Search Result
Results for "
Dual target inhibitor
" in MedChemExpress (MCE) Product Catalog:
2
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-122909
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- HY-126320
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EGFR
c-Met/HGFR
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Cancer
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EGFR-IN-8 is a dual EGFR and c-Met inhibitor, compound 48. EGFR-IN-8 can be a promising candidate for further development to target EGFR TKI-resistant NSCLC .
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- HY-178348
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PARP
c-Met/HGFR
DNA/RNA Synthesis
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Cancer
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PARP1/c-Met-IN-2 is a highly potent, orally active, PARP1 (IC50 = 21.8 nM) and c-Met (IC50 = 30.2 nM) dual inhibitor. PARP1/c-Met-IN-2 can elevate the expression level of γH2AX, cause DNA damage. PARP1/c-Met-IN-2 exhibits remarkable anti-tumor efficacy in the Olaparib (HY-10162)-resistant HCT116 (HCT116OR) xenograft models. PARP1/c-Met-IN-2 can be used for the study of Colon Cancer .
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- HY-129666
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- HY-157965
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VEGFR
FAK
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Cancer
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ZINC09875266 is a dual inhibitor targeting VEGFR2 and FAK that can be used in cancer research .
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- HY-P11225
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MAP-04-02
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Bacterial
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Infection
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DRAMP18563 is a linear antimicrobial peptide that can act as a delivery vector to transport dual-ring peptide inhibitors that cannot penetrate the outer membrane of Gram-negative bacteria to their target sites. DRAMP18563 can be used to study the delivery strategies of dual-ring peptide inhibitors .
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- HY-162952
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Bcr-Abl
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Cancer
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cSRC/BCR-ABL1-IN-1 (compund 16a) is a dual-target cSRC/BCR-ABL1 kinase inhibitor .
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- HY-178455
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Influenza Virus
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Infection
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Influenza virus-IN-10 is a dual-target antiviral agents for influenza that targets both PAC (KD = 8.9 μM) and NP (KD = 52.5 μM) simultaneously. Influenza virus-IN-10 exhibits an EC50 values of 1.64 μM) against influenza A virus (H1N1, A/WSN/33) and broad-spectrum activity against other influenza strains, including influenza B virus and multiple subtypes of influenza A .
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- HY-10725
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Factor Xa
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Cardiovascular Disease
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Tanogitran is a dual inhibitor targeting Factor Xa and thrombin (thrombin), with Ki values of 26 and 2.7 nM, respectively. Tanogitran exhibits anticoagulant activity and can be used for research in thrombotic diseases .
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- HY-161145
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EGFR
Apoptosis
Microtubule/Tubulin
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Cancer
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EGFR/microtubule-IN-1 (Compound 10c) is a dual inhibitor targeting EGFR and tubulin. The IC50 for inhibiting EGFR is 10.66 nM. EGFR/microtubule-IN-1 can reduce the phosphorylation levels of EGFR, AKT and ERK, hinder tubulin polymerization, and induce apoptosis .
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- HY-145428
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Notch
γ-secretase
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Cancer
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BT-GSI is a γ-secretase inhibitor (GSI) and a bone-targeted Notch inhibitor. BT-GSI has dual anti-myeloma and anti-resorptive properties, which can be used for the research of multiple myeloma and associated bone disease. BT-GSI inhibits tumor growth and osteolytic disease progression .
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- HY-P99166
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PD-1/PD-L1
CTLA-4
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Inflammation/Immunology
Cancer
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Vudalimab is a potent dual PD-1 and CTLA-4 inhibitor as a fully humanized bispecific monoclonal antibody. Vudalimab targets immune checkpoint receptors PD-1 and CTLA-4 and promotes tumor-selective T-cell activation .
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- HY-162143
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SphK
Akt
mTOR
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Cancer
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SKI-349 is a dual-targeted inhibitor of sphingosine kinase 1/2 (SPHK1/2) and microtubule assembly (MDA). SKI-349 has anticancer activity. SKI-349 can inhibit the vitality, invasion, and AKT/mTOR signaling pathway of liver cells .
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- HY-106056
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D 16726
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Estrogen Receptor/ERR
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Cancer
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Zindoxifene is a partial anti-estrogen. Zindoxifene works primarily by binding to estrogen receptors, thereby inhibiting the growth of estrogen-dependent tumor cells. Zindoxifene is able to exhibit the dual properties of estrogen agonists and antagonists and can be used in research and development to target estrogen-dependent tumors, such as prostate and breast cancer .
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- HY-174211
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JNK
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Cancer
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JNK-IN-23 (Compound K12) is an inhibitor of JNK. JNK-IN-23 inhibits the proliferation of MDA-MB-231 (GIC50: 30 nM). JNK-IN-23 blocks TNBC metastatic growth in vivo. JNK-IN-23 inhibits the growth of lung metastases by dual targeting of glutaminase-1 (GLS) and pyruvate dehydrogenase complex (PDHC) .
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- HY-162519
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LZ90
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NAMPT
PD-1/PD-L1
Apoptosis
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Metabolic Disease
Inflammation/Immunology
Cancer
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LZFPN-90 (LZ90) is a dual NAMPT/PD-L1 targeting compound. LZFPN-90 inhibits PD-1/PD-L1 interaction and NAMPT activity. LZFPN-90 inhibits cell growth in a NAMPT-dependent manner and blocks the cell cycle, subsequently inducing apoptosis. LZFPN-90 exerted target-dependent antitumor activities, affecting metabolic processes and the immune system .
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- HY-146160
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PARP
HDAC
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Cancer
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PARP-1/HDAC-IN-1 is a PARP-1/HDAC6 dual targeting inhibitor with IC50s of 68.90 nM and 510 nM, respectively. PARP-1/HDAC-IN-1 displays remarkable anticancer, anti-migration and anti-angiogenesis activities .
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- HY-168475
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Apoptosis
WDR5
HDAC
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Cancer
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DD0-2363 (Compound 32d) is a dual-target inhibitor of WDR5-MLL1/HDAC. DD0-2363 inhibits cells proliferation and induces apoptosis in acute myeloid leukemia cells. DD0-2363 has antitumor activity and can be used in the research of acute myeloid leukemia .
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- HY-162349
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HDAC
PARP
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Cancer
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PARP7/HDACs-IN-1 (compound 9l) is a dual-target inhibitor targeting PARP7/HDAC with anti-tumor activity. PARP7/HDACs-IN-1 inhibits different subtypes of PARPs and HDACs with IC50s of 83.3 nM (PARP1), 3.1 nM (PARP7), 35 nM (HDAC1), 30.3 nM (HDAC2), 35.4 nM (HDAC3), and 6.4 nM respectively. (HDAC6) . br/ .
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- HY-175262
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Bacterial
Cytochrome P450
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Infection
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Mtb-IN-12 (Compound 5m) is a dual-target inhibitor that can target the CYP125 (KD: 40 nM; KI: 0.1 μM) and CYP142 (KD: 160 nM; KI: 0.05 μM) enzymes of Mycobacterium tuberculosis. Mtb-IN-12 exhibits good inhibitory activity against both drug-sensitive strains and multidrug-resistant tuberculosis strains, with low toxicity to macrophages. Mtb-IN-12 can be used in the research of anti-tuberculosis drugs .
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- HY-137561A
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PLN-74809 hydrochloride
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Integrin
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Inflammation/Immunology
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Bexotegrast hydrochloride (PLN-74809 hydrochloride) is a small molecule dual selective inhibitor with activity targeting αVβ1 and αVβ6. Bexotegrast hydrochloride is used for idiopathic pulmonary fibrosis (IPF) and primary sclerosing cholangitis (PSC). Bexotegrast hydrochloride inhibits the activation of TGF-β1 by blocking the function of these integrins, thereby preventing the growth of fibrous tissue in the lungs and bile ducts .
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- HY-150755
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- HY-163537
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Cholinesterase (ChE)
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Neurological Disease
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AChE/BuChE-IN-5 (compound 5a) is a dual target inhibitor. AChE/BuChE-IN-5 has excellent nanomolar inhibitory activity on acetylcholinesterase (AChE) (IC50=46.9 nM) and butyryl cholinesterase (BuChE) (IC50=3.5 nM). AChE/BuChE-IN-5 can be used for Alzheimer's Disease research .
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- HY-176877
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Glucocorticoid Receptor
Interleukin Related
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Inflammation/Immunology
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Glucocorticoid receptor/IL-6-IN-2 (Compound 36) is a selective dual inhibitor targeting the glucocorticoid receptor (GR) and IL-6 signaling pathway (IC50 values of 40 nM and 19 nM, respectively). Glucocorticoid receptor/IL-6-IN-2 is promising for research of inflammatory diseases like rheumatoid arthritis and asthma .
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- HY-162601
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Histone Methyltransferase
HIF/HIF Prolyl-Hydroxylase
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Cancer
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D-01 is a dual-targeting inhibitor of HIF-1α and EZH2 (IC50: 4.86 μM and 0.99 μM respectively). D-01 inhibits the expression of H3K27me3 protein. D-01 inhibits the migration, clone and the invasion of A549 cells, and also inhibits tube formation of HUVECs. D-01 can be used for research of lung cancer .
