly selective dual PI3K/mTOR inhibitor. PI3K/mTOR-IN-18 shows antitumor effects via competitive binding to PI3Kα (Ki=0.130 nM) and mTOR (Ki=0.111 nM). PI3K/mTOR-IN-18 blocks the PI3K/AKT/mTOR pathway and inhibits tumor cell proliferation (IC50=144 nM). PI3K/mTOR-IN-18 is promising for research of solid tumors (e.g., breast, NSCLC) .
|
-
- HY-174855
-
|
PI3K
mTOR
Apoptosis
Bcl-2 Family
MDM-2/p53
Caspase
|
Cancer
|
PI3K/mTOR-IN-17 is a dual PI3K and mTOR inhibitor with IC50 values of 1.21 μM (PI3K), and 0.21 μM (mTOR). PI3K/mTOR-IN-17 induces cells caspase-mediated apoptosis by arresting their growth in the G1-phase. PI3K/mTOR-IN-17 upregulates the levels of caspases-3, 7, 8, and 9, p53 expression and Bax/Bcl-2 ratio. PI3K/mTOR-IN-17 suppresses the PI3K/mTOR signaling pathway. PI3K/mTOR-IN-17 can be used for research of cancer, such as non-small cell lung cancer (NSCLC) .
|
-
- HY-112823R
-
HS-10296 (Standard)
|
Reference Standards
EGFR
|
Cancer
|
Almonertinib (Standard) is the analytical standard of Almonertinib. This product is intended for research and analytical applications. Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer .
|
-
- HY-W004284R
-
|
Reference Standards
Apoptosis
PI3K
Akt
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
Heptadecanoic acid (Standard) is the analytical standard of Heptadecanoic acid. This product is intended for research and analytical applications. Heptadecanoic acid is an odd-chain saturated fatty acid (OCS-FA) with oral activity. Heptadecanoic acid can inhibit cell proliferation and induce Apoptosis. Heptadecanoic acid has antitumor activity. Heptadecanoic acid is associated with a number of diseases, including coronary heart disease, pre-diabetes and type 2 diabetes, and multiple sclerosis[1].
|
-
- HY-10824
-
PT523
|
Antifolate
Dihydrofolate reductase (DHFR)
|
Cancer
|
Talotrexin (PT523), an analog of Aminopterin (HY-14518), is a nonpolyglutamatable classic antifolate. Talotrexin is a RFC (reduced folate carrier) specific inhibitor and selectively inhibits RFC transport. Talotrexin shows antitumor activity by targeting DHFR to inhibit tumor growth .
|
-
- HY-112823
-
HS-10296
|
EGFR
|
Cancer
|
Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer .
|
-
- HY-W004284
-
|
Apoptosis
PI3K
Akt
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
Heptadecanoic acid is an odd-chain saturated fatty acid (OCS-FA) with oral activity. Heptadecanoic acid can inhibit cell proliferation and induce Apoptosis. Heptadecanoic acid has antitumor activity. Heptadecanoic acid is associated with a number of diseases, including coronary heart disease, pre-diabetes and type 2 diabetes, and multiple sclerosis .
|
-
- HY-112823B
-
HS-10296 hydrochloride
|
EGFR
|
Cancer
|
Almonertinib (HS-10296) hydrochloride is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib hydrochloride shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib hydrochloride is used for the research of the non-small cell lung cancer .
|
-
- HY-10824A
-
PT523 monoammonium
|
Dihydrofolate reductase (DHFR)
Antifolate
|
Cancer
|
Talotrexin monoammonium is the monoammonium salt form of Talotrexin (HY-10824). Talotrexin monoammonium is an analog of Aminopterin (HY-14518), and is a nonpolyglutamatable classic antifolate. Talotrexin monoammonium is a reduced folate carrier (RFC) specific inhibitor and selectively inhibits RFC transport. Talotrexin monoammonium shows antitumor activity by targeting DHFR to inhibit tumor growth .
|
-
- HY-170928
-
|
EGFR
Anaplastic lymphoma kinase (ALK)
Cytochrome P450
|
Cancer
|
DA-0157 is the orally active inhibitor for EGFR and ALK that overcomes drug-resistant mutations of EGFR C797S and ALK in NSCLC) cells. DA-0157 inhibits the proliferation of Ba/F3-EGFR Del19/T790M/C797S (IC50 = 6.9 nM), Ba/F3-EGFR WT (IC50 = 0.83 μM), Ba/F3-EML4-ALK-L1196M (IC50 = 5.5 nM), and Ba/F3-EML4-ALK (IC50 = 7.4 nM). DA-0157 inhibits CYP2D6 with IC50 of 5.26 μM. DA-0157 exhibits antitumor efficacy in mouse models .
