Search Result
Results for "
Drug-resistant cancer cells
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-127079
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Microtubule/Tubulin
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Cancer
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Epothilone F is a Microtubule/Tubulin-stabilizing agent with anti-tumor activity. Epothilone F inhibits the proliferation of breast cancer cells, non-small cell lung cancer cells, drug-resistant ovarian cancer cells .
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- HY-162324
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Survivin
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Cancer
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MX106-4C is a survivin inhibitor that selectively kills ABCB1-positive colorectal cancer cells. MX106-4C can exert synergistic anticancer effects with Doxorubicin or resensitize drug-resistant ABCB1 cells to Doxorubicin .
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- HY-151606
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Akt
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Cancer
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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 .
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- HY-P991572
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EGFR
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Cancer
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MM-151 is a humanized IgG1 monoclonal antibody targeting EGFR. MM-151 binds multiple regions of the EGFR extracellular domain (ECD) and reduces its mutations in circulating cell-free tumor DNA with EGFR resistance. MM-151 significantly inhibits EGFR signaling and cell growth. MM-151 can be used for drug-resistant cancers research, such as colorectal, non-small cell lung and triple negative breast cancer .
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- HY-178349
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P-glycoprotein
Apoptosis
Autophagy
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Cancer
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P-gp inhibitor 30 is a potent P-gp inhibitor that reverses multidrug resistance in breast cancer by sensitizing resistant cells to Doxorubicin (ADM) (HY-15142). P-gp inhibitor 30 promotes apoptosis , induces autophagy,and suppresses proliferation, migration, and invasion of drug-resistant breast cancer cells when combined with ADM. P-gp inhibitor 30 inhibits breast tumor growth both in vitro and in vivo. P-gp inhibitor 30 can be used for drug-resistant breast cancer research .
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- HY-N6611
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IGF-1R
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Infection
Inflammation/Immunology
Cancer
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Chimaphilin is an IGF-1R inhibitor (IC50: 0.086 μM). Chimaphilin has antifungal, antioxidant and anticancer activities. Chimaphilin inhibits the growth of both drug-sensitive and drug-resistant osteosarcoma cell lines. Chimaphilin can induce cancer cell apoptosis. Chimaphilin is a main component of pyrola .
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- HY-138627B
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EGFR
Drug Metabolite
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Cancer
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AST5902 mesylate is a principal metabolite of Alflutinib, exhibiting significant antineoplastic activity. AST5902 mesylate contributes to the overall pharmacological effects in the treatment of non-small cell lung cancer. AST5902 mesylate is involved in the response to activating EGFR mutations and can help overcome EGFR T790M drug-resistant mutations.
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- HY-176557
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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-W783446
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S,S-DACH-sulph
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DNA/RNA Synthesis
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Cancer
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S,S-DACH-Pt-SO4 is a platinum based drug. S,S-DACH-Pt-SO4 can cause cellular DNA damage. S,S-DACH-Pt-SO4 is toxic to sensitive cells but shows varying degrees of resistance to drug-resistant cells. S,S-DACH-Pt-SO4 can be used for cancer 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-P10669
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Caspase
Apoptosis
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Cancer
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NDI-Lyso is a lysosome-targeted anticancer agent that induces the formation of rigid long fibers in cancer cell lysosomes through an enzyme-instructed self-assembly (EISA) mechanism catalyzed by cathepsin B. This process triggers lysosomal swelling, membrane permeabilization (LMP), and membrane disruption, ultimately leading to cancer cell apoptosis via a non-classical caspase-independent pathway. NDI-Lyso exhibits significant selective anticancer activity in various cancer cell lines and drug-resistant cancer cells (IC50 ~10 μM) while showing low toxicity to normal cells (IC50 > 60 μM) .
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- HY-103255
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Apoptosis
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Cancer
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CFM-4 is a potent small molecular antagonist of CARP-1/APC-2 binding. CFM-4 prevents CARP-1 binding with APC-2, causes G2M cell cycle arrest, and induces apoptosis with an IC50 range of 10-15 μM. CFM-4 also suppresses growth of drug-resistant human breast cancer cells .
