Alsterpaullone

Inhibitor of CDK and GSK



ALX-270-275-M001	1 mg	57.00 USD

ALX-270-275-M005	5 mg	279.00 USD

Potent inhibitor of CDK1/cyclin B (IC₅₀=35nM). Potent and selective inhibitor of CDK2/cyclin A, CDK2/cyclin E (IC₅₀=200nM), CDK5/p25 (IC₅₀=40nM), CDK5/p35 (IC₅₀=40nM) and GSK-3β . Induces apoptosis by activation of caspase-8 and caspase-9 followed by disruption of the mitochondrial potential.Licensed from NCI.

Product Specification

Alternative Name:	9-Nitro-7,12-dihydroindolo-[3,2-d][1]benzazepin-6(5H)-one

Identity:	Identity determined by IR, ¹H-NMR and ¹³C-NMR.

Formula:	C₁₆H₁₁N₃O₃

MW:	293.3

Purity:	≥95%

Appearance:	Yellow to brown powder.

CAS:	237430-03-4

Solubility:	Soluble in DMSO; insoluble in water or 100% ethanol.

Long Term Storage:	+4°C

Handling:	Protect from light.

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Product Literature References

Alsterpaullone, a novel cyclin-dependent kinase inhibitor, induces apoptosis by activation of caspase-9 due to perturbation in mitochondrial membrane potential: T. Lahusen, et al.; Mol Carcinog 36, 183 (2003), Abstract;

The specificities of protein kinase inhibitors: an update: J. Bain, et al.; Biochem. J. 371, 199 (2003), Abstract;

A novel, extraneuronal role for cyclin-dependent protein kinase 5 (CDK5): modulation of cAMP-induced apoptosis in rat leukemia cells: T. Sandal, et al.; J. Biol. Chem. 277, 20783 (2002), Abstract; Full Text

Intracellular Targets of Paullones. Identification following affinity purification on immobilized inhibitor: M. Knockaert, et al.; J. Biol. Chem. 277, 25493 (2002), Abstract; Full Text

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;

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;

ATP-site directed inhibitors of cyclin-dependent kinases: N. Gray, et al.; Curr. Med. Chem. 6, 859 (1999), 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;

Fused azepinones with antitumor activity: C. Kunick; Curr. Pharm. Des. 5, 181 (1999), (Review), 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;