|
-
- HY-120387
-
|
ROS Kinase
Anaplastic lymphoma kinase (ALK)
TAM Receptor
c-Met/HGFR
|
Cancer
|
SMU-B is the orally active inhibitor for ALK (IC50<0.5 nM), c-ros oncogene 1 (ROS1), c-MET (IC50=1.87 nM) and AXL (IC50=28.9 nM). SMU-B inhibits the proliferation of MKN45, H1993 and H441 with IC50s of 0.02 μM, 1.58 μM and 2.82 μM, respectively. SMU-B exhibits antitumor efficacy in mouse models .
|
-
- HY-139920A
-
SH-1028 mesylate
|
EGFR
|
Cancer
|
Oritinib (SH-1028) mesylate is a selective, orally active, and pyrimidine-based irreversible inhibitor of EGFR with an IC50 of 18 nM. Oritinib (SH-1028) mesylate exhibits potent activity against EGFR sensitive and resistant (T790 M) mutations. Oritinib (SH-1028) mesylate significantly inhibits proliferation of tumor cells with EGFR sensitive and resistant mutation .
|
-
- HY-146293
-
|
HDAC
HSP
|
Cancer
|
HDAC6/HSP90-IN-1 (compound 17) is a potent and selective dual inhibitor of HDAC6 and HSP90, with IC50 values of 4.3 and 46.8 nM, respectively. HDAC6/HSP90-IN-1 down-regulates PD-L1 expression in INF-γ treated H1975 lung cancer cells. HDAC6/HSP90-IN-1 inhibits tumor growth in human H1975 xenograft mice .
|
-
- HY-W018324S
-
5hmC-13C,d2
|
Isotope-Labeled Compounds
|
Neurological Disease
|
5-Hydroxymethylcytosine- 13C,d2 is the 13C and deuterium labeled 5-Hydroxymethylcytosine (HY-W018324). 5-Hydroxymethylcytosine (5hmC) is an oxidized forms of 5-methylcytosine (5mC) in mammalian DNA. 5-Hydroxymethylcytosine is produced from 5mC in an enzymatic pathway involving three 5mC oxidases, Ten-eleven translocation (TET)1, TET2, and TET3. The conversion of 5mC into 5hmC can be the first step in a pathway leading towards DNA demethylation. 5-Hydroxymethylcytosine is associated with gene transcription and frequently used as a mark to investigate dynamic DNA methylation conversion during mammalian development. 5-Hydroxymethylcytosine can be used for the study of non-small cell lung cancer (NSCLC), neurodegenerative diseases (Alzheimer’s, Parkinson’s) and hematological malignancies (acute myeloid leukemia, myelodysplastic syndromes) .
|
-
- HY-P99719
-
BAY 1129980; Anti-C4.4a antibody-drug conjugates
|
Antibody-Drug Conjugates (ADCs)
|
Cancer
|
Lupartumab Amadotin (BAY 1129980) is an antibody–drug conjugate (ADC) consisting of a fully human C4.4A (LYPD3)-targeting mAb (BAY 1135626) (HY-147281) conjugated to a novel, highly potent derivative of the microtubule-disrupting cytotoxic drug auristatin via a noncleavable alkyl hydrazide linker. Lupartumab Amadotin can be used for the research of non-small cell lung cancer .
|
-
- HY-175235
-
|
MEK
|
Metabolic Disease
|
MEK4 IN-3 (Compound 39) is a selective MEK4 inhibitor with IC50s of 78 and 2920 nM for MEK4 and RSK4, respectively. MEK4 IN-3 reduces toxicity in cells. MEK4 IN-3 can be used for liver failure, particularly nonalcoholic fatty liver disease (NAFLD) research .
|
-
- HY-109061B
-
YH25448 mesylate; GNS-1480 mesylate
|
EGFR
Akt
ERK
|
Cancer
|
Lazertinib (mesylate) (YH25448 (mesylate); GNS-1480 (mesylate)) is an orally active EGFR inhibitor that can penetrate the blood-brain barrier. Lazertinib (mesylate) inhibits p-EGFR, p-AKT and p-ERK signaling pathways, leading to apoptosis. Lazertinib (mesylate) has anti-tumor activity in the mouse H1975-luc BM xenograft model. Lazertinib (mesylate) can be used in the study of non-small cell lung cancer .