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- HY-155152
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P-glycoprotein
BCRP
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Cancer
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P-gp/BCRP-IN-2 (compound 15) is an oxadiazole derivative and a dual inhibitor of the ABC transporter P-glycoprotein (IC50: 1.6 nM) and BCRP (IC50: 600 nM). P-gp/BCRP-IN-2 also enhances the anti-proliferative effects of Doxorubicin (HY-15142A) in drug-resistant human adenocarcinoma colon cancer cell lines HT29/DX and MDCK-MDR1 cells .
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- HY-138072
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EGFR
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Cancer
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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) .
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- HY-110354
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UCM05
2 Publications Verification
G28UCM
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Fatty Acid Synthase (FASN)
Bacterial
Antibiotic
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Infection
Cancer
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UCM05 (G28UCM) is a potent inhibitor of fatty acid synthase (FASN) shows activity against HER2+ breast cancer xenografts and is active in anti-HER2 drug-resistant cell lines. UCM05 is a Filamentous temperature-sensitive protein Z (FtsZ) inhibitor and inhibits the growth of the Gram-positive bacterium B. subtilis with MIC values of 100 μM but lack activity on the Gram-negative bacterium E. coli.
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- HY-178824
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EGFR
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Cancer
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EGFR-IN-180 (Compound L15) is an EGFR inhibitor. EGFR-IN-180 shows inhibitory activity against EFGR and EGFR harboring the L858R/T790M/C797S triple drug-resistant mutation, with IC50 values of 80.96 nM and 16.43 nM, reapectively. EGFR-IN-180 can be used for the study of non-small cell lung cancer (NSCLC) .
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- HY-178148
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Androgen Receptor
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Endocrinology
Cancer
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AR antagonist 17 is a selective, orally active, low brain-penetrant Androgen Receptor (AR) antagonist (IC50 = 0.010 μM), effectively blocking AR dimerization and nuclear translocation, and demonstrating potent efficacy in several castration-resistant prostate cancer (CRPC) cells. AR antagonist 17 showed superior efficacy against variant drug-resistant AR mutants. AR antagonist 17 can inhibit tumor growth in an LNCaP xenograft model without apparent toxicity. AR antagonist 17 can be used for the study of castration-resistant prostate cancer (CRPC) .
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- HY-19542
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C6-Cer; N-Hexanoylsphingosine
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Apoptosis
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Cancer
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C6 Ceramide (C6-Cer) is a short-chain, cell-permeable ceramide pathway activator with anticancer activity. C6 Ceramide-mediated miR-29b expression participates in the progression of multiple myeloma through suppressing the proliferation, migration and angiogenesis of endothelial cells by targeting Akt signal pathway. C6 Ceramide exhibits multiple anti-cancer properties including cell cycle arrest, Apoptosis, inhibition of tumor growth and enhances the effects of chemotherapy in drug-resistant cancer cells. C6-ceramide can be used as an adjuvant for chemotherapeutic agents, to enhance anti-tumor effects .
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- HY-156632
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KIN-3248
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FGFR
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Cancer
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Resigratinib (KIN-3248) is an irreversible and orally active covalent inhibitor of FGFR1-4 that effectively inhibits wild-type and drug-resistant mutations (such as FGFR2 V565F, FGFR3 V555M). Resigratinib covalently binds to the Cys492 site of FGFR, blocks the FGFR signaling pathway, inhibits tumor cell proliferation and induces apoptosis. Resigratinib can be used for the study of FGFR2/3-driven solid tumors (such as cholangiocarcinoma and bladder cancer) .
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- HY-176269
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Bcr-Abl
ERK
STAT
PARP
Caspase
Apoptosis
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Cancer
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VS1150 (Compound 11) is a BCR-ABL-targeting phosphorylation-inducing chimeric small molecule (PHICS). VS1150 significantly inhibits oncogenic kinase BCR-ABL signaling by inducing inhibitory phosphorylation at its Y253 (EC50: 69 nM), subsequently triggering cell apoptosis. VS1150 also inhibits other oncogenic ABL fusions and drug-resistant mutants like T315I. VS1150 can be used for chronic myeloid leukemia (CML) and other ABL fusion-driven cancers research .
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- HY-101522
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EGFR
BMX Kinase
Btk
MEK
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Cancer
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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 .
