Senexin A|cas 1366002-50-7

Cas No.:	1366002-50-7
SMILES:	N#CC1=CC=C2C(C(NCCC3=CC=CC=C3)=NC=N2)=C1
Formula:	C₁₇H₁₄N₄
M.Wt:	274.32
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

In vitro: p21 is shown to activate NF-κB–dependent transcription, and Senexin A inhibits p21-stimulated activity of the consensus NF-κB–dependent promoter. Senexin A has no effect on p21 induction by IPTG, on cell growth with or without p21, or on p21-induced senescent phenotype. Senexin A does not affect the inhibition of gene expression by p21 and does not interfere with p21-mediated inhibition of large sets of genes belonging to Gene Ontology (GO) categories of mitosis and DNA replication. Senexin A inhibits only p21-induced transcription but not other biological effects of p21. Senexin A inhibits CDK8 and CDK19 ATP site binding with Kd50 of 0.83 μM and 0.31 μM, respectively and CDK8 kinase activity with IC50 of 0.28 μM. Senexin A inhibits β-catenin–dependent transcription in HCT116 colon carcinoma cells. It does not inhibit ROCK and did not share cortistatin A's strong antiendothelial cell activity. In vivo: The CDK8/19 inhibitor Senexin A reverses chemotherapy-induced paracrine tumor-promoting activities in vivo and does not inhibit reporter cell growth and showed no detectable toxicity in a mouse study.

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