Kenpaullone represents a novel chemotype for compounds that preferentially inhibit CDKs. Kenpaullone inhibits CDK2/cyclin A, CDK2/cyclin E and CDK5/cyclin/p35 (IC50 values are 0.68, 7.5 and 0.85 μM respectively). Kenpaullone is selective over c-src (IC50 = 15 μM), casein kinase 2 (IC50 = 20 μM), ERK1 (IC50 = 20 μM), ERK2 (IC50 = 9 μM) and a range of other protein kinases (IC50 values > 35 μM). Kenpaullone generates induced pluripotent stem cells (iPSCs) from somatic cells when used in combination with reprogramming factors. Kenpaullone can take the place of Klf4.
|Cell lines||HEK-293 cells|
|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||DMSO 18 mg/mL|
Reprogramming of murine fibroblasts to induced pluripotent stem cells with chemical complementation of Klf4.v
Lyssiotis CA, et al. Proc Natl Acad Sci U S A. 2009 Jun 2;106(22):8912-7. PMID: 19447925.
Cell cycle molecular targets in novel anticancer drug discovery.
Buolamwini JK. Curr Pharm Des. 2000 Mar;6(4):379-92. PMID: 10788588.
Paullones, a series of cyclin-dependent kinase inhibitors: synthesis, evaluation of CDK1/cyclin B inhibition, and in vitro antitumor activity.
Schultz C, et al. J Med Chem. 1999 Jul 29;42(15):2909-19. PMID: 10425100.
Discovery and initial characterization of the paullones, a novel class of small-molecule inhibitors of cyclin-dependent kinases.
Zaharevitz DW, et al. Cancer Res. 1999 Jun 1;59(11):2566-9. PMID: 10363974.
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NU2058 is a guanine-based CDK inhibitor with IC50 of 17 μM and 26 μM for CDK2 and CDK1.
LDC000067 is a highly selective CDK9 inhibitor with IC50 of 44 nM, 55/125/210/ >227/ >227-fold selectivity over CDK2/1/4/6/7.
RO-3306 is an ATP-competitive, and selective CDK1 inhibitor with Ki of 20 nM, >15-fold selectivity against a diverse panel of human kinases.
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