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LDC000067

Chemical Structure : LDC000067

CAS No.: 1073485-20-7

LDC000067 (LDC-000067, LDC 000067, LDC067)

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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 370.43
Formula C18H18N4O3S
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

(3-((6-(2-methoxyphenyl)pyrimidin-4-yl)amino)phenyl) methanesulfonamide

References

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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