Chemical Name: 3-[[6-(2-Methoxyphenyl)-4-pyrimidinyl]amino]benzenemethanesulfonamide
Biological ActivityLDC 000067 is a potent and selective CDK9 inhibitor (IC50 = 44 nM at CDK9-cyclin T1). Inhibits other CDKs in the micromolar range (IC50 values are 2.4, 5.5, 9.2, >10 and >10 μM for CDK2-cyclin A, CDK1-cyclin B1, CDK4-cyclin D1, CDK6-cyclin D3 and CDK7-cyclin H-MAT1, respectively). Inhibits P-TEFb-dependent in vitro transcription. Induces apoptosis in vitro and in vivo in combination with BI 894999.
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For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Characterization of molecular and cellular functions of the cyclin-dependent kinase CDK9 using a novel specific inhibitor.
Albert et al.
The novel BET bromodomain inhibitor BI 894999 represses super-enhancer-associated transcription and synergizes with CDK9 inhibition in AML.
Gerlach et al.
Systematic kinase inhibitor profiling identifies CDK9 as a synthetic lethal target in NUT midline carcinoma.
Brägelmann et al.
Cell Rep., 2017;20:2833
How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases?
Jorda et al.
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