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- HY-P11102
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Bacterial
Fungal
HIV
Parasite
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Infection
Cancer
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Temporin-Sha is an antibacterial peptide with extensive biological activity. Temporin-Sha exhibits broad-spectrum antibacterial activity (e.g., against L. ivanovii, MIC = 6.25 μM), and is effective against Gram-negative bacteria (such as Escherichia coli, MIC = 10 μM), including drug-resistant strains (such as Methicillin (HY-121544)-resistant Staphylococcus aureus). Temporin-Sha also has inhibitory effects on Candida albicans (MIC = 25 μM), Saccharomyces cerevisiae (MIC = 12 μM), the pre-flagellated and non-flagellated forms of Leishmania infantum (IC50 = 5-20 μM), and Trypanosoma cruzi (IC50 = 17 μM). Temporin-Sha exhibits antiviral activity against HSV-1 and has anti-cancer effects (cytotoxicity against breast cancer cells MCF-7 and lung cancer cells H460, etc.) .
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- HY-101741
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A-289099
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Microtubule/Tubulin
Apoptosis
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Cancer
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A-259745 is an orally active antimitotic agent that binds to the colchicine-binding site of tubulin. A-259745 exhibits potent in vitro cytotoxic activity against both multi-drug-resistant and non-multi-drug-resistant cancer cell lines, with ED50 values of 0.018 μM against HCT-15 and 0.028 μM against NCI-H460 cell lines. A-259745 inhibits tubulin polymerization, disrupts the dynamic equilibrium of the mitotic spindle, arrests dividing cells in metaphase, and subsequently induces apoptosis. A-259745 shows dose-dependent antitumor efficacy in murine tumor models. A-259745 can be used for the study of cancer .
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- HY-121656
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Endogenous Metabolite
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Cancer
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AKR1C2/3-IN-2 is a potential AKR1C3 inhibitor with selective AKR1C3 activity. AKR1C2/3-IN-2 is able to block AKR1C3-mediated testosterone (T) production and PSA induction, affecting the endocrine activity of prostate cancer cells. AKR1C2/3-IN-2 shows selectivity over other AKR1C enzymes, indicating its potential application in inhibiting drug-resistant prostate cancer. AKR1C2/3-IN-2 has no inhibitory activity against COX isomerases, further emphasizing its specificity as a prostate cancer inhibitory compound .
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- HY-176225
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PROTACs
Src
Estrogen Receptor/ERR
Apoptosis
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BY13 is a SRC-3 PROTAC degrader with a DC50 of 0.031 μM. BY13 selectively blocks the ER signaling pathway over that of androgen receptor (AR)) through down-regulating ERα level. BY13 potently overcomes endocrine resistance in breast cancer by inducing cell cycle arrest in G1 phase and apoptosis, with superior effect over Fulvestrant (HY-13636). BY13 significantly inhibits the growth of drug-resistant breast tumors without obvious toxicity in LCC2 xenograft mice model . Pink: SRC-3 ligand (SI-2) (HY-101447); Blue: CRBN ligase ligand (HY-41547); Black: linker (HY-176226)
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- HY-W766368
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C6-Cer-13C2,d2; N-Hexanoylsphingosine-13C2,d2
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Isotope-Labeled Compounds
Apoptosis
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Cancer
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C6 Ceramide- 13C2,d2 (C6-Cer- 13C2,d2) is the deuterium labeled and 13C-labeled C6 Ceramide (HY-19542). C6 Ceramide (C6-Cer) is a short-chain, cell-permeable ceramide pathway activator with anticancer activity. C6 Ceramide-mediated miR-29b expression participates in the progression of multiple myeloma through suppressing the proliferation, migration and angiogenesis of endothelial cells by targeting Akt signal pathway. C6 Ceramide exhibits multiple anti-cancer properties including cell cycle arrest, Apoptosis, inhibition of tumor growth and enhances the effects of chemotherapy in drug-resistant cancer cells. C6-ceramide can be used as an adjuvant for chemotherapeutic agents, to enhance anti-tumor effects .
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- HY-135748A
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Toll-like Receptor (TLR)
Apoptosis
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Infection
Cancer
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Poly (I:C):Kanamycin (1:1) sodium is an isometric complex of Poly (I:C) (HY-135748) and Kanamycin (HY-16566). Poly(I:C) sodium, a synthetic analog of double-stranded RNA, is a TLR3 and retinoic acid-inducible gene I receptor (RIG-I and b>MDA5) agonist. Poly(I:C) sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses and induce apoptosis in cancer cells . Kanamycin is an orally active antibacterial agent (Gram-negative/positive bacteria) that inhibits translocation and causes miscoding by binding to the 70S ribosomal subunit. Kanamycin shows good inhibitory activity against Mycobacterium tuberculosis (susceptible and drug-resistant) and Klebsiella pneumoniae, and can be used in the research of tuberculosis and pneumonia .
