TCS JNK 5a

A selective inhibitor of JNK2 and JNK3

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Background

TCS JNK 5a is a selective inhibitor of JNK2 and JNK3 with pIC50 values of 6.7 and 7.5, respectively [1].

c-Jun N-terminal kinases (JNK) belong to the mitogen-activated protein kinase (MAPK) family. JNK1 and JNK2 are widely expressed, whereas JNK3 is mainly expressed in the brain and plays an important role to mediate neurodegeneration such as Alzheimer’s Disease and Parkinson’s Disease [1].

TCS JNK 5a is a selective JNK2 and JNK3 inhibitor. TCS JNK 5a exhibited selective against JNK1 and p38α with pIC50 values of 6.7, 6.5, <5.0 and <4.8 for JNK3, JNK2, JNK1 and p38α, respectively. Also, TCS JNK 5a was inactive at EGFR, ErbB2, VegFr2, Src, Tie-2, Alk5, c-Fms, CDK-2, GSK3β and PLK1 with pIC50 values of < 5.0 [1].

Reference:
[1].? Angell RM, Atkinson FL, Brown MJ, et al. N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3. Bioorg Med Chem Lett, 2007, 17(5): 1296-1301.