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TAK1-inhibitor

" in MedChemExpress (MCE) Product Catalog:
Cat. No. 상품명 Target 연구분야 Chemical Structure
  • HY-103490
    Takinib
    Maximum Cited Publications
    28 Publications Verification

    EDHS-206

    		 MAP3K Apoptosis Infection Inflammation/Immunology Cancer
    Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor (IC50=9.5 nM), more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is also a P. falciparum protein kinase 9 (PfPK9) inhibitor (KD(app) of 0.46 μM) [1] .
    Takinib
  • HY-147141
    HS-276
    2 Publications Verification

    		 IRAK TNF Receptor Casein Kinase Interleukin Related Inflammation/Immunology
    HS-276 is an orally active, potent and highly selective TAK1 inhibitor, with a Ki of 2.5 nM. HS-276 shows significant inhibition of TAK1, CLK2, GCK, ULK2, MAP4K5, IRAK1, NUAK, CSNK1G2, CAMKKβ-1, and MLK1, with IC50 values of 8.25, 29, 33, 63, 125, 264, 270, 810, 1280, and 5585 nM, respectively. HS-276 reduces the expression of TNF, IL-6, and IL-1β. HS-276 can be used for rheumatoid arthritis (RA) research [1].
    HS-276
  • HY-136848
    SM1-71

    		MAP3K Src FGFR Ribosomal S6 Kinase (RSK) LIM Kinase (LIMK) Cancer
    SM1-71 (compound 5) is a potent TAK1 inhibitor, with a Ki of 160 nM, it also can covalently inhibit MKNK2, MAP2K1/2/3/4/6/7, GAK, AAK1, BMP2K, MAP3K7, MAPKAPK5, GSK3A/B, MAPK1/3, SRC, YES1, FGFR1, ZAK (MLTK), MAP3K1, LIMK1 and RSK2. SM1-71 can inhibit proliferation of multiple cancer cell lines [1] .
    SM1-71
  • HY-122642
    TAK1-IN-4

    		MAP3K Inflammation/Immunology
    TAK1-IN-4 (Compound 14) is a TAK1 inhibitor [1].
    TAK1-IN-4
  • HY-115743
    TAK1-IN-3

    		MAP3K Cancer
    TAK1-IN-3 is a potent ATP-competitive TAK1 inhibitor.
    TAK1-IN-3
  • HY-132172
    TAK1-IN-2

    		MAP3K Cancer
    TAK1-IN-2 is a potent and selective TAK1 inhibitor, with an IC50> of 2 nM [1].
    TAK1-IN-2
  • HY-169949
    TAK-756

    		MAP3K NF-κB MMP Leukotriene Receptor Inflammation/Immunology
    TAK-756 is a selective transforming growth factor β-activated kinase 1 (TAK1) inhibitor with a target pIC50 of 8.6. TAK-756 can inhibit TAK1 autophosphorylation and downstream NF-κB phosphorylation, suppress the production of inflammatory and catabolic factors such as MMP-3 and IL-6. TAK-756 exhibits anti-inflammatory effects in a rat joint inflammation model. TAK-756 can be used for the research of inflammatory joint disease, osteoarthritis [1].
    TAK-756
  • HY-103490R
    Takinib (Standard)

    EDHS-206 (Standard)

    		 Reference Standards MAP3K Apoptosis Infection Inflammation/Immunology Cancer
    Takinib (Standard) is the analytical standard of Takinib. This product is intended for research and analytical applications. Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor (IC50=9.5 nM), more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is also a P. falciparum protein kinase 9 (PfPK9) inhibitor (KD(app) of 0.46 μM) [1] .
    Takinib (Standard)
  • HY-147141A
    HS-276 hydrochloride

    		IRAK TNF Receptor Casein Kinase Interleukin Related Inflammation/Immunology
    HS-276 hydrochloride is an orally active, potent and highly selective TAK1 inhibitor, with a Ki of 2.5 nM. HS-276 hydrochloride shows significant inhibition of TAK1, CLK2, GCK, ULK2, MAP4K5, IRAK1, NUAK, CSNK1G2, CAMKKβ-1, and MLK1, with IC50 values of 8.25, 29, 33, 63, 125, 264, 270, 810, 1280, and 5585 nM, respectively. HS-276 hydrochloride reduces the expression of TNF, IL-6, and IL-1β. HS-276 hydrochloride can be used for rheumatoid arthritis (RA) research [1].
    HS-276 hydrochloride
  • HY-147141B
    HS-276 formic

    		IRAK TNF Receptor Casein Kinase Interleukin Related Inflammation/Immunology
    HS-276 formic is an orally active, potent and highly selective TAK1 inhibitor, with a Ki of 2.5 nM. HS-276 formic shows significant inhibition of TAK1, CLK2, GCK, ULK2, MAP4K5, IRAK1, NUAK, CSNK1G2, CAMKKβ-1, and MLK1, with IC50 values of 8.25, 29, 33, 63, 125, 264, 270, 810, 1280, and 5585 nM, respectively. HS-276 formic reduces the expression of TNF, IL-6, and IL-1β. HS-276 formic can be used for rheumatoid arthritis (RA) research [1].
    HS-276 formic

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