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- HY-165606
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Oct3/4
c-Myc
Apoptosis
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Cancer
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SB-T-1214 (SBT) is a taxane. SB-T-1214 efficiently inhibits expression of stem cell-related genes (Oct4, Sox2, and c-Myc) and induces apoptosis of colon cancer spheroids with drug resistant tumorigenic CD133 +/CD44 + cells. SB-T-1214 strongly represses tumor growth in Pgp+ DLD-1 human colon tumor xenografts mice model. SB-T-1214 can be used for antitumor research, especially against tumors with drug resistance, such as colon, pancreatic and renal cancers .
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- HY-178942
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VEGFR
EGFR
Apoptosis
Bcl-2 Family
Caspase
MDM-2/p53
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Cancer
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EGFR/VEGFR2-IN-9 (Compound 9b) is an inhibitor of VEGFR-2 (IC50 = 1.325 μM) and EGFR (IC50 = 1.891 μM). EGFR/VEGFR2-IN-9 significantly inhibits the proliferation of multiple cancer cell lines, particularly leukemia cells. EGFR/VEGFR2-IN-9 upregulates the expression levels of Bax, caspase-3, and p53, while downregulating the expression of Bcl-2. EGFR/VEGFR2-IN-9 induces apoptosis and arrests the cell cycle in the G1 phase. EGFR/VEGFR2-IN-9 can be used to investigate anti-tumor angiogenesis and multi-drug resistant cancers .
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- HY-146392
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HDAC
Microtubule/Tubulin
Apoptosis
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Cancer
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HDAC-IN-39 (compound 16c) is a potent HDAC inhibitor, with IC50 values of 1.07 μM (HDAC1), 1.47 μM (HDAC2), and 2.27 μM (HDAC3), respectively. HDAC-IN-39 also significantly inhibits microtubule polymerization. HDAC-IN-39 induces cell cycle arrest at the G2/M phase. HDAC-IN-39 displays promising anticancer activity against resistant cancer cells .
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- HY-158106
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CDK
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Cancer
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AZD8421 is a selective CDK2 inhibitor (IC50 = 9 nM) as well as achieving CDK family selectivity in cells versus key off-targets (CDK1, CDK4/6, CDK9), AZD8421 had no significant kinase inhibition outside the CDK family. AZD8421 inhibits cancer cell proliferation by inhibiting pRB phosphorylation, inducing cell cycle arrest in G1/S phase and senescence. AZD8421 can be studied in research for breast cancer and ovarian cancer .
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- HY-N1050
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mTOR
Ribosomal S6 Kinase (RSK)
Bacterial
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Infection
Neurological Disease
Cancer
|
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Zederone is a sesquiterpene. Zederone inhibits ovarian cancer cell proliferation through mTOR/p70s6K signalling pathway. Zederone inhibits CYP activities with IC50s of 2.9 μM (CYP2B6), 9.2 μM (CYP2C9), 11,2 μM (CYP2C19) and >30 μM (CYP1A2 and CYP2D6). Zederone is hepatotoxic with LD50 value at 24 hours in mice of approximately 223 mg/kg and cytotoxic against the KG1a cell line. Zederone shows antibacterial activity against a number of multi-drug resistant and Methicillin (HY-121544)-resistant Staphylococcus aureus strain. Zederone shows cognition improving capacity and assists in the modulation of gut bacterial dysbiosis .
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HY-L169
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539 compounds
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Resistance refers to the decrease in the effectiveness of drugs in treating diseases or symptoms. Due to the increasing global antibiotic resistance, it may threaten our ability to treat common infectious diseases. Drug resistance is also the main cause of chemotherapy failure in malignant tumors. In approximately 50% of cases, drug resistance exists even before chemotherapy begins. There are many mechanisms of anticancer drug resistance, including increased protein expression that leads to drug removal, mutations in drug binding sites, recovery of tumor protein production, and pre-existing genetic heterogeneity in tumor cell populations. In addition, the issue of drug resistance seems to have affected the development of new anticancer drugs. Drug resistance may be caused by various conditions, such as mutations, epigenetic modifications, and upregulation of drug efflux protein expression. Overcoming multidrug resistance in cancer treatment is becoming increasingly important.
