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Kenpaullone

BML-EI310

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Inhibitor of CDK and GSK

Potent inhibitor of CDK1/cyclin B (IC50=400nM). Also inhibits CDK2/cyclin A (IC50=680nM) , CDK5 (IC50=850nM) and with much less effect other kinases. More recently, kenpaullone has been found to be a useful GSK-3β inhibitor (IC50=23nM). Induces pluripotency in somatic cells when used in combination with reprogramming factors. Increases neurogenesis of human neural progenitor cells through stimulation of Wnt/β-catenin signaling pathway.

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Product Details

Alternative Name	9-Bromo-7,12-dihydroindolo-[3,2-d][1]benzazepin-6(5H)-one
Appearance	Tan solid.
CAS	142273-20-9
Couple Target	CDK, GSK
Couple Type	Inhibitor
Formula	C₁₆H₁₁BrN₂O
Identity	Determined by 1H-NMR.
MW	327.2
Purity	≥98% (TLC)
Solubility	Soluble in DMSO (>25mg/ml); insoluble in water or ethanol.

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended. Stable for at least 1 year after receipt when stored, as supplied, at -20°C. Stock solutions are stable for up to 3 months at -20°C.
Long Term Storage	-20°C
Shipping	Ambient Temperature

Regulatory Status	RUO – Research Use Only

The specificities of protein kinase inhibitors: an update: J. Bain, et al.; Biochem. J. 371, 199 (2003), Abstract
Indirubins inhibit glycogen synthase kinase-3 beta and CDK5/p25, two protein kinases involved in abnormal tau phosphorylation in Alzheimer’s disease. A property common to most cyclin-dependent kinase inhibitors?: S. Leclerc, et al.; J. Biol. Chem. 276, 251 (2001), Abstract
Inhibition of CDKs as a therapeutic modality: E.A. Sausville, et al.; Ann. NY Acad. Sci. 910, 207 (2000), Abstract
Paullones are potent inhibitors of glycogen synthase kinase-3beta and cyclin-dependent kinase 5/p25: M. Leost, et al.; Eur. J. Biochem. 267, 5983 (2000), Abstract
2-Substituted paullones: CDK1/cyclin B-inhibiting property and in vitro antiproliferative activity: C. Kunick, et al.; Bioorg. Med. Chem. Lett. 10, 567 (2000), Abstract
Structure-based design modifications of the paullone molecular scaffold for cyclin-dependent kinase inhibition: R. Gussio; Anticancer Drug Des. 15, 53 (2000), Abstract
Paullones, a series of cyclin-dependent kinase inhibitors: synthesis, evaluation of CDK1/cyclin B inhibition, and in vitro antitumor activity: C. Schultz, et al.; J. Med. Chem. 42, 2909 (1999), Abstract
ATP-site directed inhibitors of cyclin-dependent kinases: N. Gray, et al.; Curr. Med. Chem. 6, 859 (1999), Abstract
Fused azepinones with antitumor activity: C. Kunick; Curr. Pharm. Des. 5, 181 (1999), (Review), Abstract
Discovery and initial characterization of the paullones, a novel class of small-molecule inhibitors of cyclin-dependent kinases: D.W. Zaharevitz, et al.; Cancer Res. 59, 2566 (1999), Abstract