An ATP-competitive, potent CDK1 inhibitor
CAS：872573-93-8
分子式：C18H13N3OS2
分子量：351.45
纯度：98%
存储：Store at -20°C

Background:

RO-3306 is an ATP-competitive, potent cyclin-dependent kinase (CDK) 1 inhibitor with Ki values of 35 and 110 nM for cdk1/cyclin B1 and cdk1/cyclin A, respectively.
Cell cycle progression is regulated by a series of CDKs. Cdk1 controls the cell cycle entry into mitosis. It forms a bipartite complex with cyclin B and phosphorylates a spectrum of substrates that coordinate nuclear envelope breakdown, chromosome condensation, assembly of the mitotic spindle and activation of the spindle assembly checkpoint.  
CDK1 inhibitor RO-3306 was reported to impair BRCA1 localization to DSBs, and consistent with this, suppressed RAD51 focus formation in DU145 cells when applied at the GI50 (1μM).  Co-treatment of 100 nM AZ12253801 and 1 μM RO-3306 manifested a marked increase in pre-G1
DNA, indicating apoptosis induction. In viability assays, RO-3306 induced a significant shift to the left of the AZ12253801 dose-response curve, with 2.4-fold reduction in GI50, comparable to RAD51 depletion or inhibition. At sub-50nM AZ12253801 concentrations there was more striking sensitization, with 13-fold reduction in GI80. Paralleling effects of RAD51 knockdown, RO-3306 did not affect AZ12253801 sensitivity of PC3 or LNCaP cells, but did sensitize 22Rv1 cells.
参考文献:
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