| S8663 |
Takinib (EDHS-206)
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Takinib is a potent and selective TAK1 inhibitor with an IC50 of 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 induces apoptosis.
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Gut Microbes, 2024, 16(1):2402543
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Chemosphere, 2024, 368:143785
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Nat Commun, 2023, 14(1):143
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| S8868 |
NG25
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NG25 is a novel inhibitor of TAK1 with enzymatic IC50s of 149 and 21.7 nM for TAK1 and MAP4K2 respectively.
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Int J Biol Sci, 2024, 20(2):606-620
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Biochem J, 2022, 479(20):2195-2216
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Lab Invest, 2021, 10.1038/s41374-021-00671-w
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| E1155 |
HS-276
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HS-276, a potent and highly selective orally bioavailable transforming growth factor-β activated kinase-1 (TAK1) inhibitor with the Ki and IC50 of 2.5 nM and 2.3 nM respectively, shows significant inhibition of TNF-mediated cytokine profiles, correlating with significant attenuation of arthritic-like symptoms in the collagen-induced arthritis (CIA) mouse model of inflammatory rheumatoid arthritis (RA).
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| S3607 |
Sarsasapogenin
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Sarsasapogenin (SAR, Parigenin) is a steroidal sapogenin. It can provoke the generation of reactive oxygen species and activate unfolded protein response (UPR) signalling pathways. This compound potently inhibits NF-κB and MAPK activation, as well as IRAK1, TAK1, and IκBα phosphorylation in LPS-stimulated macrophages.
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J Exp Clin Cancer Res, 2022, 41(1):174
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| S3226 |
Dehydroabietic acid
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Dehydroabietic acid (DAA, DHAA), a naturally occurring diterpene resin acid derived from coniferous plants such as Pinus and Picea, displays anti-inflammatory activity via suppression of Src-, Syk-, and TAK1-mediated pathways.
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| E2821 |
RGB-286638 free base
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RGB-286638 free base is a Cyclin-dependent kinase (CDK) inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
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