EDHS-206 MedChemExpress (MCE)

Product Name	Takinib
Synonyms	Takinib EDHS-206 1111556-37-6 N-(1-Propyl-1H-benzo[d]imidazol-2-yl)isophthalamide N1-(1-Propyl-1H-benzo[d]imidazol-2-yl)isophthalamide 3-N-(1-propylbenzimidazol-2-yl)benzene-1,3-dicarboxamide Synonyms Takinib EDHS-206 1111556-37-6 N-(1-Propyl-1H-benzo[d]imidazol-2-yl)isophthalamide N1-(1-Propyl-1H-benzo[d]imidazol-2-yl)isophthalamide 3-N-(1-propylbenzimidazol-2-yl)benzene-1,3-dicarboxamide 1,3-Benzenedicarboxamide, N1-(1-propyl-1H-benzimidazol-2-yl)- 1-N-(1-propyl-1H-1,3-benzodiazol-2-yl)benzene-1,3-dicarboxamide
CAS	1111556-37-6
EINECS
Chemical Formula	C18H18N4O2
Molecular Weight	322.36
inchi
Package	10 mM * 1 mL;1 mg;5 mg;25 mg;50 mg;100 mg
Price	Email to quote
Descriptions	Takinib Takinib MedChemExpress (MCE) HY-103490 1111556-37-6 EDHS-206 98.92% Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months Room temperature in continental US Descriptions Takinib Takinib MedChemExpress (MCE) HY-103490 1111556-37-6 EDHS-206 98.92% Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months Room temperature in continental US may vary elsewhere. 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). Takinib (10-10000 nM 24 hours) induces apoptosis following TNF-α stimulation in MDA-MB-231 cells[1]. Takinib (10 μM 0-1 hours) reduces phosphorylation of IKK and p65[1]. Takinib serves as a chemical starting point for the development of PfPK9 (KD(app) of 0.46 μM) inhibitors for malaria[3]. Takinib (2 hours 0.1-20 μM human RASFs) induces phosphorylation of TAK1Thr184/187, STAT3Tyr705 and STAT3Ser727 in IL-1β-treated (10 ng/mL 30 min) RASFs[4]. Takinib (50 mg/kg intraperitoneally daily from days 18-36) reduces the clinical score in type II collagen-induced arthritis (CIA) mouse model of rheumatoid arthritis[4]. Takinib (50 mg/kg oral gavage daily until 17 days) slows tumor growth in the Hodgkin lymphoma xenograft NSG mice[5]. TAK1 9.5 nM (IC50) IRAK4 120 nM (IC50) IRAK1 390 nM (IC50) GCK 430 nM (IC50) CLK2 430 nM (IC50) MINK1 1.9 μM (IC50) \| \| \| \| \| \| \| \| \| \| [1]. Totzke J, et al. Takinib, a Selective TAK1 Inhibitor, Broadens the Therapeutic Efficacy of TNF-α Inhibition for Cancer and Autoimmune Disease. Cell Chem Biol. 2017 Aug 17 24(8):1029-1039. [Content Brief] [2]. Scarneo SA, et.al. Pharmacological inhibition of TAK1, with the selective inhibitor takinib, alleviates clinical manifestation of arthritis in CIA mice. Arthritis Res Ther. 2019 Dec 17 21(1):292. [Content Brief] [3]. Raphemot R, et al. Plasmodium PK9 Inhibitors Promote Growth of Liver-Stage Parasites. Cell Chem Biol. 2019 Mar 21 26(3):411-419.e7. [Content Brief] [4]. Panipinto PM, et.al. Takinib Inhibits Inflammation in Human Rheumatoid Arthritis Synovial Fibroblasts by Targeting the Janus Kinase-Signal Transducer and Activator of Transcription 3 (JAK/STAT3) Pathway. Int J Mol Sci. 2021 22(22):12580. Published 2021 Nov 22. [Content Brief] [5]. Song Z,et.al. Essential role of the linear ubiquitin chain assembly complex and TAK1 kinase in A20 mutant Hodgkin lymphoma. Proc Natl Acad Sci U S A. 2020 Nov 17 117(46):28980-28991. [Content Brief]
Last Update	2025-04-01 14:45:47

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