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LDC000067 CAS: 1073485-20-7

Category: Inhibitors
Product Name: LDC000067
Cat No: I000339
CAS No: 1073485-20-7
Synonyms: (3-((6-(2-methoxyphenyl)pyrimidin-4-yl)amino)phenyl)methanesulfonamide
Molecular Formula: C18H18N4O3S
Molecular Weight: 370.43
SMILES: COC1=CC=CC=C1C2=CC(NC3=CC=CC(CS(N)(=O)=O)=C3)=NC=N2
Solubility: DMSO: ≥ 47 mg/mL
Target: Cyclin-Dependent Kinases
IC50: 32.7 nM [1]
Storage: Desiccate at -20°C
CAS 1073485-20-7,LDC000067
  • Description

LDC000067(LDC-067) is a highly specific CDK9 inhibitor with IC50 of 32.7 nM for CDK9/cyclin T1; displays 55/125/210/ >227/ >227-fold selectivity for CDK9 versus CDK2/1/4/6/7.
IC50 value: 32.7 nM [1]
Target: CDK9 inhibitor
The selectivity of LDC000067 for CDK9 over other CDKs exceeded that of the known inhibitors flavopiridol and DRB. LDC000067 inhibited in vitro transcription in an ATP-competitive and dose-dependent manner. Gene expression profiling of cells treated with LDC000067 demonstrated a selective reduction of short-lived mRNAs, including important regulators of proliferation and apoptosis. LDC000067 represents a promising lead for the development of clinically useful, highly specific CDK9 inhibitors.

  • References


[1]. Albert TK, et al. Characterization of molecular and cellular functions of the cyclin-dependent kinase CDK9 using a novel specific inhibitor. Br J Pharmacol. 2014 Jan;171(1):55-68.


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