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- HY-164455
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STAT
JAK
Aurora Kinase
Mitosis
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Inflammation/Immunology
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AJI-214 is a dual-target inhibitor of Aurora kinase A and JAK2. AJI-214 directly blocks Aurora kinase A to inhibit T cell mitotic progression and cell polarity, and inhibits JAK2 activation to inhibit STAT3 phosphorylation, thereby reducing the differentiation of TH1 and TH17 cells. AJI-214 can be used in studies on regulating immune responses and preventing graft-versus-host disease (GVHD) .
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- HY-128171
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FLAP
Epoxide Hydrolase
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Inflammation/Immunology
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Diflapolin is a highly active dual 5-lipoxygenase-activating protein (FLAP)/soluble epoxide hydrolase (sEH) inhibitor with marked anti-inflammatory efficacy and high target selectivity. Diflapolin inhibits 5-LOX product formation in intact human monocytes and neutrophils with IC50s?of? 30 and 170?nM, respectively, and suppressed the activity of isolated sEH (IC50=20?nM) .
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- HY-157480
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EGFR
Aurora Kinase
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Cancer
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EGFR/AURKB-IN-1 (compound 7) is a dual-targeted EGFR/AURKB inhibitor, and inhibits the phpsphorylations of L858R EGFR and AURKB with IC50s of 0.07 and 1.1, respectively. EGFR/AURKB-IN-1 occupies the hydrophobic region I or the αC-helix out pocket of EGFR and the back pocket of AURKB, inhibiting the growth, division and metastasis of tumor cells, thus can be used for cancer research .
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- HY-177134
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VEGFR
c-Met/HGFR
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Cancer
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Taligantinib (Compound Example 70) is an orally active and selective dual inhibitor targeting vascular endothelial growth factor receptor 2 (VEGFR-2) and hepatocyte growth factor receptor (c-Met). Taligantinib suppresses tumor angiogenesis and cell proliferation. Taligantinib is promising for research of solid tumors such as non-small cell lung cancer and hepatocellular carcinoma .
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- HY-163439
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Amylases
Glycosidase
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Metabolic Disease
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α-Amylase/α-Glucosidase-IN-12 (compound 10k) is a dual inhibitor targeting α-glucosidase and α-amylase with IC50 of 34.52 nM and 24.62 nM, respectively. α-Amylase/α-Glucosidase-IN-12 is an inhibitor designed based on triazolo[4,3-b][1,2,4]triazine and has the potential to be used in diabetes research .
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- HY-168968S
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EGFR
Histone Demethylase
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Cancer
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ZJY-54 is an orally active dual-target inhibitor of EGFR/LSD1, with IC50 values of 3.8 nM and 0.6 μM, respectively. ZJY-54 can inhibit the proliferation of non-small cell lung cancer cells, induce the accumulation of H3K4me2 and H3K9me2, and inhibit the phosphorylation of the EGFR signaling pathway. ZJY-54 has anti-tumor activity .
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- HY-112440
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Methuosis inducer 1
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Others
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Cancer
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HZX-02-059 is a potent methuosis inducer and dual-target PIKfyve/tubulin inhibitor with anticancer activity. Methuosis mainly disrupts the balance of endocytosis and exocytosis, forming a large number of vesicles and inducing cell death. HZX-02-059 also induces cell vacuolization, promotes apoptosis, downregulates the p53 pathway, inhibits PI3K/AKT phosphorylation, and inhibits c-Myc and NF-κB transcription .
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- HY-12680
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PRN694
2 Publications Verification
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Itk
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Inflammation/Immunology
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PRN694 is an irreversible, highly selective and potent covalent interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) dual inhibitor with IC50s of 0.3 nM and 1.4 nM, respectively. PRN694 exhibits extended target residence time on ITK and RLK, enabling durable attenuation of effector cells in vitro and in vivo .
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- HY-144315
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Snail/HDAC-IN-1
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HDAC
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Cancer
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CYD19 is a potent Snail/HDAC dual target inhibitor. CYD19 displays potent inhibitory activity against HDAC1 with an IC50 of 0.405 μM and potent inhibition against Snail with a Kd of 0.18 μM. CYD19 increases histone H4 acetylation in HCT-116 cells and decreases the expression of Snail protein to induce cell apoptosis .
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- HY-164454
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Aurora Kinase
STAT
JAK
Mitosis
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Inflammation/Immunology
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AJI-100 is a dual-target inhibitor of Aurora kinase A and JAK2 with IC50 values of 12.7 nM and 18.5 nM, respectively. AJI-100 directly blocks Aurora kinase A to inhibit T cell mitosis and cell polarity, and inhibits JAK2 activation to inhibit STAT3 phosphorylation, thereby reducing the differentiation of TH1 and TH17 cells. AJI-100 can be used in studies on regulating immune responses and preventing graft-versus-host disease (GVHD) .
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- HY-176287
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Dopamine Receptor
GSK-3
PKA
P-glycoprotein
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Neurological Disease
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ARN25657 is a dual-acting D3R/GSK-3β modulator. ARN25657 has both partial D3R agonist activity (EC50 = 15.2 nM, Ki =1.5 nM) and potent GSK-3β inhibitor activity (IC50 = 19.3 nM). ARN25657 exhibits excellent GSK-3β selectivity over FYN, PKA, and CDK5/p35. ARN25657 inhibits P-glycoprotein (P-gP)-mediated acetoxymethyl calcein efflux and improves in vitro ADME properties while maintaining a balanced dual-target profile. ARN25657 is useful for studying bipolar disorder and related neuropsychiatric disorders .
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- HY-171027
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Ligands for Target Protein for PROTAC
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Cancer
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PTP1B/TC-PTP IN-1 is a PTP1B and TC-PTP dual inhibitor. PTP1B/TC-PTP IN-1 can be used as a target protein ligand for the synthesis of DU-14 (PTP1B/TC-PTP PROTAC) (HY-164864) .
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- HY-160557
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Epigenetic Reader Domain
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Cancer
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PLK1/BRD4-IN-2 (compound 15) is a BI-2536 (HY-50698) analog and dual inhibitor that targets both Polo-like kinase 1 (PLK1) and BRD4bromodomain (BRD4-BD1 IC50=28 nM, PLK1 IC50=40 nM) .
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- HY-169509
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PARP
Necroptosis
Topoisomerase
RIP kinase
Mixed Lineage Kinase
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Cancer
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Topoisomerase I/II Inhibitor 8 (Compound Ru7) is a dual catalytic inhibitor of Topoisomerase I/II, capable of inducing DNA damage and PARP-1 activation, which subsequently leads to the activation of RIPK1, RIPK3, and MLKL, ultimately triggering necroptosis. Topoisomerase I/II Inhibitor 8 demonstrates remarkable anticancer activity by effectively targeting the nuclei of cancer cells and inducing cell death through necroptosis, showing great clinical potential in circumventing drug resistance in cancer treatment .
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- HY-163006
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EGFR
c-Met/HGFR
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Cancer
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EGFR/c-Met-IN-1 (compound TS-41) is a dual-target inhibitor of EGFR/c-Met. The IC50 for inhibiting EGFR L858R and c-Met is 68.1 nM and 0.26 nM respectively. . EGFR/c-Met-IN-1 induces apoptosis and cell cycle arrest in A549-P cells, downregulating the phosphorylation of EGFR, c-Met, and downstream AKT. EGFR/c-Met-IN-1 inhibits tumor growth in vitro and in vivo .
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- HY-149283
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JAK
HDAC
Apoptosis
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Cancer
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JAK/HDAC-IN-2 is a potent 2-amino-4-phenylaminopyrimidine JAK/HDAC dual-target inhibitor. JAK/HDAC-IN-2 potently inhibits HDAC3/6 and JAK1/2 at nanomolar levels. JAK/HDAC-IN-2 has proapoptotic activity and inhibits histone deacetylation and STAT3 phosphorylation. JAK/HDAC-IN-2 presents remarkable antiproliferative activity in both hematological malignancies and solid cancers .
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- HY-161083
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PARP
Histone Methyltransferase
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Cancer
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PARP/EZH2-IN-2 (compound 12e) is a dual target PARP1 and EZH2 inhibitor, with IC50 values of 6.89 and 27.34 nM, respectively. PARP/EZH2-IN-2 shows anticancer activity, with no toxicity to normal cells. PARP/EZH2-IN-2 achieves synthetic lethality indirectly by inhibiting EZH2 to increase the sensitivity to PARP1, and induces cell death by regulating excessive autophagy .
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- HY-169212
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PI3K
Annexin A
ERK
VEGFR
STAT
Raf
FAK
Akt
Ras
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Cancer
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I194496 is a potent cystathionine γ-lyase (CSE) inhibitor, with an IC50 of 0.79 mM. I194496 can inhibit the growth of human TNBC cells via the dual targeting PI3K/Akt and Ras/Raf/ERK pathway and suppress the metastasis of human TNBC cells via down-regulating Anxa2/STAT3 and VEGF/FAK/Paxillin signaling pathways .
