KI-ARv-03

KI-ARv-03 is an academic-stage **small-molecule** selective inhibitor of cyclin-dependent kinase 9 developed in the Koehler Lab as a chemical probe and potential therapeutic lead for **castration-resistant prostate cancer**, particularly androgen receptor splice variant driven disease such as AR-V7 positive and enzalutamide-resistant models. The compound was identified through a lysate-based small-molecule microarray screen for modulators of androgen receptor variant activity and has been reported to suppress CDK9-dependent transcriptional programs, reducing androgen receptor activity and stability in prostate cancer cells. Its proposed therapeutic rationale is to disrupt transcriptional support for oncogenic androgen receptor variant signaling in resistant prostate cancer rather than directly antagonizing the androgen receptor ligand-binding domain.

Other names

(1R,3R)-N1-(5-propylpyrazolo[1,5-a]pyrimidin-7-yl)cyclopentane-1,3-diamine