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Multi-kinase inhibition

" in MedChemExpress (MCE) Product Catalog:

7

Inhibitors & Agonists

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Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-12037A
    Rigosertib
    5+ Cited Publications

    ON-01910

    Polo-like Kinase (PLK) PI3K Apoptosis Cancer
    Rigosertib (ON-01910) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3 kinase/Akt pathway, promots the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle . Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM .
    Rigosertib
  • HY-12037
    Rigosertib sodium
    5+ Cited Publications

    ON-01910 sodium

    Polo-like Kinase (PLK) PI3K Apoptosis Cancer
    Rigosertib sodium (ON-01910 sodium) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3K/Akt pathway, promotes the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle . Rigosertib sodium is a selective and non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM .
    Rigosertib sodium
  • HY-149415

    RET FGFR VEGFR c-Kit c-Met/HGFR PDGFR Raf Cancer
    Multi-kinase-IN-5 (compound 15c) is a promising multi-kinase inhibitory agent. Multi-kinase-IN-5 inhibits a panel of protein kinases (RET, KIT, cMet, VEGFR1,2, FGFR1, PDGFR and BRAF), showing % inhibition of 74%, 31%, 62%, 40%, 73%, 74%, 59%, and 69%, respectively, and IC50 of 1.287, 0.117 and 1.185 μM against FGFR1, VEGFR, and RET kinases, respectively .
    Multi-kinase-IN-5
  • HY-150027

    VEGFR PDGFR Cancer
    Multi-kinase-IN-3 (compound 2) is a potent angiokinase inhibitor. Multi-kinase-IN-3 shows inhibition activity against VEGFR-2 and PDGFRβ, with IC50 values of 58.3 and 55 nM, respectively .
    Multi-kinase-IN-3
  • HY-178942

    VEGFR EGFR Apoptosis Bcl-2 Family Caspase MDM-2/p53 Cancer
    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 .
    EGFR/VEGFR2-IN-9
  • HY-175477

    DAPK DYRK PDGFR IPK Superfamily Cancer
    UNC9750 is an inositol phosphate multikinase (IPMK) inhibitor with IC50 values ​​of 31.6 and 374 nM for IPMK and IP6K2, respectively.. UNC9750 inhibits cellular accumulation of InsP5, the direct product of IPMK kinase activity, while having no effect on either InsP6 or InsP7 levels. UNC9750 has ≥ 75% inhibition of four kinases (DAPK1, DYRK1B, PDGFR, and KDR). UNC9750 can be used for the study of glioblastoma .
    UNC9750
  • HY-125387

    Src Inflammation/Immunology
    TOP1210 is a narrow-spectrum tyrosine kinase inhibitor with potent inhibitory activity against P38α, Src, and Syk kinases. TOP1210 effectively reduced proinflammatory cytokines released by peripheral blood monocytes, primary macrophages, HT29 cells, inflammatory cells in ulcerative colitis (UC) biopsies, and myofibroblasts isolated from inflamed colonic UC mucosa. TOP1210 showed significant anti-inflammatory effects in cell experiments and UC biopsies, superior to some selective kinase inhibitors. The multi-kinase inhibition of TOP1210 provides the possibility of obtaining a wider range of therapeutic effects, especially in the regulation of autoimmune responses .
    TOP1210

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