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- HY-113289
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Akt
Androgen Receptor
Bacterial
Drug Metabolite
HSV
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Infection
Cardiovascular Disease
Neurological Disease
Cancer
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Brassicasterol is a metabolite of Ergosterol and has cardiovascular protective effects. Brassicasterol exerts anticancer effects in prostate cancer through dual targeting of AKT and androgen receptor signaling pathways. Brassicasterol inhibits HSV-1 (IC50=1.2 μM) and Mycobacterium tuberculosis. Brassicasterol also inhibits sterol δ 24-reductase, slowing the progression of atherosclerosis. Brassicasterol is also a cerebrospinal fluid biomarker for Alzheimer's disease .
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- HY-120826
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Monoamine Oxidase
Adenosine Receptor
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Neurological Disease
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A2AAR/hMAO-B-IN-1 (compoudn 17) is a non-xanthine dual-target inhibitor targeting the A2A adenosine receptor (A2AAR) (IC50: 34.9 nM) andMAO-B (Ki: 39.5 nM, human). A2AAR/hMAO-B-IN-1 inhibits A2AAR-induced cAMP accumulation and exhibits competitive, reversible inhibition of MAO-B. A2AAR/hMAO-B-IN-1 can be used in the study of neurodegenerative diseases such as Parkinson's disease (PD) .
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- HY-173081
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SARS-CoV
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Infection
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4"-(2-(p-Chlorophenyl)acetoxyl)spiramycin (Compound 2d) is a broad-spectrum anti-coronaviral agent via targeting frameshifting element (FSE). 4"-(2-(p-Chlorophenyl)acetoxyl)spiramycin inhibits HCoV-OC43 and HCoV-229E with EC50 values of 0.85 μM and 1.45 μM. 4"-(2-(p-Chlorophenyl)acetoxyl)spiramycin shows a dual-target mechanism that acts on both viral FSE RNA and host DIS3L2 .
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- HY-149734
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Bacterial
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Infection
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MA220607 is an antibacterial agent with low hemolytic toxicity and a dual-target mechanism of action (MOA). MA220607 promotes FtsZ protein polymerization, also increases the permeability of bacterial membranes and inhibits biofilm formation. The resistance rate of MA220607 is low, and the MICs against Gram-positive bacteria and Gram-negative bacteria are Table 0.062-2 μg/mL and 0.5-4 μg/mL, respectively) .
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- HY-162312
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Deubiquitinase
Apoptosis
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Cancer
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LLK203 is a potent USP2/USP8 dual-target inhibitor with IC50s of 0.89 μM and 0.52 μM, respectively. LLK203 leads a degradation of ERα and induces apoptosis of breast cancer MCF-7 cells. LLK203 demonstrates antitumor activities against the 4T1 tumor mice model .
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- HY-174383
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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PDE3/4-IN-2 (Compound 1) is a PDE3/PDE4 dual-target inhibitor, with IC50 values of 0.13 nM and 50 nM against PDE3A and PDE4B1, respectively. PDE3/4-IN-2 can be used in the research of PDE-related diseases, such as asthma, obstructive pulmonary disease, sepsis, and nephritis .
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- HY-168554
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PROTACs
STING
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Inflammation/Immunology
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STING-IN-10 (P8) is a dual STING PROTAC degrader and inhibitor with a DC50 value of 2.58 μM in THP-1 cells. STING-IN-10 has anti-inflammatory activity .(Pink: Target protein ligand (HY-168676); Black: linker (HY-W123015); Blue: E3 ligase ligand (HY-126457))
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- HY-179053
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- HY-162803
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Apoptosis
c-Met/HGFR
STAT
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Cancer
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c-Met-IN-24 (compound 3g) is a dual-target inhibitor of STAT-3 ( =4.7 μM) and c-MET ( =12.67 μM) with anticancer activity. c-Met-IN-24 arrests the G2/M cell cycle and induces apoptosis in SNB-75 cells. c-Met-IN-24 can be used in the study of central nervous system cancers .
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- HY-126249
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Aurora Kinase
Polo-like Kinase (PLK)
Apoptosis
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Cancer
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AAPK-25 is a potent and selective Aurora/PLK dual inhibitor with anti-tumor activity, which can cause mitotic delay and arrest cells in a prometaphase, reflecting by the biomarker histone H3 Ser10 phosphorylation and followed by a surge in apoptosis. AAPK-25 targets Aurora-A, -B, and -C with Kd values ranging from 23-289 nM, as well as PLK-1, -2, and -3 with Kd values ranging from 55-456 nM .
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- HY-178366
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Influenza Virus
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Infection
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PAC/NP-IN-1 (Compound 30) is a dual-target anti-influenza agent that specifically binds to nucleoprotein (NP) and the C-terminal domain of PA protein (PAc). PAC/NP-IN-1 inhibits influenza A virus A/WSN/33 (H1N1) (EC50 = 3.63 μM, IC50 = 3.08 μM). PAC/NP-IN-1 can be used for the study of influenza infection .
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- HY-138215
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ERK
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Cancer
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ADTL-EI1712 is a potent, orally active, and selective dual-target inhibitor of ERK1 and ERK5, inhibition rates of ERK1/5 at 1 μM are 93.54% and 89.35%, respectively. ADTL-EI1712 can induce regulated cell death, a form of cell death that relies on the activation of genetically encoded machinery, to overcome compensatory mechanism in specific cancer cells in vitro and in vivo .
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- HY-175656
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LIM Kinase (LIMK)
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Neurological Disease
Cancer
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MDI-117740 is a dual LIMK1/2 inhibitor. MDI-117740 shows effective cellular target engagement with LIMK1 (pIC50 = 6.73) and LIMK2 (pIC50 = 7.18) in HEK293 cells. MDI-117740 exerts significant anti-migratory activity in MDA-MB-231 cells. MDI-117740 can be used for the study of diseases associated with LIMK dysregulation, such as cancers and neurodegenerative disorders .
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- HY-174130
-
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Parasite
PI4K
PKG
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Infection
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PI4Kβ/PKG-IN-1 (Compound 19) is an orally active dual inhibitor targeting Plasmodium phosphatidylinositol 4-kinase beta (PI4Kβ) and cGMP-dependent protein kinase (PKG). PI4Kβ/PKG-IN-1 exhibits potent antiplasmodial activity. PI4Kβ/PKG-IN-1 is promising for research of malaria .
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- HY-178440
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EGFR
COX
Apoptosis
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Inflammation/Immunology
Cancer
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EGFR/COX-2-IN-2 (Compound 10a) is a dual inhibitor targeting epidermal growth factor receptor (EGFR) (IC50= 6.0 μM) and cyclooxygenase-2 (COX-2) (IC50=50 μM). EGFR/COX-2-IN-2 induces S-phase cell cycle arrest and apoptosis. EGFR/COX-2-IN-2 is promising for research of cancers and inflammation-related diseases .
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- HY-177086
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Indoleamine 2,3-Dioxygenase (IDO)
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Cancer
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IDO1/TDO-IN-9 (Compound 66) is a potent dual inhibitor targeting indoleamine 2,3-dioxygenase 1 (IDO1) and tryptophan 2,3-dioxygenase (TDO) with IC50s of <1 μM. IDO1/TDO-IN-9 inhibits the activity of IDO1 and TDO, blocking tryptophan degradation to kynurenine, restoring immune activity in the tumor microenvironment, and suppressing tumor growth. IDO1/TDO-IN-9 is promising for research of cancers .
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- HY-159513
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Bcl-2 Family
Apoptosis
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Cancer
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Bcl-2/Mcl-1-IN-4 (compound 20) is a dual inhibitor targeting Bcl-2 (Ki=0.49 μM) and Mcl-1 (Ki=0.51 μM). Bcl-2/Mcl-1-IN-4 significantly inhibits cancer cell proliferation and effectively induces apoptosis in U937 cells. Bcl-2/Mcl-1-IN-4 can be used in cancer research .
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-
- HY-176876
-
|
|
Glucocorticoid Receptor
Interleukin Related
JAK
STAT
|
Inflammation/Immunology
|
|
Glucocorticoid receptor/IL-6-IN-1 (Compound 35) is a selective dual inhibitor targeting the glucocorticoid receptor (GR) and IL-6 signaling pathway (IC50 values of 120 nM and 59 nM, respectively). Glucocorticoid receptor/IL-6-IN-1 inhibits IL-6-induced JAK/STAT3 phosphorylation, blocking inflammatory cytokine transcription. Glucocorticoid receptor/IL-6-IN-1 is promising for research of inflammatory diseases like rheumatoid arthritis and asthma .
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-
- HY-151263
-
|
|
HDAC
G-quadruplex
|
Cancer
|
|
G4/HDAC-IN-1 (compound a6) is a G4/HDAC dual-targeting compound. G4/HDAC-IN-1 inhibits intracellular HDAC activity with an IC50 value of 1.1 μM, and induces G4 formation. G4/HDAC-IN-1 inhibits TNBC proliferation and tumor growth in TNBC xenograft model. G4/HDAC-IN-1 can be used for the research of cancer .