|
-
- HY-177021
-
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
Tubulin-IN-51 is an orally available, potent tubulin inhibitor (IC50 = 31 nM). Tubulin-IN-51 promotes tubulin polymerization in vitro and does not compete with Paclitaxel (HY-B0015) for binding. Tubulin-IN-51 inhibits the binding of Vinblastine (HY-13780) to tubulin. Tubulin-IN-51 downregulates the proportion of cells in the G1 phase and induces apoptosis. Tubulin-IN-51 inhibits tumor growth in multiple nude mouse xenograft models .
|
-
- HY-P10757
-
-
- HY-P9971
-
SHR-1210
|
PD-1/PD-L1
|
Cancer
|
Camrelizumab (SHR-1210) is a potent humanied high-affinity IgG4-κ monoclonal antibody (mAb) to PD-1. Camrelizumab binds PD-1 at a high affinity of 3 nM and inhibits the binding interaction of PD-1 and PD-L1 with an IC50 of 0.70 nM. Camrelizumab acts as anti-PD-1/PD-L1 agent and can be used for cancer research, including NSCLC, ESCC, Hodgkin lymphoma, and advanced HCC et,al .
|
-
- HY-19357
-
-
-
-
HY-L075
-
|
2,449 compounds
|
Lung cancer is a major global health problem, as it is the leading cause of cancer-related deaths worldwide. Lung cancer is divided into two categories: small cell lung cancer and non-small cell lung cancer (NSCLC). Non-small cell lung cancer accounts for about 85 percent of lung cancers.
As with all cancers, lung cancer may be treated with surgery, chemotherapy, radiation therapy, targeted therapy, immunotherapy or a combination thereof. Targeted therapy is one of the most exciting developments in lung cancer medicine, especially for NSCLC. Extensive genomic characterization of NSCLC has led to the identification of molecular subtypes of NSCLC that are oncogene addicted and exquisitely sensitive to targeted therapies. These include activating mutations in epidermal growth factor receptor (EGFR) and BRAF or echinoderm microtubule-associated protein-like 4 (EML4)-anaplastic lymphoma kinase (ALK) fusions and ROS1 receptor tyrosine kinase fusions. These are important targets for target therapy.
MCE offers a unique collection of 2,449 compounds with identified and potential anti-lung cancer activity. These compounds target lung cancer’s major targets and signaling pathways. MCE anti-lung cancer compound library is a useful tool for anti-lung cancer drugs screening and other related research.
|
Cat. No. |
Product Name |
Type |
-
- HY-50895G
-
ZD1839 (GMP)
|
Fluorescent Dye
|
Gefitinib (ZD1839) (GMP) is Gefitinib (HY-50895) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Gefitinib is a potent, selective and orally active EGFR tyrosine kinase inhibitor .
|
Cat. No. |
Product Name |
Type |
-
- HY-50895G
-
ZD1839 (GMP)
|
Biochemical Assay Reagents
|
Gefitinib (ZD1839) (GMP) is Gefitinib (HY-50895) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Gefitinib is a potent, selective and orally active EGFR tyrosine kinase inhibitor .
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P5005
-
|
CMV
PD-1/PD-L1
|
Infection
Inflammation/Immunology
Cancer
|
VIPhyb is a vasoactive intestinal polypeptide (VIP) receptor antagonist. VIPhyb can inhibit VIP signaling, increase T-cell immunity and downregulate PD1. VIPhyb can inhibit cancer cell proliferation. VIPhyb can reduce inflammatory cytokine expression. VIPhyb can enhance viral clearance. VIPhyb can be used for the researches of cancer, infection and inflammation and immunology, such as non-small cell lung cancer (NSCLC), cytomegalovirus infection and colitis .
|
-
- HY-P10944
-
NNS309
|
FAP
|
Cancer
|
Unlabeled FXX489 (NNS309) is a fibroblast activation protein (FAP)-targeting ligand. Unlabeled FXX489 can be labeled with 68Ga and 177Lu and shows anticancer effects. Unlabeled FXX489 can be used for the study of pancreatic ductal adenocarcinoma (PDAC), non-small cell lung cancer (NSCLC), breast cancer (BC), and colorectal cancer (CRC) .
