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|
|SCH 900776 (CAS:891494-64-7)
MK-8776 (SCH 900776) is a selective Chk1 inhibitor with IC50 of 3 nM in a cell-free assay. It shows 500-fold selectivity against Chk2.
MSC2530818, a CDK8 inhibitor with the IC50 of 2.6 nM, displays excellent kinase selectivity, biochemical and cellular potency, microsomal stability, and is orally bioavailable.
Palbociclib is a highly specific inhibitor of Cdk4 (IC50=11 nM) and Cdk6 (IC50=16 nM), having no activity against a panel of 36 additional protein kinases.
M2I-1 a small Mad2 inhibitor-1. the first small molecule inhibitor targeting the binding of Mad2 to Cdc20, an essential proteinprotein interaction (PPI) within the SAC.
NU2058 is a guanine-based CDK inhibitor with IC50 of 17 μM and 26 μM for CDK2 and CDK1.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.