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-
- HY-116191
-
|
|
PI3K
mTOR
|
Cancer
|
|
WJD008 is a potent dual phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor with antiproliferative and anticlonogenic activity in tumor cells and transformed cells with PIK3CA mutant. WJD008 inhibits kinase activity of PI3K α and mTOR and abrogates insulin-like growth factor-I-activated PI3K-Akt-mTOR signaling cascade. WJD008 is promising for research of cancers .
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-
- HY-179031
-
|
|
EGFR
VEGFR
Apoptosis
|
Cancer
|
|
EGFR/VEGFR2-IN-7 (Compound 3e) is a dual-target EGFR/VEGFR2 inhibitor, with IC50 values of 142 (EGFR) and 71 nM (VEGFR2). EGFR/VEGFR2-IN-7 exhibits broad-spectrum and potent anti-proliferative activity, especially being sensitive to breast cancer. EGFR/VEGFR2-IN-7 induces cell cycle arrest and apoptosis, inhibits cell migration and invasion. EGFR/VEGFR2-IN-7 can be used for research on breast cancer .
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-
- HY-172617
-
|
|
BMI1
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
APD-94 is a dual inhibitor targeting tubulin and Bmi-1. APD-94 interfers tubulin normal polymerization. APD-94 suppresses the expression of Bmi-1. APD-94 causes cell cycle arrest at the G2/M phase in cancer cells and induces apoptosis, thus inhibiting cancer cell proliferation. APD-94 represses the growth of HT29 cell xenografts in NOD/SCID mice. APD-94 can be used for colorectal cancer study .
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-
- HY-163105
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin/NEDDylation-IN-1 (compound C11) is a dual inhibitor of tubulin (Microtubule/Tubulin)-NEDDylation (IC50 for tubulin=2.40 μM), which has strong anti-proliferative activity. Neddylation is a protein post-translational modification that covalently tags the ubiquitin-like protein NEDD8 to target proteins. Tubulin/NEDDylation-IN-1 forms hydrogen bonds with residues of tubulin and E1 NEDD8 activating enzyme (NAE) through methoxy and dithiocarbamate groups and inhibits NEDDylation and microtubulin in an ATP-dependent manner. tube polymerization .
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-
- HY-158328A
-
-
- HY-174221
-
|
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IMPDH
HDAC
Apoptosis
|
Cancer
|
|
IMPDH II/HDAC1-IN-1 (Compound C12) is an orally active dual-target inhibitor of IMPDH II and IMPDH II (IC50 values are 84.69 nM and 81.75 nM, respectively). IMPDH II/HDAC1-IN-1 has significant anti-tumor activity and has an anti-proliferative effect on K-562 cells (IC50 = 305.31 nM). IMPDH II/HDAC1-IN-1 exerts a synergistic anti-tumor effect by simultaneously targeting IMPDH II and HDAC1, inhibiting tumor cell proliferation and inducing apoptosis. IMPDH II/HDAC1-IN-1 can be used in the study of cancers such as chronic myeloid leukemia (CML) .
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-
- HY-159078
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
PolQi1 is a selective inhibitor targeting the Polθ domain of DNA polymerase. PolQi1 inhibits the Polθ-mediated microhomology end joining (TMEJ/alt-EJ) pathway, reducing insertion/deletion (Indels) and imprecise editing events during DNA repair. PolQi1 can enhance the efficiency and accuracy of homology-directed repair (HDR) or Prime editing, and reduce off-target effects; and in combination with DNA-PK inhibitor AZD-7648 (HY-111783), exert efficient genome editing capabilities with dual pathway regulation. PolQi1 can be mainly used in gene editing research (such as CRISPR-Cas9 or Prime editing system optimization) to improve the precision editing efficiency of difficult-to-edit cells (such as primary hepatocytes and mouse embryos) .
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-
- HY-155222
-
|
|
Epigenetic Reader Domain
HDAC
|
Cancer
|
|
TW9 is a potent dual inhibitor simultaneously targeting BET and HDAC proteins with KDs of 0.069 μM, 0.231 μM for BRD4(1), BRD4(2), and an IC50 of 0.29 μM for HDAC1, respectively. TW9 is a newly generated adduct of the BET inhibitor (+)-JQ1 (HY-13030) and class I HDAC inhibitor CI994 (HY-50934). TW9 shows high potency in suppressing tumor growth in pancreatic ductal adenocarcinoma (PDAC). TW9 improves the efficacy of the chemotherapeutic agent Gemcitabine (HY-17026) .
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-
- HY-176165
-
|
|
CDK
Histone Methyltransferase
|
Cancer
|
|
CDK9/EZH2-IN-1 (Compound D16) is a CDK9/EZH2 dual-target inhibitor (IC50: 83.9/108.6 nM). CDK9/EZH2-IN-1 induces apoptosis and DNA double-strand breaks (DSBs). CDK9/EZH2-IN-1 inhibits the proliferation activity of MKN45, MDA-MB-453 and SW620 cancer cells (IC50 values are 136.3, 171.3 and 315.7 nM, respectively) .
|
-
- HY-156094
-
|
|
HDAC
Histone Demethylase
Apoptosis
|
Cancer
|
|
JMJD3/HDAC-IN-1 (compound A5b) is a dual inhibitor targeting Jumonji domain-containing protein demethylase 3 (JMJD3) and histone deacetylase (HDAC1, IC50=16 nM). JMJD3/HDAC-IN-1 promotes hypermethylation of histone H3K27 and hyperacetylation of H3K9, and also cleaves caspase-7 and PARP to induce apoptosis. JMJD3/HDAC-IN-1 effectively inhibits cancer cell cloning, migration, and invasion .
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-
- HY-178031
-
|
|
HIV
|
Infection
|
|
HIV-1-IN-87 (Compound 11x) is a dual-site HIV-1 inhibitor targeting the non-nucleoside reverse transcriptase inhibitor binding pocket (NNIBP) and its adjacent site (NNIAS). HIV-1-IN-87 has potent antiviral activities against wild-type and mutant strains (such as L100I, K103N and Y181C) (EC50s: 4.1-150 nM). HIV-1-IN-87 can be used for HIV-1 infections like acquired immune deficiency syndrome (AIDS) research .
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-
- HY-174457
-
|
|
STAT
Carbonic Anhydrase
Ferroptosis
Apoptosis
Reactive Oxygen Species (ROS)
Caspase
Bcl-2 Family
|
Cancer
|
|
STAT3/CAIX-IN-1 is a dual-target inhibitor of STAT3 (Kd: 60.03 μM) and CAIX (IC50: 80.45 nM). STAT3/CAIX-IN-1 induces ferroptosis by increases the levels of reactive oxygen species (ROS) and lipid peroxides. STAT3/CAIX-IN-1 inhibits cell migration, induces apoptosis, and causes cell cycle arrest in MDA-MB-231 cells. STAT3/CAIX-IN-1 can be used for the study of triple-negative breast cancer (TNBC) .
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-
- HY-170793
-
|
|
PD-1/PD-L1
VISTA
|
Cancer
|
|
PD-L1/VISTA-IN-1 (Compound P17) is an orally active dual-target inhibitor of PD-L1 and VISTA. PD-L1/VISTA-IN-1 can block the PD-1/PD-L1 interaction (IC50: 0.1492 μM) and the VISTA pathway (KD: 0.2723 μM), thereby reactivating T cells. PD-L1/VISTA-IN-1 has anti-tumor activity .
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-
- HY-170651
-
|
|
CDK
HDAC
Apoptosis
|
Cancer
|
|
CDK4/6/HDAC-IN-1 (Compound N14) is a dual-targeting inhibitor of CDK4/6 and HDAC (IC50: CDK4 = 7.23 nM, CDK6 = 13.20 nM, HDAC1 = 55.66 nM, HDAC6 = 48.38 nM). CDK4/6/HDAC-IN-1 induces cell Apoptosis and G0/G1 phase arrest through HDAC-p21-CDK signaling pathway. CDK4/6/HDAC-IN-1 inhibits hepatocellular carcinoma .
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-
- HY-162319
-
|
|
Apoptosis
HDAC
Microtubule/Tubulin
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Tubulin/HDAC-IN-4 (compound 9n) is a dual Tubulin and HDAC inhibitor with IC50 values of 0.73, 0.43, 0.62, 2.34 µM for HDAC1, HDAC2, HDAC6, HDAC7, respectively. Tubulin/HDAC-IN-4 inhibits the tubulin polymerization by targeting the colchicine binding site. Tubulin/HDAC-IN-4 induces apoptosis and cell cycle arrest at G2/M phase. Tubulin/HDAC-IN-4 induces a significant elevation of intracellular ROS levels. Tubulin/HDAC-IN-4 shows anti-angiogenesis activity and anticancer activity .
|
-
- HY-173280
-
|
CHNQD-01228
|
Arf Family GTPase
BMX Kinase
|
Cancer
|
|
Brefeldin A 4-O-nicotinate (CHNQD-01228) is a dual inhibitor of Arf1 and BMX proteins. The IC50 value for the proliferation of T24 cells is 0.22 μM. It can also dose-dependently inhibit the migration and colony formation of T24 cells, induce G1 phase arrest and trigger Apoptosis. Brefeldin A 4-O-nicotinate exerts its anti-cancer activity by targeting the BMX protein to inhibit the AKT/p-AKT and STAT3/p-STAT3 signaling pathways, as well as by inhibiting the Arf1 protein to eliminate bladder cancer stem cells and activate anti-tumor immunity. Brefeldin A 4-O-nicotinate can be used in the research related to bladder cancer .