|
-
- HY-P11110
-
|
PD-1/PD-L1
|
Cancer
|
RK-10 is a PD-L1 binding peptide. RK-10 conjugated with Cy5 (HY-D0821) or Biotin (HY-B0511) can used to detect PD-L1 expressing tumors with flow cytometry or immunohistochemistry. RK-10 can be used for cancers like NSCLC, breast cancer, squamous cell carcinoma and melanoma detection research .
|
-
- HY-P10386
-
|
Bcl-2 Family
|
Cancer
|
155H1 (Compound 11) is a stapled peptide, that covalently binds hMcl1 (172-323) with IC50 of 18 nM .
|
-
- HY-P10757
-
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99202
-
|
Transmembrane Glycoprotein
|
Cancer
|
Vibostolimab is an anti-TIGIT (T cell immunoglobulin and ITIM domain) monoclonal antibody. Vibostolimab shows antitumor activity, and can be used in non-small cell lung cancer (NSCLC) and melanoma research .
|
-
- HY-P99827
-
TSR-022; GSK4069889
|
Tim3
|
Cancer
|
Cobolimab (TSR-022) is an anti-TIM-3 monoclonal antibody. Cobolimab mediates the internalization of TIM3 with an IC50 value of 0.4464 nM. Cobolimab has potential application in solid tumors and non-small cell lung cancer (NSCLC) .
|
-
- HY-P99223
-
MEDI-575
|
PDGFR
|
Cancer
|
Tovetumab (MEDI-575) is an anti-PDGFRα monoclonal antibody that selectively blocks the PDGFRα signal transduction. Tovetumab can be used in the research of glioblastoma and non-small cell lung cancer (NSCLC) .
|
-
- HY-P99705
-
RG-7599; DNIB-0600A; NaPi2b-ADC
|
Antibody-Drug Conjugates (ADCs)
|
Cancer
|
Lifastuzumab vedotin (RG-7599; DNIB0600A) is an antibody-drug conjugate (ADC) that comprises a humanized IgG1 anti-NaPi2b monoclonal antibody (MNIB2126A) and a potent antimitotic agent, monomethyl auristatin E (MMAE), which inhibits cell division by blocking the polymerization of tubulin. Lifastuzumab vedotin has the potential for non-small cell lung cancer (NSCLC) and platinum-resistant ovarian cancer (PROC) research .
|
-
- HY-P99269
-
BIBH 1; Anti-Human FAP Recombinant Antibody
|
FAP
|
Cancer
|
Sibrotuzumab (BIBH 1) is a humanized IgG1 monoclonal antibody targets fibroblast activation protein (FAP). Sibrotuzumab can be used for the research of colorectal cancer and non-small cell lung cancer (NSCLC) .
|
-
- HY-P991669
-
|
Caspase
Apoptosis
|
Cancer
|
IGN523 is an anti-CD98 antibody (hCD98, KD = 0.55 nM). IGN523 induces antibody-dependent cell-mediated cytotoxicity (ADCC) activity, lysosomal membrane permeabilization, and inhibition of essential amino acid transport, ultimately leading to caspase-3 and caspase-7-mediated apoptosis of tumor cells. IGN523 inhibits tumor growth in multiple tumor xenograft models. IGN523 is useful in the research of non-small cell lung cancer (NSCLC), acute myeloid leukemia (AML), and other cancers. .
|
-
- HY-P991620
-
|
Transmembrane Glycoprotein
|
Cancer
|
JS006 is a humanized IgG4κ monoclonal antibody inhibitor targeting TIGIT/CD155. JS006 can be used to study advanced and/or metastatic cancers with resistance to PD-1/PD-L1 inhibitor such as non-small cell lung cancer (NSCLC), advanced lymphoma and advanced/metastatic triple negative breast cancer (TNBC) .
|
-
- HY-P991635
-
|
TNF Receptor
|
Cancer
|
PF-07329640 is a humanized monoclonal antibody inhibitor targeting TNFRSF3. PF-07329640 can be used for advanced/metastatic solid tumors like non-small cell lung cancer (NSCLC) and colorectal cancer (CRC) research .
|
-
- HY-P99921
-
HuMax-AXL-ADC
|
Antibody-Drug Conjugates (ADCs)
TAM Receptor
|
Cancer
|
Enapotamab vedotin is an AXL-targeted antibody-drug conjugate (ADC) with inhibitory potential against high AXL expressing non-small cell lung cancer (NSCLC). Enapotamab vedotin also exhibits resistant to EGFR inhibitor such as Osimertinib (HY-15772) .
