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Chemical Structure : LDC000067
CAS No.: 1073485-20-7
Catalog No.: PC-21088Not For Human Use, Lab Use Only.
LDC000067 (LDC067) is a highly specific inhibitor of CDK9 with IC50 of 44 nM (CDK9-Cyclin T1), highly selective over other CDKs in the range of 55-fold (CDK2) to over 230-fold (CDK6 and CDK7).
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LDC000067 (LDC067) is a highly specific inhibitor of CDK9 with IC50 of 44 nM (CDK9-Cyclin T1), highly selective over other CDKs in the range of 55-fold (CDK2) to over 230-fold (CDK6 and CDK7).
LDC000067 displays 55/125/210/ >227/ >227-fold selectivity for CDK9 versus CDK2/1/4/6/7, shows better selectivity profile than the known and widely used inhibitors DRB and flavopiridol.
LDC000067 inhibits P-TEFb-dependent in vitro transcription in an ATP-competitive manner, decreases phosphorylation of the Ser2 residue within the CTD of RNAPII, both in cells and nuclear extracts.
CDK9 inhibition by LDC067 increases promoter-proximal RNAPII levels.
LDC000067 attenuates atherosclerosis by inhibiting inflammation and phenotypic switching of vascular smooth muscle cells.
| M.Wt | 370.43 | |
| Formula | C18H18N4O3S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(3-((6-(2-methoxyphenyl)pyrimidin-4-yl)amino)phenyl) methanesulfonamide |
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1. Albert TK, et al. Br J Pharmacol. 2014 Jan;171(1):55-68.
2. Huang S, et al. Aging (Albany NY). 2021 Jun 8;13(11):14892-14909.
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