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-
- HY-172919
-
|
|
Phosphodiesterase (PDE)
NAMPT
Apoptosis
|
Cancer
|
|
PDEδ/NAMPT IN-1 (Compound 17d) is a dual inhibitor targeting phosphodiesterase 6 (PDE6) (KD=0.410 nM) and nicotinamide phosphoribosyl transferase (NAMPT) (IC50=2.21 nM). PDEδ/NAMPT IN-1 blocks KRAS-related signal transduction and interferes with the synthesis of nicotinamide adenine dinucleotide (NAD +), inducing apoptosis in KRAS mutant pancreatic cancer cells. PDEδ/NAMPT IN-1 is promising for research of KRAS mutant pancreatic cancer .
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-
- HY-163786
-
|
|
PROTACs
CDK
Apoptosis
|
Cancer
|
|
PROTAC CDK4/6 degrader 1 (Compound 7f) is a dual degrader for CDK4 and CDK6 with DC50 of 10.5 and 2.5 nM. PROTAC CDK4/6 degrader 1 inhibits the proliferation of cell Jurkat (IC50 is 0.18 μM), arrests the cell cycle at G1 phase and induces apoptosis. (Pink: ligand for target protein YY173 (HY-163787); Black: linker (HY-163788); Blue: ligand for E3 ligase (HY-10984))
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-
- HY-162606
-
|
|
Monoamine Oxidase
Cholinesterase (ChE)
|
Neurological Disease
|
|
MAO-A/B-IN-3 (Compound 12) stands out as a key dual MAO-AChE inhibitor, displaying excellent multi-target efficacy against MAO-A, MAO-B, and AChE with IC50 values of 67 nM, 29 nM, and 1370 nM respectively. MAO-A/B-IN-3 is adept at altering the A site (hydrophobic ring) and C site (semicarbazone chain) within ketone amine-based MTDLs to bolster the inhibitory potential against MAO-A/B while notably diminishing activity against AChE. MAO-A/B-IN-3 is poised for research applications in the field of neurodegenerative diseases .
|
-
- HY-149617
-
|
|
Cytochrome P450
PD-1/PD-L1
|
Infection
|
|
CYP51/PD-L1-IN-4 (compound 14a-2) is a potent dual-target (CYP51/PD-L1) inhibitor, with IC50 values of 0.17 and 0.021 μM, respectively. CYP51/PD-L1-IN-4 exhibits excellent antifungal and antidrug-resistant fungal activity in vitro. CYP51/PD-L1-IN-4 can be used for fungal infections research .
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-
- HY-N4150
-
|
Quercetagetin-7-O-glucoside
|
Phosphatase
Tau Protein
NF-κB
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Quercetagitrin (Quercetagetin-7-O-glucoside) is a natural product that can be isolated from the African marigold (Tagetes erecta). Quercetagitrin has anti-inflammatory activity. Quercetagitrin inhibits Tau accumulation. Quercetagitrin can reverse neuroinflammation and cognitive deficits in P301S-Tau transgenic mouse model through inhibiting NF-κB activation. Quercetagitrin is a dual-target inhibitor of PTPN6 (IC50 = 1 μM) and PTPN9 (IC50 = 1.7 μM). Quercetagitrin enhances glucose uptake by mature C2C12 myoblasts. Quercetagitrin can be studied in research for Alzheimer’s disease and type 2 diabetes .
|
-
- HY-155227S
-
|
|
Isotope-Labeled Compounds
EGFR
Anaplastic lymphoma kinase (ALK)
BRK
Apoptosis
Mitochondrial Metabolism
|
Cancer
|
|
ALK/EGFR-IN-1-d5 (Compound (-)-9a) is a deuterated dual-target inhibitor of EGFR and ALK, with an IC50 of 1.08 nM for EGFR and an IC50 of 2.395 nM for ALK. ALK/EGFR-IN-1-d5 inhibits the phosphorylated proteins in the EGFR, ALK, and BRK signaling pathways, blocking the cell cycle, leading to a reduction in mitochondrial membrane potential and cell apoptosis (Apoptosis). ALK/EGFR-IN-1-d5 also significantly inhibits tumor growth in animal models and demonstrates good safety. ALK/EGFR-IN-1-d5 holds promise for research in the field of cancer treatment
|
-
- HY-W023758
-
|
4-(4-Bromo-1H-pyrazol-5-yl)pyridine
|
DNA/RNA Synthesis
|
Cancer
|
|
HDGFRP2/PSIP1-IN-1 (compound BPP) is a dual inhibitor targeting the PWWP domain of hepatocarcinogenic growth factor-related protein 2 (HDGFRP2) and its homologous protein PSIP1, hinder the development and progression of diffuse intrinsic pontine glioma (DIPG). HDGFRP2/PSIP1-IN-1 binds to HDGFRP2 with a Kd value of 7 μM and a ligand efficiency of 0.47; it binds to the PSIP1 PWWP domain with a Kd value of 27 μM; meanwhile, it has a Kd value of 14 μM for HDGFRP3, indicating its effectiveness as an inhibitor of the HDGFRP2 PWWP subfamily .
|
-
- HY-158310
-
|
|
SOS1
EGFR
Ras
|
Cancer
|
|
SOS1/EGFR-IN-1 (compound SE-9) is a dual-target inhibitor for the prostate cancer. SOS1/EGFR-IN-1 inhibits effectively SOS1(IC50=42.13±1.55 nM) and EGFR(IC50=1.01±0.04 nM) by inhibiting their downstream effector molecules. SOS1/EGFR-IN-1 induces apoptosis and G1 phase cell cycle arrest, reducing angiogenesis and migration. SOS1/EGFR-IN-1 shows significant antitumor effects in prostate cancer cells PC-3 (IC50=0.45±0.03 μM) .
|
-
- HY-N4150R
-
|
Quercetagetin-7-O-glucoside (Standard)
|
Reference Standards
Phosphatase
Tau Protein
NF-κB
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Quercetagitrin (Standard) is the analytical standard of Quercetagitrin. This product is intended for research and analytical applications. Quercetagitrin (Quercetagetin-7-O-glucoside) is a natural product that can be isolated from the African marigold (Tagetes erecta). Quercetagitrin has anti-inflammatory activity. Quercetagitrin inhibits Tau accumulation. Quercetagitrin can reverse neuroinflammation and cognitive deficits in P301S-Tau transgenic mouse model through inhibiting NF-κB activation. Quercetagitrin is a dual-target inhibitor of PTPN6 (IC50 = 1 μM) and PTPN9 (IC50 = 1.7 μM). Quercetagitrin enhances glucose uptake by mature C2C12 myoblasts. Quercetagitrin can be studied in research for Alzheimer’s disease and type 2 diabetes .
|
-
- HY-178475
-
|
|
Carbonic Anhydrase
Glutathione Peroxidase
Ferroptosis
|
Cancer
|
|
CA IX/GPX4-IN-1 (Compound 22abcb) is a dual targeted inhibitor of CA IX and GPX4 activity. CA IX/GPX4-IN-1 can effectively kill SUM159PT cells (IC50 = 416 nM) by inducing iron death under hypoxic conditions. CA IX/GPX4-IN-1 has an IC50 of 663 nM to CA IX in SUM159PT-CAIX-FL cells. CA IX/GPX4-IN-1 can significantly inhibit tumor growth and can be reversed by ferroptosis inhibitors. CA IX/GPX4-IN-1 can be used for research on breast cancer and other cancers .
|
-
- HY-152254
-
|
|
FAAH
Cannabinoid Receptor
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
CB2R/FAAH modulator-3 (compound 27) is a dual targeting modulator that acts as a CB2R agonist and FAAH inhibitor. The Ki values for CB2R/FAAH modulator-3 are 20.1 and 67.6 nM for CB2R and CB1R, respectively, and the IC50 value for FAAH is 3.4 μM. CB2R/FAAH modulator-3 can be used in studies related to cancer, deleterious inflammatory cascades occurring in neurodegenerative diseases, and COVID-19 infection .
|
-
- HY-152253
-
|
|
FAAH
Cannabinoid Receptor
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
CB2R/FAAH modulator-2 (compound 26) is a dual targeting modulator that acts as a CB2R agonist and FAAH inhibitor. The Ki values for CB2R/FAAH modulator-2 are 10.8 and 152.9 nM for CB2R and CB1R, respectively, and the IC50 value for FAAH is 6.2 μM. CB2R/FAAH modulator-2 can be used in studies related to cancer, deleterious inflammatory cascades occurring in neurodegenerative diseases, and COVID-19 infection .