|
-
- HY-P991244
-
|
EGFR
|
Cancer
|
REGN-1400 is a humanized monoclonal antibody inhibitor targeting ErbB3. REGN-1400 reduces tumor cell proliferation by inhibiting ErbB3 and blocking related signaling pathways. REGN-1400 is promising for research of solid tumors such as non-small cell lung cancer (NSCLC), colorectal cancer (CRC), and squamous cell carcinoma of the head and neck (SCCHN) .
|
-
- HY-P991612
-
Sym024
|
CD73
|
Inflammation/Immunology
Cancer
|
S095024 is a humanized IgG1 monoclonal antibody inhibitor targeting CD73. S095024 can be used to study acute respiratory distress syndrome (ARDS), non-small cell lung cancer (NSCLC) and advanced solid tumor malignancies .
|
-
- HY-P9986
-
MTIG-7192A; RG-6058
|
CD28
|
Cancer
|
Tiragolumab is an immune checkpoint inhibitor binding to the T-cell immunoglobulin and ITIM domain (TIGIT). Tiragolumab in combination with Atezolizumab (HY-P9904) and Bevacizumab (HY-P9906) has benefit in unresectable hepatocellular carcinoma. Tiragolumab can be used to study non-small cell lung cancer (NSCLC) and melanoma .
|
-
- HY-P991628
-
|
PD-1/PD-L1
VEGFR
|
Cancer
|
SSGJ-707 is a bispecific, recombinant humanized IgG4 monoclonal antibody inhibitor targeting PD-1 and VEGF. SSGJ-707 can be used for cancers research, such as advanced non-small cell lung cancer (NSCLC) and recurrent endometrial cancer
|
-
- HY-P991058
-
BMS-986315
|
Checkpoint Kinase (Chk)
|
Cancer
|
Zimistobart (BMS-986315) is a fully human IgG1 antibody that targets NKG2A. Zimistobart can be used for the study of non-small cell lung cancer (NSCLC). The isotype control for Zimistobart can refer to Human IgG1 kappa, Isotype Control (HY-P99001) .
|
-
- HY-P99961
-
JS004; Icatolimab
|
CD28
|
Cancer
|
Tifcemalimab (JS004) is a humanized anti-BTLA (B and T lymphocyte attenuation factor) monoclonal antibody. Tifcemalimab blocks the interaction of HVEM-BTLA by binding to BTLA, and thus blocks the inhibitory signaling pathway mediated by BTLA. Tifcemalimab can be used in research of cancer, such as lymphoma and non-small cell lung cancer (NSCLC) .
|
-
- HY-P99157
-
|
CD276/B7-H3
|
Cancer
|
Omburtamab is a humanized monoclonal antibody targeting B7-H3 (CD276). Omburtamab selectively binds to B7-H3 highly expressed on the surface of tumor cells and activates anti-tumor immune responses mediated by T cells and natural killer (NK) cells. Omburtamab can promote the specific infiltration of CAR-T cells into tumors, enhance the killing function of NK cells through the CD16 signaling pathway, and regulate tumor cell glucose metabolism (such as inhibiting the Warburg effect). Omburtamab has the potential to inhibit solid tumors such as non-small cell lung cancer (NSCLC) .
|
-
- HY-P99379
-
CAN04; Anti-IL-1RAP/IL-1R3 Reference Antibody (nidanilimab)
|
Interleukin Related
|
Cancer
|
Nidanilimab (CAN04) is a fully humanized monoclonal anti-IL1RAP antibody with a Kd value of 1.10 pM. Nidanilimab blocks IL1α and IL1β signaling and stimulates the immune system to destroy tumour cells. Nidanilimab can be used in research of non-small lung cancer (NSCLC) and pancreatic ductal adenocarcinoma (PDAC) .
|
-
- HY-P99117
-
AK104
|
PD-1/PD-L1
CTLA-4
|
Inflammation/Immunology
Cancer
|
Cadonilimab (AK104) is a humanized tetravalent IgG1 bispecific antibody targeting PD1/CTLA4. Cadonilimab blocks both PD-1 and CTLA-4 pathways, thereby relieving their corresponding immunosuppressive effects and reversing tumor specific T cell exhaustion. Cadonilimab significantly downregulates Fc-mediated effector functions, including antibody-dependent cell-mediated cytotoxicity (ADCC), antibody-dependent cellular phagocytosis (ADCP), complement dependent cytotoxicity (CDC). Cadonilimab can be used for research of metastatic cervical cancer, as well as other malignancies such as gastric cancer, GEJ adenocarcinoma and non-small cell lung cancer (NSCLC) .
