Cortistatin A |CAS:882976-95-6 Probechem Biochemicals

Chemical Structure : Cortistatin A

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Cortistatin A ((+)-cortistatin A)

货号: PC-60894Not For Human Use, Lab Use Only.

Cortistatin A is a potent and selective inhibitor of mediator-associated kinase CDK8 (IC50=12 nM) and its paralogue CDK19.

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生物&药学活性

Cortistatin A is a potent and selective inhibitor of mediator-associated kinase CDK8 (IC50=12 nM) and its paralogue CDK19.
Cortistatin A does not inhibit other transcriptional CDKs CDK7 (TFIIH), CDK9 (P-TEFb), CDK12, or CDK13 in vitro, and no activity against CDK9, CDK12, CDK13, ROCK1 or ROCK2 in MOLM-14 cell lysate (>2.5 uM), also binds to ROCK1 and ROCK2.
Cortistatin A demonstrates antileukaemic activity by inhibiting Mediator kinases in vitro and in vivo.

物理化学性质&存储条件

分子量	472.629
分子式	C30H36N2O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(3S,3aR,7R,8R,9S,10aR,12aS,12bR)-9-(Dimethylamino)-1,2,3,3a,4,7,8,9,10,11,12,12b-dodecahydro-3-(7-isoquinolinyl)-3a-methyl-10a,12a-epoxybenzo[4,5]cyclohept[1,2-e]indene-7,8-diol

参考文献

1. Johannessen L, et al. Nat Chem Biol. 2017 Oct;13(10):1102-1108.

2. Cee VJ, et al. Angew Chem Int Ed Engl. 2009;48(47):8952-7.

3. Poss ZC, et al. Cell Rep. 2016 Apr 12;15(2):436-50.

4. Pelish HE, et al. Nature. 2015 Oct 8;526(7572):273-276.

Cortistatin A ((+)-cortistatin A)

生物&药学活性

物理化学性质&存储条件

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Cortistatin A ((+)-cortistatin A)

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物理化学性质&存储条件

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