LDC000067

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

LDC000067 是一种高度特异性和选择性的 CDK9 抑制剂，IC50 值为 44±10 nM。

LDC000067 is a potent and selective CDK9 inhibitor. 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. Analysis of de novo?RNA synthesis suggested a wide ranging positive role of CDK9. At the molecular and cellular level, LDC000067 reproduced effects characteristic of CDK9 inhibition such as enhanced pausing of RNA polymerase II on genes and, most importantly, induction of apoptosis in cancer cells.

The selectivity of LDC000067 for CDK9 over other CDKs exceeds that of the known inhibitors flavopiridol and DRB. LDC000067 displayed 55/125/210/ >227/ >227-fold selectivity for CDK9 versus CDK2/1/4/6/7. LDC000067 inhibits in vitro transcription in an ATP-competitive and dose-dependent manner. Gene expression profiling of cells treated with LDC000067 demonstrates a selective reduction of short-lived mRNAs, including important regulators of proliferation and apoptosis.

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LDC000067 | LDC-000067 | LDC 000067

Others

Other Targets

CDK1| CDK2| CDK4| CDK6| CDK9

Cancer

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1073485-20-7

370.43

C18H18N4O3S

>98% (HPLC)

DMSO : ≥ 47 mg/mL 126.88 mM

COc1ccccc1c1cc(ncn1)Nc1cccc(c1)CS(=O)(=O)N

6-(6-(1-Methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-ylthio)quinoline

(-20℃)

With Ice Pack

≥ 2 years