NU2058 is a guanine-based CDK inhibitor with IC50 of 17 uM and 26 uM for CDK2 and CDK1.IC50 value: 17uM (CDK2), 26uM (CDK1)Target: CDKin vitro: NU2058 is a competitive inhibitor of CDK2 with respect to ATP (Ki value CDK2, 12 3 uM) that binds in the ATP binding pocket in a different orientation from other purine-based inhibitors, including olomoucine and roscovotine. NU2058 is the lead compound in a structure-based drug discovery program to develop more potent and selective CDK inhibitors.
References:
[1]. Rigas AC, et al. Therapeutic potential of CDK inhibitor NU2058 in androgen-independent prostate cancer. Oncogene. 2007 Dec 6;26(55):7611-7619.