KB-0742 Dihydrochloride is a potent, selective, and orally bioavailable small molecule inhibitor of the transcription elongation cofactor CDK9 with IC50 of 6 nM for CDK9/cyclin T1 inhibition at 10 μM ATP.
KB-0742 Dihydrochloride is a potent, selective, and orally bioavailable small molecule inhibitor of the transcription elongation cofactor CDK9 with IC50 of 6 nM for CDK9/cyclin T1 inhibition at 10 μM ATP.
KB-0742 rapidly downregulates nascent transcription, preferentially depleting short half-life transcripts and AR-driven oncogenic programs in 22Rv1 cells. [1]
KB-0742 is a remarkably selective CDK9 inhibitor that leads to global downregulation of nascent transcription and AR-driven prostate cancer gene expression programs and displays in vivo efficacy in CRPC- and AML-derived xenograft models.[1]
[1] André Richters, et al. Cell Chem Biol . 2021 Feb 18;28(2):134-147.e14.
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