872573-93-8

RO-3306 (872573-93-8) is a selective inhibitor of CDK1 (IC50?= 35 nM versus CDK2 IC50?= 340nM).1,2?It induces G2/M phase cell cycle arrest and apoptosis. Inhibition of CDK1 with RO-3306 has been shown to have synergistic effects with PARP inhibitors in treating various breast cancers.3,4?It has also been demonstrated to overcome apoptotic resistance in BRAFV600E?human colorectal cancer cells.5

Inhibitor of CDK1/cyclin B1 and CDK1/cyclin A. Reversibly arrests human cells at the G2/M border of the cell cycle. Allows for effective cell synchronisation in early mitosis. Downregulates expression of the antiapoptotic proteins Bcl-2 and survivin and blocks p53-mediated induction of p21 and MDM2.

RO-3306 is a selective ATP-competitive inhibitor of CDK1. It inhibites CDK1 cyclin B1 activity with Ki of 35 nM, nearly 10-fold selectivity relative to CDK2/cyclin E and over 50-fold relative to CDK4/cyclin D. RO-3306 has been used to cause cell cycle arrest at the G2/M boundary.

CDK1: 20 nM (Ki); CDK1/cyclinB1: 35 nM (Ki); CDK1/cyclin A: 110 nM (Ki); CDK2/cyclinE: 340 nM (Ki); PKCδ: 318 nM (Ki); SGK: 497 nM (Ki); ERK: 1980 nM (Ki)

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1) Vassilev?et al.?(2006),?Selective small-molecule inhibitor reveals critical mitotic functions of human CDK1; Proc. Nat. Acad. Sci. USA?103?10660 2) Krasinska?et al.?(2008),?Selective chemical inhibition as a tool to study Cdk1 and Cdk2 functions in the cell cycle; Cell Cycle?7?1702 3) Pierce?et al.?(2013),?Comparative antiproliferative effects of iniparib and olaparib on a panel of triple-negative and non-triple-negative breast cancer cell lines; Cancer Biol. Ther.?14?537 4) Xia?et al.?(2014),?The CDK1 inhibitor RO3306 improves the response of BRCA-proficient breast cancer cells to PARP inhibition;?Int. J. Oncol.?44?735 5) Zhang?et al.?(2018),?Targeting CDK1 and MEK/ERK Overcomes Apoptotic Resistance in BRAF-Mutant Human Colorectal Cancer; Mol. Cancer Res.?16?378