|
-
- HY-170947
-
|
|
STAT
Quinone Reductase
|
Cancer
|
|
Antitumor agent-195 (compound 16c) is a dual targeting agent of STAT3 and NQO1. Antitumor agent-195 significantly inhibits phosphorylation of STAT3 at Tyr705 at a concentration of 1 μM and effectively induce Apoptosis in MDAMB-231 and MDA-MB-468 breast cancer cells. Antitumor agent-195 as a NQO1 substrate strongly increases ROS generation and causes severe DNA damage in a dose-dependent manner. Antitumor agent-195 shows encouraging anti-tumor efficacy in the MDA-MB-231 xenograft model .
|
-
- HY-175713
-
|
|
Microtubule/Tubulin
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Tubulin/CDC5L-IN-1 is a Tubulin/CDC5L dual inhibitor. Tubulin/CDC5L-IN-1 targets to CDCL5 with a KD of 103.7 μM. Tubulin/CDC5L-IN-1 can inhibit multiple cancer cell proliferation and induce G2/M phase arrest. Tubulin/CDC5L-IN-1 induce cell apoptosis and ROS production. Tubulin/CDC5L-IN-1 exhibits antiangiogenic effects. Tubulin/CDC5L-IN-1 can be used for the research of cancer, such as colon carcinoma .
|
-
- HY-170779
-
|
|
FAP
|
Cancer
|
|
DOTA-NI-FAPI-04 is a FAP inhibitor (IC50 = 7.44 nM). By integrating FAP targeting with hypoxia-sensitive groups (nitroimidazole), DOTA-NI-FAPI-04 significantly enhances tumor uptake and retention capabilities. DOTA-NI-FAPI-04 chelates metallic isotopes (such as 68Ga and 177Lu) through DOTA to produce radioactive probes ([ 68Ga]Ga/DOTA-NI-FAPI-04 and [ 177Lu]Lu/DOTA-NI-FAPI-04), which can be used for research in tumor diagnostics and therapeutic agents. DOTA-NI-FAPI-04 holds dual targeting potential in the fields of cancer imaging, tumor microenvironment analysis, and radionuclide therapy, particularly suitable for scenarios where the tumor stroma and hypoxic regions synergistically interact .
|
-
- HY-145260
-
|
|
Epigenetic Reader Domain
Casein Kinase
Apoptosis
Autophagy
|
Cancer
|
|
BRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), with IC50s of 180 nM and 230 nM for BRD4 and CK2, respectively. BRD4/CK2-IN-1 has strong anticancer activity without obvious toxicities. BRD4/CK2-IN-1 induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC)
|
-
- HY-159519
-
|
|
Apoptosis
EGFR
|
Cancer
|
|
EGFR/HER2-IN-16 (compound 12K) is an effective dual-target inhibitor of EGFR (IC50=6.15 nM) and HER-2 (IC50=9.78 nM) with anti-tumor activity. EGFR/HER2-IN-16 can inhibit the migration of SK-BR-3 cells, arrest the cell cycle in the G0/G1 phase, and induce apoptosis. EGFR/HER2-IN-16 exhibits good anti-proliferative activity against tumor cell models and has little damage to healthy cells. EGFR/HER2-IN-16 can be used in breast cancer research .
|
-
- HY-153858
-
|
|
Raf
Discoidin Domain Receptor
MEK
TNF Receptor
Interleukin Related
JAK
STAT
Ras
|
Cancer
|
|
PHI-501 is a dual inhibitor targeting RAF/DDR. PHI-501 exhibits significant anti-proliferative effects in melanoma cell lines and significantly inhibits the colony formation of drug-resistant cells. PHI-501 strongly inhibits ERK and AKT phosphorylation. PHI-501 downregulates the gene sets in drug-resistant cells of TNFA-NFKB, IL6-JAK-STAT3, and KRAS signaling pathways as well as the epithelial-mesenchymal transition (EMT) signaling pathways. PHI-501 demonstrates significant anti-tumor effects in the SK-MEL3DR xenograft model. PHI-501 can be used for research on the problem of drug resistance in melanoma .
|
-
- HY-178907
-
|
|
Serotonin Transporter
5-HT Receptor
|
Neurological Disease
|
|
SERT/5-HT-IN-1 is an orally active and potent dual target inhibitor of SERT/5-HT3A (SERT IC50 = 1.5 nM, NET IC50 = 49 nM, DAT IC50 = 91 nM, 5-HT3A Ki = 12 nM). SERT/5-HT-IN-1 has an IC50 of 39 nM to 5-HT3A. SERT/5-HT-IN-1 has a lower risk of liver, kidney, and cardiac toxicity. SERT/5-HT-IN-1 can be used for research on depressive disorders .
|
-
- HY-179020
-
|
|
PARP
VEGFR
DNA/RNA Synthesis
Apoptosis
Autophagy
|
Cancer
|
|
PARP/VEGFR3-IN-1 (Compound 18) is a dual PARP-VEGFR3 target inhibitor. Its IC50 values for PARP1, PARP2, and VEGFR3 are 0.0763, 0.0366, and 4.25 nM respectively. PARP/VEGFR3-IN-1 has no inhibitory effect on VEGFR1/2 and shows subtype selectivity. PARP/VEGFR3-IN-1 exhibits significant anti-proliferative activity in various cancer cells (leukemia, lung cancer, and triple-negative breast cancer). PARP/VEGFR3-IN-1 induces DNA damage and cell cycle arrest. PARP/VEGFR3-IN-1 triggers various forms of cell death by inducing apoptosis and autophagy. PARP/VEGFR3-IN-1 can be formulated into nanodelivery systems, significantly enhancing tumor targeting and therapeutic window .
|
-
- HY-178984
-
|
|
PI3K
Epigenetic Reader Domain
DNA/RNA Synthesis
Akt
c-Myc
AMPK
|
Cancer
|
|
PI3Kα-IN-28 is an efficient dual targeted PI3K/BRD4 inhibitor. PI3Kα-IN-28 can inhibit the proliferation of various cells, such as KYSE180 (IC50 = 1.46 µM) and KYSE450 (IC50 = 0.57 µM) cells. PI3Kα-IN-28 can concentration dependently inhibit migration and colony formation, induce G0/G1 phase arrest, significantly inhibit DNA synthesis, and significantly increase the proportion of senescent cells. PI3Kα-IN-28 can inhibit the expression of p-AKT and c-Myc and activate the AMPK-p27 pathway. PI3Kα-IN-28 can be used for research on cancers such as esophageal cancer .
|
-
- HY-141853
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
BU08028 is a dual-functional agonist that targets both the μ-opioid peptide receptor (MOP) and the neuropeptide FQ receptor (NOP). BU08028 activates the inhibitory G protein (Giα), thereby inhibiting the activity of adenylate cyclase (AC), resulting in a decrease in intracellular second messenger cyclic adenosine monophosphate (cAMP) levels, and suppressing the generation and transmission of pain signals. BU08028 can take effect within 30 minutes in mouse models of neuropathic pain and inflammatory pain, and its analgesic effect can last for up to 24 hours. BU08028 has excellent safety, no addiction, respiratory depression, or side effects. BU08028 can be used for pain research .
|
-
- HY-149209
-
|
|
PROTACs
CDK
STAT
Early 2 Factor (E2F)
|
Cancer
|
|
LL-K8-22 is a potent, selective and durable PROTAC CDK8-cyclin C dual degrader, with DC50 values of 2.52 and 2.64 μM, respectively. LL-K8-22 also suppresses STAT1 Ser 727 phosphorylation. LL-K8-22 inhibits E2F- and MYC-driven carcinogenic transcriptional programs. LL-K8-22 can be used for triplenegative breast cancer (TNBC) research. (Pink: Ligand for target protein (HY-168683); Black: Linker (HY-Y0340); Blue: Ligand for E3 ligase (HY-N2427)) .
|
-
- HY-178163
-
|
|
Ferroptosis
Necroptosis
RIP kinase
Reactive Oxygen Species (ROS)
Mixed Lineage Kinase
|
Inflammation/Immunology
|
|
Zharp1-163 is a dual inhibitor of ferroptosis and necroptosis. Zharp1-163 effectively blocks ferroptosis by reducing reactive oxygen species (ROS) levels and inhibits necroptosis by potently and selectively targeting RIPK1 kinase activity (KD = 240 nM; IC50 = 406.1 nM). Zharp1-163 inhibits the cellular activation of RIPK1, RIPK3 and MLKL in response to necroptotic stimulation. Zharp1-163 markedly attenuates TNF-α (HY-P1875)-induced systemic inflammatory syndrome, including the prevention of TNF-α-induced mortality and hypothermia in mice. Zharp1-163 significantly alleviates acute kidney injury associated with both necroptosis and ferroptosis in models induced by Cisplatin (HY-17394) and ischemia-reperfusion. Zharp1-163 can be used for the study of diseases associated with cell death pathways, such as kidney disease .
|
-
- HY-176283
-
|
|
Microtubule/Tubulin
Histone Demethylase
Apoptosis
Wee1
Bcl-2 Family
Caspase
|
Cancer
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Tubulin/LSD1-IN-1 is an effective dual inhibitor of Tubulin polymerization and LSD1 (IC50 = 1.72 μM). Tubulin/LSD1-IN-1 has broad-spectrum antiproliferative activity against cancer cell lines. Tubulin/LSD1-IN-1 inhibits tubulin polymerization by targeting colchicine binding sites, thereby disrupting the microtubule network in gastric cancer cells. Tubulin/LSD1-IN-1 increases the methylation levels of H3K4me1/2 and H3K9me2/3, thereby achieving epigenetic regulation. Tubulin/LSD1-IN-1 induces G2/M arrest, promotes apoptosis, and effectively inhibits colony formation of gastric cancer cells .