MCE designs a unique collection of 539 anti-drug-resistant compounds. It is a good tool to be used for research on cancer and other diseases.
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P10669
-
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Caspase
Apoptosis
|
Cancer
|
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NDI-Lyso is a lysosome-targeted anticancer agent that induces the formation of rigid long fibers in cancer cell lysosomes through an enzyme-instructed self-assembly (EISA) mechanism catalyzed by cathepsin B. This process triggers lysosomal swelling, membrane permeabilization (LMP), and membrane disruption, ultimately leading to cancer cell apoptosis via a non-classical caspase-independent pathway. NDI-Lyso exhibits significant selective anticancer activity in various cancer cell lines and drug-resistant cancer cells (IC50 ~10 μM) while showing low toxicity to normal cells (IC50 > 60 μM) .
|
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- HY-P11102
-
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Bacterial
Fungal
HIV
Parasite
|
Infection
Cancer
|
|
Temporin-Sha is an antibacterial peptide with extensive biological activity. Temporin-Sha exhibits broad-spectrum antibacterial activity (e.g., against L. ivanovii, MIC = 6.25 μM), and is effective against Gram-negative bacteria (such as Escherichia coli, MIC = 10 μM), including drug-resistant strains (such as Methicillin (HY-121544)-resistant Staphylococcus aureus). Temporin-Sha also has inhibitory effects on Candida albicans (MIC = 25 μM), Saccharomyces cerevisiae (MIC = 12 μM), the pre-flagellated and non-flagellated forms of Leishmania infantum (IC50 = 5-20 μM), and Trypanosoma cruzi (IC50 = 17 μM). Temporin-Sha exhibits antiviral activity against HSV-1 and has anti-cancer effects (cytotoxicity against breast cancer cells MCF-7 and lung cancer cells H460, etc.) .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P991572
-
|
|
EGFR
|
Cancer
|
|
MM-151 is a humanized IgG1 monoclonal antibody targeting EGFR. MM-151 binds multiple regions of the EGFR extracellular domain (ECD) and reduces its mutations in circulating cell-free tumor DNA with EGFR resistance. MM-151 significantly inhibits EGFR signaling and cell growth. MM-151 can be used for drug-resistant cancers research, such as colorectal, non-small cell lung and triple negative breast cancer .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N1050
-
|
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Terpenoids
Sesquiterpenes
Source classification
Plants
Curcuma elata Roxb.
Zingiberaceae
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mTOR
Ribosomal S6 Kinase (RSK)
Bacterial
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Zederone is a sesquiterpene. Zederone inhibits ovarian cancer cell proliferation through mTOR/p70s6K signalling pathway. Zederone inhibits CYP activities with IC50s of 2.9 μM (CYP2B6), 9.2 μM (CYP2C9), 11,2 μM (CYP2C19) and >30 μM (CYP1A2 and CYP2D6). Zederone is hepatotoxic with LD50 value at 24 hours in mice of approximately 223 mg/kg and cytotoxic against the KG1a cell line. Zederone shows antibacterial activity against a number of multi-drug resistant and Methicillin (HY-121544)-resistant Staphylococcus aureus strain. Zederone shows cognition improving capacity and assists in the modulation of gut bacterial dysbiosis .
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- HY-N6611
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| Cat. No. |
Product Name |
Chemical Structure |
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- HY-W766368
-
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C6 Ceramide- 13C2,d2 (C6-Cer- 13C2,d2) is the deuterium labeled and 13C-labeled C6 Ceramide (HY-19542). C6 Ceramide (C6-Cer) is a short-chain, cell-permeable ceramide pathway activator with anticancer activity. C6 Ceramide-mediated miR-29b expression participates in the progression of multiple myeloma through suppressing the proliferation, migration and angiogenesis of endothelial cells by targeting Akt signal pathway. C6 Ceramide exhibits multiple anti-cancer properties including cell cycle arrest, Apoptosis, inhibition of tumor growth and enhances the effects of chemotherapy in drug-resistant cancer cells. C6-ceramide can be used as an adjuvant for chemotherapeutic agents, to enhance anti-tumor effects .
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