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.
|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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