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- HY-176547
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FGFR
Cytochrome P450
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Endocrinology
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FGFR2/3-IN-3 is a dual-target FGFR2/3 inhibitor with IC50s of 2.7 nM (TEL-FGFR2) and 3.9 nM (TEL-FGFR3), respectively. FGFR2/3-IN-3 has effective activity against both wild-type and mutant FGFR3. FGFR2/3-IN-3 has low CYP3A4 inhibitory effect and hERG toxicity. FGFR2/3-IN-3 improves the imbalance between chondrocyte proliferation and differentiation and promotes bone growth by inhibiting the signaling pathway mediated by mutant FGFR3. FGFR2/3-IN-3 shows a growth-promoting effect in a dwarfism mouse model and has the potential to study bone development disorder-related diseases such as achondroplasia (ACH) .
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- HY-164445
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STAT
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Cancer
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STAT3-IN-32 (compound 2p) is an orally active, potent STAT3 dual phosphorylation inhibitor with an indole-containing tetra-aromatic heterocycle scaffold. STAT3-IN-32 exhibits STAT3 luciferase inhibition activity using HEK293T cells with an IC50 of 5.3 nM and ATP production inhibition activity using BxPC-3 cells with an IC50 of 4.2 nM. STAT3-IN-32 significantly blocks p-Tyr705 and p-Ser727 and causes the abrogation of the corresponding nuclear transcription and mitochondrial oxidative phosphorylation functions of STAT3 by targeting the STAT3 SH2 domain (KD=21.3 nM). STAT3-IN-32 exhibits significant suppressive effects in a pancreatic cancer xenograft model .
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- HY-159510
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Apoptosis
VEGFR
Microtubule/Tubulin
Reactive Oxygen Species (ROS)
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Cancer
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VEGFR-2-IN-51 (compound 19) is an orally active dual-target inhibitor of VEGFR-2 (IC50=15.33 μM) and tubulin (IC50=0.76 μM) with anti-tumor activity. VEGFR-2-IN-51 induces tumor cell apoptosis by reducing mitochondrial membrane potential and increasing reactive oxygen species (ROS) levels. VEGFR-2-IN-51 exerts anti-angiogenic effects by blocking the VEGFR-2/PI3K/AKT signaling pathway. In addition, VEGFR-2-IN-51 has significant anti-proliferative activity against the gastric cancer cell line MGC-803 (IC50=0.005 μM) .
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- HY-178485
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PI3K
HDAC
Akt
Histone Methyltransferase
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Cancer
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SJY26 is a PI3K/HDAC dual-target inhibitor with IC50s of 0.59 nM (PI3Kα and PI3Kδ), 2.02 nM (PI3Kγ), 12.69 nM (PI3Kβ) and 114 nM (HDAC1). SJY26 exhibits potent broad-spectrum anti-proliferative activity, and is particularly sensitive to Jurkat and PC9R cells. SJY26 inhibited the migration of PC9R cells, arrested the cell cycle and induced cell apoptosis. SJY26 reduces AKT phosphorylation, and decreases histone H3 deacetylation (Ac-H3). SJY26 can be used for the studies of non-small cell lung cancer and leukemia .
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- HY-178029
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Ribosomal S6 Kinase (RSK)
Topoisomerase
Apoptosis
Autophagy
Reactive Oxygen Species (ROS)
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Cancer
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RSK2/TOP2-IN-1 is a RSK2/TOP2 dual inhibitor. RSK2/TOP2-IN-1 targets key tumor progression enzymes including ribosomal S6 kinase 2 and topoisomerases IIα/IIβ. RSK2/TOP2-IN-1 shows selectivity index > 2 against all squamous cell carcinoma (SCC) cell lines. RSK2/TOP2-IN-1 can induce cell apoptosis, autophagy and ROS production. RSK2/TOP2-IN-1 can be used for the research of cancer, such as squamous cell carcinoma .
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- HY-172878
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Small Interfering RNA (siRNA)
HDAC
Apoptosis
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Cancer
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HDAC/PSMD14-IN-1 (Compound 8B) is a thiolutin derivative. HDAC/PSMD14-IN-1 is a orally active dual-target inhibitor of PSMD14/HDAC1 (IC50 238.7 nM/141.2 nM, respectively). HDAC/PSMD14-IN-1 has good cytotoxicity against ESCC cell lines (IC50: 30-250 nM) and effectively reverses epithelial-mesenchymal transition (EMT). HDAC/PSMD14-IN-1 can induce apoptosis. HDAC/PSMD14-IN-1 has anti-tumor activity in a KYSE30 cell mouse xenograft model. HDAC/PSMD14-IN-1 can be used in anti-esophageal cancer research .
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- HY-179049
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EGFR
Microtubule/Tubulin
Akt
ERK
Autophagy
Atg8/LC3
p62
Ferroptosis
Reactive Oxygen Species (ROS)
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Cancer
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EGFR/tubulin-IN-1 (Compound 26) is a dual-target inhibitor of EGFR and tubulin. EGFR/tubulin-IN-1 significantly reduces the levels of p-EGFR, p-AKT, and p-ERK in cells, disrupting the microtubule structure of the cells. EGFR/tubulin-IN-1 significantly inhibits the proliferation of H1975 cells and significantly blocks the cells in the G2/M phase. EGFR/tubulin-IN-1 induces the expression of autophagy markers LC3B-II and Beclin-1, while down-regulating the expression of p62. EGFR/tubulin-IN-1 induces ferroptosis, with increased ROS content and depletion of glutathione (GSH). EGFR/tubulin-IN-1 inhibits epithelial-mesenchymal transition (EMT) and tumor metastasis. EGFR/tubulin-IN-1 has a significant tumor-suppressing effect in the H1975 transplanted tumor nude mouse model. EGFR/tubulin-IN-1 can be used for the study of non-small cell lung cancer .
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- HY-174403
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Bcl-2 Family
c-Myc
Apoptosis
Caspase
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Cancer
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c-MYC/BCL2 ligand 1 iodide is a dual-targeting c-MYC/Bcl-2 G4 ligand with Kd values of 0.90 μM (c-MYC G4) and 0.56 μM (Bcl-2 G4). c-MYC/BCL2 ligand 1 iodide inhibits c-MYC and Bcl-2 gene transcription by binding to G4-forming sequences and downregulates their protein expression. c-MYC/BCL2 ligand 1 iodide inhibits suppresses migration, induces caspase-dependent apoptosis, and triggers cell cycle G1 arrest in MCF-7 cells. c-MYC/BCL2 ligand 1 iodide significantly suppresses tumor growth in a 4T1 syngeneic model with no observable toxicity. c-MYC/BCL2 ligand 1 iodide can be used for the research of breast cancer.
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- HY-179003
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mTOR
Glutaminase
Reactive Oxygen Species (ROS)
Autophagy
Apoptosis
Ferroptosis
Glutathione Peroxidase
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Cancer
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mTOR/GLS1-IN-1 is a potent dual targeted mTOR/GLS1 inhibitor. Has anti proliferative activity against various tumor cells, such as MDA-MB-231 (IC90 = 2.14 µM), MCF-7 (IC90 = 0.91 µM), SK-BR-3 (IC90 = 0.84 µM), and 4T1 (IC90 = 0.32 µM) cells. mTOR/GLS1-IN-1 dose dependently induces ROS accumulation, induces autophagosome formation, and induces apoptosis. mTOR/GLS1-IN-1 can increase Fe 2+, decrease GPX4, and induce ferroptosis. mTOR/GLS1-IN-1 can inhibit cell migration, invasion, and angiogenesis. mTOR/GLS1-IN-1 can be used in the research of cancer, such as breast cancer .
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- HY-175655
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p38 MAPK
Cholinesterase (ChE)
Interleukin Related
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Neurological Disease
Inflammation/Immunology
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BChE/p38-α MAPK-IN-1 is a selective dual inhibitor of hBChE (IC50 = 772 nM) and p38α MAPK (IC50 = 191 nM). BChE/p38-α MAPK-IN-1 reduces the production of pro-inflammatory cytokines (IL-1β, IL-6, IL-8, TNF-α) in cells. BChE/p38-α MAPK-IN-1 improves Scopolamine (HY-N0296)-induced cognitive impairment, as well as alleviates LPS (HY-D1056)-induced spatial learning impairment and exerts anti-neuroinflammatory effects in mice. BChE/p38-α MAPK-IN-1 can be used for the study of Alzheimer’s disease (AD) by targeting both cholinergic deficit and neuroinflammation .
