Senexin A

製品コードS8520 バッチS852001

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₇H₁₄N₄
	分子量	274.32	CAS No.	1366002-50-7
Solubility (25°C)*	体外	DMSO	54 mg/mL (196.85 mM)
		Ethanol	54 mg/mL (196.85 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Senexin A is a potent and selective inhibitor of CDK8 and its nearest relative, CDK19 with Kd values of 0.83 μM and 0.31 μM for CDK8 and CDK19 ATP site binding, respectively.
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^[1].
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^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	MEF
	濃度	1 μM
	反応時間	24 h
	実験の流れ	For conditioned media mitogenic assays, MEF, untreated or treated for 24 h with 200 nM doxorubicin, alone or in combination with 1 μM Senexin A, were washed and cultured for 48 h without drugs to collect conditioned media. The media were added to A549 cells, plated on 12-well plates at 10⁴ cells per well; cells were counted after 48 h using the trypan blue exclusion assay. Experiments were performed in triplicate, and cells counted in at least three optical fields per experiment.
動物実験	動物モデル	C57BL/6 mice
	投薬量	20 mg/kg
	投与方法	i.p.

参考

[1] Porter DC, et al. Proc Natl Acad Sci U S A. 2012, 109(34):13799-804.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

P-TEFb promotes cell survival upon p53 activation by suppressing intrinsic apoptosis pathway [ Nucleic Acids Res, 2023, gkad001]	PubMed: 36727434
Combined inhibition of EZH2 and ATM is synthetic lethal in BRCA1-deficient breast cancer [ Breast Cancer Res, 2022, 24(1):41]	PubMed: 35715861

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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