|
-
- HY-P99284
-
MK-0646; h7C10
|
IGF-1R
Apoptosis
|
Cancer
|
Dalotuzumab (MK-0646) is a recombinant humanized monoclonal antibody (IgG1 type) targeting IGF-1R. Dalotuzumab acts by inhibiting IGF-1- and IGF-2-mediated tumor cell proliferation, IGF-1R autophosphorylation, and Akt phosphorylation. Dalotuzumab also induces apoptosis and cycle arrest. Dalotuzumab in combination with other anticancer agents such as statins can enhance the antitumor activity of Dalotuzumab in vitro and in vivo .
|
-
- HY-P99254
-
1E10
|
Inhibitory Antibodies
|
Inflammation/Immunology
Cancer
|
Racotumomab (Anti-Human NGcGM3 Recombinant Antibody) is an anti-idiotype monoclonal antibody (MAb). Racotumomab reacts to Neu-glycolyl (NeuGc)-containing gangliosides, sulfatides, and other antigens expressed in tumors. Racotumomab is an active anticancer agent for lung cancer .
|
-
- HY-P99109
-
GLS-010; AB-122; WBP-3055
|
PD-1/PD-L1
|
Cancer
|
Zimberelimab (GLS-010) is a fully human IgG4 anti-PD-1 monoclonal antibody with an EC50 of 210 pM for human PD-1. Zimberelimab effectively blocks the binding of PD-L1 and PD-L2 to cell-surface PD-1 in CHO-S cells, with IC50 values of 580 pM and 670 pM, respectively. Zimberelimab shows antitumor activities, and can be used for various cancers research, including cervical cancer, non-small cell lung cancer and classical Hodgkin’s lymphoma .
|
-
- HY-P99114
-
|
PD-1/PD-L1
|
Cancer
|
Sugemalimab is a fully human, full length, anti-programmed death ligand 1 (PD-L1) immunoglobulin G4 (IgG4) monoclonal antibody (mAb). Sugemalimab shows anticancer activities and can be used for non-small cell lung cancer research .
|
-
- HY-P99719
-
BAY 1129980; Anti-C4.4a antibody-drug conjugates
|
Antibody-Drug Conjugates (ADCs)
|
Cancer
|
Lupartumab Amadotin (BAY 1129980) is an antibody–drug conjugate (ADC) consisting of a fully human C4.4A (LYPD3)-targeting mAb (BAY 1135626) (HY-147281) conjugated to a novel, highly potent derivative of the microtubule-disrupting cytotoxic drug auristatin via a noncleavable alkyl hydrazide linker. Lupartumab Amadotin can be used for the research of non-small cell lung cancer .
|
-
- HY-P9971
-
SHR-1210
|
PD-1/PD-L1
|
Cancer
|
Camrelizumab (SHR-1210) is a potent humanied high-affinity IgG4-κ monoclonal antibody (mAb) to PD-1. Camrelizumab binds PD-1 at a high affinity of 3 nM and inhibits the binding interaction of PD-1 and PD-L1 with an IC50 of 0.70 nM. Camrelizumab acts as anti-PD-1/PD-L1 agent and can be used for cancer research, including NSCLC, ESCC, Hodgkin lymphoma, and advanced HCC et,al .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-137295
-
-
-
- HY-N6871
-
|
Infection
Structural Classification
Colophony
Classification of Application Fields
Pinaceae
Ketones, Aldehydes, Acids
Metabolic Disease
Plants
Inflammation/Immunology
Disease Research Fields
|
Bacterial
IKK
Ferroptosis
|
Abietic acid, an orally active diterpene isolated from Colophony, displays significant anti-proliferative, anti-inflammatory, anti-obesity effect, bacteriostatic, cell cycle arresting and pro-apoptotic activities. Abietic acid inhibits lipoxygenase activity for allergy. Abietic acid enhances cell migration and tube formation in HUVECs. Abietic acid induces significant angiogenic potential, which is associated with upregulation of extracellular signal-regulated kinase (ERK) and p38 expression. Abietic acid attenuates sepsis-induced lung injury by inhibiting nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) pathway to inhibit M1 macrophage polarization. Abietic acid exhibits a positive effect against liver injury by attenuating inflammation and ferroptosis. Abietic acid shows accelerated wound closure in a mouse model of cutaneous wounds. Abietic acid significantly reduces the proliferation and growth of NSCLC cells by IKKβ inhibition.Additionally, Abietic acid ameliorates psoriasis-like inflammation and modulates gut microbiota in mice. Abietic acid is promising for research in non-small-cell lung cancer (NSCLC), liver injury-related deseases and psoriasis .
