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

Chemical Structure : Cortistatin A

Cortistatin A ((+)-cortistatin A)

Catalog No.: 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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Biological Activity

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.

Physicochemical Properties

M.Wt	472.629
Formula	C30H36N2O3
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
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

References

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)

Biological Activity

Physicochemical Properties

References

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