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- HY-172892
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PI3K
Reactive Oxygen Species (ROS)
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Cancer
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PI3K-IN-59 (Compound 3d) is a PI3K inhibitor (IC50: 17.44 μM). PI3K-IN-59 has significant antiproliferative activity and exhibits potent inhibitory effects on breast cancer 4T1 cells (IC50: 3.70 μM) and colon cancer CT26 cells (IC50: 1.98 μM) as well as human breast cancer cells (IC50: 19.72 μM). PI3K-IN-59 exerts a dual anti-tumor mechanism by inhibiting PI3Kα enzymatic activity and triggering the Fenton reaction to generate hydroxyl radicals (•OH). PI3K-IN-59 shows promising anti-4T1 tumor effects and is suitable for synergistic targeting studies in breast and colon cancers .
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- HY-117947
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Histone Methyltransferase
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Cancer
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(R)-OR-S1 is an isomer of OR-S1. The dual ZH1/2 inhibitors OR-S1 and OR-S2 exhibit strong inhibitory activity against both EZH1 and EZH2. OR-S1 and OR-S2 are highly selective methyltransferase inhibitors against EZH1 and EZH2, and they have very similar molecular features. Therefore, we investigated the effect of OR-S1 on acute myeloid leukemia (AML). We found that OR-S1 was able to induce cell differentiation and apoptosis in AML cells. These findings encouraged us to investigate whether functional LT-HSCs could survive PRC2-targeted therapy with OR-S1 or OR-S1 combined with cytarabine. The results showed that OR-S1 did not cause significant myelosuppression, and BM cells treated with the combination therapy were able to undergo normal hematopoiesis even 4 months after treatment. Therefore, temporary inhibition of EZH1 and EZH2 is clinically tolerable, making this combination therapy suitable for AML patients. AML is generally believed to originate from myeloid progenitor cells that inherit a large number of biological properties.
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- HY-163679
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Estrogen Receptor/ERR
Cytochrome P450
PROTACs
Apoptosis
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Cancer
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PROTAC ERα Degrader-9 (Compound 18c) is a dual-targeting PROTAC degrader, which degrades estrogen receptor α (ERα) and aromatase (ARO). PROTAC ERα Degrader-9 binds to ERα with a Ki of 0.25 μM, inhibits ARO with an IC50 of 4.6 μM. PROTAC ERα Degrader-9 inhibits the proliferation of MCF-7 wildtype (IC50=0.54 μM) and ERα mutants MCF-7 EGFR (IC50=0.075 μM), MCF-7 D538G (IC50=0.31 μM), MCF-7 Y537S (IC50=2.3 μM), downregulates the expressions of ERS1 and MYC. PROTAC ERα Degrader-9 arrests the cell cycle at G2/M, induces apoptosis in MCF-7. PROTAC ERα Degrader-9 exhibits antitumor efficacy in mouse models. (Pink: ligand for target protein (HY-163680); Black: linker (HY-W007559); Blue: ligand for E3 ligase (HY-112078))
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- HY-162275
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Histone Demethylase
Histone Methyltransferase
STAT
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Cancer
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JMJD1C-IN-1 is an orally active and selective inhibitor of JMJD1C (IC50 = 0.59 μM, Kd = 1.96 μM). JMJD1C-IN-1 inhibits the binding of JMJD1C to H3K9me2 peptide substrate in the HTRF assay (IC50 = 1.47 μM). JMJD1C-IN-1 disrupts intratumoral regulatory T (Treg) cell fitness by dual mechanisms: promoting H3K9me2 accumulation to downregulate PD1 expression and reducing STAT3 demethylation to enhance STAT3 activation. JMJD1C-IN-1 demonstrates dose-dependent antitumor efficacy in multiple mouse tumor models (MCA205 fibrosarcoma, B16-F10 melanoma, LLC lung cancer, Hepa1-6 hepatocellular carcinoma, CT26 colorectal cancer). JMJD1C-IN-1 can be used for the study of tumor immunotherapy by selectively targeting intratumoral Treg cells .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P11225
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MAP-04-02
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Bacterial
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Infection
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DRAMP18563 is a linear antimicrobial peptide that can act as a delivery vector to transport dual-ring peptide inhibitors that cannot penetrate the outer membrane of Gram-negative bacteria to their target sites. DRAMP18563 can be used to study the delivery strategies of dual-ring peptide inhibitors .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P99166
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PD-1/PD-L1
CTLA-4
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Inflammation/Immunology
Cancer
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Vudalimab is a potent dual PD-1 and CTLA-4 inhibitor as a fully humanized bispecific monoclonal antibody. Vudalimab targets immune checkpoint receptors PD-1 and CTLA-4 and promotes tumor-selective T-cell activation .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-113289
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- HY-N4150
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- HY-N4150R
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Quercetagetin-7-O-glucoside (Standard)
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Flavonols
Flavonoids
Source classification
Erythrina melanacantha Taub. ex Harms
Phenols
Polyphenols
Plants
Compositae
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Reference Standards
Phosphatase
Tau Protein
NF-κB
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Quercetagitrin (Standard) is the analytical standard of Quercetagitrin. This product is intended for research and analytical applications. Quercetagitrin (Quercetagetin-7-O-glucoside) is a natural product that can be isolated from the African marigold (Tagetes erecta). Quercetagitrin has anti-inflammatory activity. Quercetagitrin inhibits Tau accumulation. Quercetagitrin can reverse neuroinflammation and cognitive deficits in P301S-Tau transgenic mouse model through inhibiting NF-κB activation. Quercetagitrin is a dual-target inhibitor of PTPN6 (IC50 = 1 μM) and PTPN9 (IC50 = 1.7 μM). Quercetagitrin enhances glucose uptake by mature C2C12 myoblasts. Quercetagitrin can be studied in research for Alzheimer’s disease and type 2 diabetes .
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| Cat. No. |
Product Name |
Chemical Structure |
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- HY-168968S
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ZJY-54 is an orally active dual-target inhibitor of EGFR/LSD1, with IC50 values of 3.8 nM and 0.6 μM, respectively. ZJY-54 can inhibit the proliferation of non-small cell lung cancer cells, induce the accumulation of H3K4me2 and H3K9me2, and inhibit the phosphorylation of the EGFR signaling pathway. ZJY-54 has anti-tumor activity .
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- HY-155227S
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ALK/EGFR-IN-1-d5 (Compound (-)-9a) is a deuterated dual-target inhibitor of EGFR and ALK, with an IC50 of 1.08 nM for EGFR and an IC50 of 2.395 nM for ALK. ALK/EGFR-IN-1-d5 inhibits the phosphorylated proteins in the EGFR, ALK, and BRK signaling pathways, blocking the cell cycle, leading to a reduction in mitochondrial membrane potential and cell apoptosis (Apoptosis). ALK/EGFR-IN-1-d5 also significantly inhibits tumor growth in animal models and demonstrates good safety. ALK/EGFR-IN-1-d5 holds promise for research in the field of cancer treatment
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| Cat. No. |
Product Name |
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Classification |
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- HY-178475
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Alkynes
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CA IX/GPX4-IN-1 (Compound 22abcb) is a dual targeted inhibitor of CA IX and GPX4 activity. CA IX/GPX4-IN-1 can effectively kill SUM159PT cells (IC50 = 416 nM) by inducing iron death under hypoxic conditions. CA IX/GPX4-IN-1 has an IC50 of 663 nM to CA IX in SUM159PT-CAIX-FL cells. CA IX/GPX4-IN-1 can significantly inhibit tumor growth and can be reversed by ferroptosis inhibitors. CA IX/GPX4-IN-1 can be used for research on breast cancer and other cancers .
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- HY-159519
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Azide
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EGFR/HER2-IN-16 (compound 12K) is an effective dual-target inhibitor of EGFR (IC50=6.15 nM) and HER-2 (IC50=9.78 nM) with anti-tumor activity. EGFR/HER2-IN-16 can inhibit the migration of SK-BR-3 cells, arrest the cell cycle in the G0/G1 phase, and induce apoptosis. EGFR/HER2-IN-16 exhibits good anti-proliferative activity against tumor cell models and has little damage to healthy cells. EGFR/HER2-IN-16 can be used in breast cancer research .
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| Cat. No. |
Product Name |
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Classification |
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- HY-113289
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Cholesterol
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Brassicasterol is a metabolite of Ergosterol and has cardiovascular protective effects. Brassicasterol exerts anticancer effects in prostate cancer through dual targeting of AKT and androgen receptor signaling pathways. Brassicasterol inhibits HSV-1 (IC50=1.2 μM) and Mycobacterium tuberculosis. Brassicasterol also inhibits sterol δ 24-reductase, slowing the progression of atherosclerosis. Brassicasterol is also a cerebrospinal fluid biomarker for Alzheimer's disease .
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