tak1

TAK1/MAP4K2 inhibitor 1 (compound 5) is a dual kinase inhibitor of TAK1 and MAP4K2 with IC50 values of 41.1 nM and 18.2 nM, respectively.

TAK1-IN-3 is a novel ATP-competitive TAK1 inhibitor for the study of cancer.

TAK1 inhibitor is an inhibitor, which can inhibit MCF-7, A549, DU-145 and MDA MB-231, with IC50 of 0.021, 0.14, 0.064 and 0.19, respectively. TAK1 inhibitor showed good antibacterial activity with microphones ranging from 93.7 to 46.9μg/mL and from 7.8 to 5.8μg/mL.

TAK1-IN-2 is a potent and selective TAK1 inhibitor with an IC50 of greater than 2 nM [1].

AZ-Tak1 is a potent and a relatively selective inhibitor of TAK1 kinase activity, with an IC50 of 0.009 mM. AZ-Tak1 treatment decreased the level of p38 and ERK in mantle cell lymphoma cells, and induced apoptosis in a dose and time dependent manner, with an IC50 of 0.1–0.5 mM. Using the annexin-V and PI staining and FACS analysis, After 48 hours of incubation, AZ-Tak1 (0.1 mM) induced apoptosis in 28%, 34% and 86% of Mino, SP53, and Jeko cells, respectively, which was increased to 32%, 42%, and 86% when 0.5 mM concentration was used.

5Z-7-Oxozeaenol (FR148083) is a potent, irreversible and selective inhibitor of transforming growth factor (TGF)-β-activated kinase 1 with IC50 of 8.1 nM for TAK1 and low activity against MEK1 with IC50 of 411 nM, it is also an inhibitor of VEGF-R2 with IC50 of 52 nM.

SM1-71 is a potent multi-targeted acrylamide-modified TAK1 inhibitor that inhibits 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 be used as a kinase probe with anticancer activity and inhibits the proliferation of various cancer cell lines.

Takinib (EDHS-206) is a specific and effective TAK1 inhibitor(IC50= 9.5 nM).

HS220 is an inhibitor of TAK1 which plays a key role in the signaling pathways of inflammation and cell survival.

HS-243 is an inhibitor of IRAK-4 and IRAK-1 with IC50s of 20 and 24 nM. HS-243 shows anti-inflammatory and anticancer activity.

(R)-STU104 is a novel TAK1-MKK3 protein-protein interaction (PPI) inhibitor that inhibits TNF-α and suppresses the TAK1/MKK3/p38/MnK1/MK2/elF4E signalling pathway by binding to MKK3 and disrupting TAK1 phosphorylation of MKK3. (R)-STU104 is a candidate compound for the treatment of ulcerative colitis.

TAK-715 is a p38 MAPK inhibitor for p38α.

HS-276 is a highly selective, orally active inhibitor of TAK1 (Ki: 2.5 nM). HS-276 significantly inhibits TAK1 (IC50: 8.25 nM), CLK2 (IC50: 29 nM), GCK (IC50: 22 nM), ULK2 (IC50: 63 nM), MAP4K5 (IC50. HS-276 can be used to study rheumatoid arthritis (RA).

NG25 is a potent dual inhibitor of TAK1 and MAP4K2, with IC50s of 149 nM and 21.7 nM, respectively.

KW 4099 is a thromboxane A2 antagonist.

TAK1-IN-5 (Compound 26) is an inhibitor of transforming growth factor-β activated kinase (TAK1) with an IC50 value of 55 nM. It effectively suppresses the growth of MPC-11 and H929 cells, with a GI50 below 30 nM. TAK1-IN-5 is a useful tool for research in multiple myeloma.

TAK-137 is an AMPA receptor enhancer with antidepressant effects. TAK-137 has the ability to improve cognition and could be used to study schizophrenia.

RGB-286638 free base is a novel CDK inhibitor with IC50s of 1 nM/2 nM/3 nM/4 nM/5 nM for cyclin T1-CDK9/cyclin B1-CDK1/cyclin E-CDK2/cyclin D1-CDK4/cyclin E-CDK3/p35-CDK5 respectively; less potent against cyclin H-CDK7 and cyclin D3-CDK6.

PF-05381941 is a selective and potent dual inhibitor of TAK1 and p38α with IC 50 =156 nM/186nM that inhibits the kinase activity of TAK1 by binding to its active site.

RGB-286638 is a multi-target CDK inhibitor that effectively hampers the kinase activity of a range of cyclin-CDK complexes, including cyclin T1-CDK9 (IC50 = 1 nM), cyclin B1-CDK1 (IC50 = 2 nM), cyclin E-CDK2 (IC50 = 3 nM), cyclin D1-CDK4 (IC50 = 4 nM), cyclin E-CDK3 (IC50 = 5 nM), and p35-CDK5 (IC50 = 5 nM). Additionally, it inhibits other kinases such as GSK-3β (IC50 = 3 nM), TAK1 (IC50 = 5 nM), Jak2 (IC50 = 50 nM), and MEK1 (IC50 = 54 nM), showcasing its versatile inhibitory potential.

Tak 187 is a long-lasting inhibitor of ergosterol biosynthesis.

Zanapezil is an acetylcholinesterase (AChE) inhibitor. Zanapezil increases choline acetyltransferase activity in cultured rat septal cholinergic neurons.

Serabelisib (INK1117) is a p110α/β/γ/δ inhibitor (IC50: 15/4.5/1.9/13.39 μM).

Zanapezil (TAK-147) is a powerful and selective inhibitor of acetylcholine esterase (AChE). It demonstrates significant and reversible inhibition of AChE activity in rat cerebral cortex homogenates (IC50 = 51.2 nM). Furthermore, Zanapezil exhibits moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. This compound holds promise for the investigation of the initial stages of Alzheimer's disease (AD).