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Chemical Structure : CDK7 and 9 inhibitor 14
Catalog No.: PC-61180Not For Human Use, Lab Use Only.
CDK7/9-IN-14 is a potent, selective transcriptional CDK inhibitor with Ki of 2.3 and 0.38 nM for CDK7 and CDK9, respectively.
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CDK7/9-IN-14 is a potent, selective transcriptional CDK inhibitor with Ki of 2.3 and 0.38 nM for CDK7 and CDK9, respectively.
CDK7/9-IN-14 displays >30-fold selectivity over CDK1/2/4, inhibits VEGFR2 with IC50 of 180 nM in a panel of non-CDK kinases.
CDK7/9-IN-14 demonstrates a broad spectrum of in vitro antitumor activity with average IC50 of 0.3 uM with no selectivity toward cell line types based on p53, p21, p16, or pRb status.
CDK7/9-IN-14 significantly reduces phosphorylation of both Ser-2 and Ser-5 of the RNAP-II CTD, reduces antiapoptotic protein levels in cells, and selectively induces apoptosis in transformed cells.
CDK7/9-IN-14 demonstrates antitumor activity in murine xenograft solid tumor models.
| M.Wt | 382.486 | |
| Formula | C19H22N6OS | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Wang S, et al. Chem Biol. 2010 Oct 29;17(10):1111-21.
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