|
-
-
- HY-N4139
-
-
-
- HY-N0429
-
-
-
- HY-N11912
-
-
-
- HY-N3764
-
-
-
- HY-N7459
-
-
-
- HY-N13164
-
-
-
- HY-N2199
-
-
-
- HY-N4139R
-
-
-
- HY-N2993R
-
|
Triterpenes
Structural Classification
Terpenoids
Polyporaceae
Source classification
Poria cocos
Plants
|
Apoptosis
Caspase
PARP
Akt
PTEN
MDM-2/p53
JNK
|
Polyporenic acid C (Standard) is an analytical standard of Polyporenic acid C (HY-N2993). This product is intended for research and analytical applications. Polyporenic acid C is a lanostane-type triterpenoid. Polyporenic acid C can be isolated from Poria cocos. Polyporenic acid C causes the cleavage of caspase-8 and caspase-3, as well as the cleavage of PARP. Polyporenic acid C reduces the phosphorylation level of Akt (Ser473), increases the phosphorylation of PTEN and p53 (Ser15), and activates JNK. Polyporenic acid C induces Apoptosis. Polyporenic acid C shows anticancer activity against non-small cell lung cancer .
|
-
-
- HY-N2993
-
-
-
- HY-W403933R
-
|
Structural Classification
Human Gut Microbiota Metabolites
Microorganisms
Ketones, Aldehydes, Acids
Source classification
Endogenous metabolite
|
Autophagy
Reference Standards
|
Afatinib (Standard) is the analytical standard of Afatinib. This product is intended for research and analytical applications. Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
|
-
-
- HY-125847
-
-
-
- HY-N7694
-
-
-
- HY-N3610
-
|
Alkaloids
Structural Classification
Source classification
Phenols
Polyphenols
Plants
Lauraceae
Isoquinoline Alkaloids
Lindera aggregata (Sims) Kosterm.
|
nAChR
|
Coclaurine is a class of tetrahydroisoquinoline alkaloids that can be isolated from Sarcopetalum harveyanum with anticancer activity. Coclaurine is a nicotinic acetylcholine receptor (nAChRs) antagonist. Coclaurine is a key molecule in S. tetrandra responsible for EFHD2 inhibition. Coclaurine can downregulate EFHD2-related NOX4-ABCC1 signaling and enhanced Cisplatin (HY-17394) sensitivity. Coclaurine suppresses the stemness and metastatic properties of NSCLC cells. Coclaurine disrupts the interaction between the transcription factor FOXG1 and the EFHD2 promoter, leading to a reduction in EFHD2 transcription .
|
-
-
- HY-N0373
-
-
-
- HY-N0373R
-
-
-
- HY-W018324
-
5hmC
|
Structural Classification
Natural Products
Classification of Application Fields
Source classification
Metabolic Disease
Endogenous metabolite
Disease Research Fields
Cancer
|
Endogenous Metabolite
|
5-Hydroxymethylcytosine (5hmC) is an oxidized forms of 5-methylcytosine (5mC) in mammalian DNA. 5-Hydroxymethylcytosine is produced from 5mC in an enzymatic pathway involving three 5mC oxidases, Ten-eleven translocation (TET)1, TET2, and TET3. The conversion of 5mC into 5hmC can be the first step in a pathway leading towards DNA demethylation. 5-Hydroxymethylcytosine is associated with gene transcription and frequently used as a mark to investigate dynamic DNA methylation conversion during mammalian development. 5-Hydroxymethylcytosine can be used for the study of non-small cell lung cancer (NSCLC), neurodegenerative diseases (Alzheimer’s, Parkinson’s) and hematological malignancies (acute myeloid leukemia, myelodysplastic syndromes) .
|
-
-
- HY-N1930
-
-
-
- HY-W004284R
-
-
-
- HY-W004284
-
-
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-142283AS
-
|
Dosimertinib-d5 (mesylate) is a potent and orally active EGFR inhibitor. Dosimertinib-d5 (mesylate) decreases the expression of p-EGFR and p-ERK protein levels. Dosimertinib-d5 (mesylate) shows antiproliferative and anti-tumor activity. Dosimertinib-d5 (mesylate) has the potential for the research of non-small-cell lung cancer (NSCLC) .
