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).
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.
