NU2058 is a competitive inhibitor of CDK2 with respect to ATP (Ki value CDK2, 12 3 μM) 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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||≥ 32 mg/mL in DMSO|
The kinase inhibitor O6-cyclohexylmethylguanine (NU2058) potentiates the cytotoxicity of cisplatin by mechanisms that are independent of its effect upon CDK2.
Harrison LR, et al. Biochem Pharmacol. 2009 May 15;77(10):1586-92. PMID: 19426695.
Therapeutic potential of CDK inhibitor NU2058 in androgen-independent prostate cancer.
Rigas AC, et al. Oncogene. 2007 Dec 6;26(55):7611-9. PMID: 17599054.
|Related CDK Products|
THZ2 (an analog of THZ1) is a potent and selective CDK7 inhibitor which overcomes the instability of THZ1 in vivo (IC50s: CDK7=13.9 nM; TNBC cells=10 nM).
LY-3177833 is a potent and selective inhibitor of CDC7 with IC50 of 3.3 nM.
Voruciclib (P1446A-05) is a protein kinase inhibitor specific for the cyclin-dependent kinase 4 (CDK4) with IC50s of 90nM, 25nM, and 22nM for CDK4-CyclinD1, CDK1-Cyclin B, and CDK9-Cyclin T, respectively.
CVT-313 is a potent and selective inhibitor of CDK2 that prevents neointimal proliferation, which has an IC50 of 0.5 microM in vitro.
ON123300 is a potent inhibitor of CDK4, with an IC50 of 3.8 nM, with little inhibitory activity against CDKs 1,2,5 and 8.
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