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Alsterpaullone

ALX-270-275

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Inhibitor of CDK and GSK

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.

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Product Details

Appearance	Yellow to brown powder.
CAS	237430-03-4
Couple Target	Caspase, Caspase-8, Caspase-9, CDK, GSK
Couple Type	Activator, Inhibitor
Formula	C₁₆H₁₁N₃O₃
Identity	Determined by IR, 1H-NMR and 13C-NMR.
MW	293.3
Purity	≥95%
Solubility	Soluble in DMSO; insoluble in water or 100% ethanol.

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended.
Handling	Protect from light.
Long Term Storage	+4°C
Shipping	Ambient Temperature

Regulatory Status	RUO – Research Use Only

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
Intracellular Targets of Paullones. Identification following affinity purification on immobilized inhibitor: M. Knockaert, et al.; J. Biol. Chem. 277, 25493 (2002), Abstract — Full Text
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
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
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
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
ATP-site directed inhibitors of cyclin-dependent kinases: N. Gray, et al.; Curr. Med. Chem. 6, 859 (1999), Abstract

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Alsterpaullone

ALX-270-275

Product Details

Handling & Storage

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