Takinib

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][2][3].

Product Specifications

CAS Number

[1111556-37-6]

Product Name Alternative

EDHS-206

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; MAP3K

Type

Reference compound

Related Pathways

Apoptosis; MAPK/ERK Pathway

Applications

Cancer-Kinase/protease

Field of Research

Cancer; Infection; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/Takinib.html

Purity

99.48

Solubility

DMSO : 2.5 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

CCCN1C2=CC=CC=C2N=C1NC(C3=CC(C(N)=O)=CC=C3)=O

Molecular Formula

C18H18N4O2

Molecular Weight

322.36

Precautions

H302, H315, H319, H335

References & Citations

[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.|[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.|[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.|[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.|[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.