|
-
-
- HY-19939S
-
4 Publications Verification
|
VX-984 is an orally active, potent, selective and BBB-penetrated DNA-PK inhibitor. VX-984 efficiently inhibits NHEJ (non-homologous end joining) and increases DSBs (DNA double-strand breaks). VX-984 can be used for glioblastomas (GBM) and non-small cell lung cancer (NSCLC) research. VX-984 is a de novo deuterium .
|
-
-
- HY-114277S
-
|
Sotorasib-d7 (AMG-510-d7) is a deuterium-labeled Sotorasib (HY-114277). Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C‑mutated locally advanced or metastatic non‑small cell lung cancer (NSCLC) .
|
-
-
- HY-142283
-
|
Dosimertinib-d3-d3 is a potent and orally active EGFR inhibitor. Dosimertinib-d3-d3 decreases the expression of p-EGFR and p-ERK protein levels. Dosimertinib-d3-d3 shows antiproliferative and anti-tumor activity. Dosimertinib-d3-d3 has the potential for the research of non-small-cell lung cancer (NSCLC) .
|
-
-
- HY-114277S2
-
|
Sotorasib-d3 (AMG-510-d3) is deuterium labeled Sotorasib. Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C?mutated locally advanced or metastatic non?small cell lung cancer (NSCLC) .
|
-
-
- HY-172733S
-
|
PRMT5-MTA-IN-3-d3 (compound P22) is the deuterium labeled PRMT5-MTA-IN-3 (HY-172733). PRMT5-MTA-IN-3-d3 is an orally active PRMT5-MTA inhibitor. PRMT5-MTA-IN-3-d3 has antiproliferative effects on HTC116-MTAP del and wild type colorectal cancer HCT-116 cell lines, with IC50 values of 6 nM and 961 nM, respectively. PRMT5-MTA-IN-3-d3 has anticancer effects, especially for MTAP-deficient tumors, such as non-small cell lung cancer (NSCLC), pancreatic cancer .
|
-
-
- HY-121246S
-
|
Fluorofenidone-d3 (AKF-PD-d3) is deuterium labeled Fluorofenidone (AKF-PD) (HY-121246). Fluorofenidone is an orally active compound with anti-fibrotic, antioxidant, and anti-inflammatory pharmacological effects. Fluorofenidone downregulates the expression of ACSL4, upregulates GPX4 expression and inhibits the NF-κB signaling pathway to alleviate inflammation and fibrosis. Fluorofenidone ameliorates cholestasis and fibrosis by inhibiting hepatic Erk/-Egr-1 signaling and Tgfβ1/Smad pathway in mice. Fluorofenidone demonstrates protective effects against chronic lung injury in mice. Fluorofenidone can be used for the study of chronic obstructive pulmonary disease (COPD), pulmonary interstitial fibrosis (PIF) and non-small cell lung cancer (NSCLC) .
|
-
-
- HY-W018324S
-
|
5-Hydroxymethylcytosine- 13C,d2 is the 13C and deuterium labeled 5-Hydroxymethylcytosine (HY-W018324). 5-Hydroxymethylcytosine (5hmC) is an oxidized forms of 5-methylcytosine (5mC) in mammalian DNA. 5-Hydroxymethylcytosine is produced from 5mC in an enzymatic pathway involving three 5mC oxidases, Ten-eleven translocation (TET)1, TET2, and TET3. The conversion of 5mC into 5hmC can be the first step in a pathway leading towards DNA demethylation. 5-Hydroxymethylcytosine is associated with gene transcription and frequently used as a mark to investigate dynamic DNA methylation conversion during mammalian development. 5-Hydroxymethylcytosine can be used for the study of non-small cell lung cancer (NSCLC), neurodegenerative diseases (Alzheimer’s, Parkinson’s) and hematological malignancies (acute myeloid leukemia, myelodysplastic syndromes) .
|
-
Cat. No. |
Product Name |
|
Classification |
-
- HY-147858
-
|
|
Alkynes
PROTAC Synthesis
|
PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFR L858R/T790M degrader, with a DC50 of 13.2 nM. PROTAC EGFR degrader 7 inhibits NCI–H1975 cells proliferation, with an IC50 of 46.82 nM. PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI–H1975 cell. PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research . PROTAC EGFR degrader 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
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