2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
生物活性
Description
In Vivo
In Vitro
化合物的使用
Kinase Assay
Cell Assay
Animal Administration
参考文献
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.
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.