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Biological Activity for Alsterpaullone
Alsterpaullone is a potent CDK1 and 2 inhibitor (IC50 values are 0.035 and 0.08 μM, respectively). Also inhibits GSK-3β and Lck (IC50 values are 0.11 and 0.47 μM, respectively). Induces apoptosis by activation of caspase-9; inhibits growth of cancer cell lines in vitro. Also glucocorticoid receptor inhibitor.
Technical Data for Alsterpaullone
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Alsterpaullone
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for Alsterpaullone
The following data is based on the product molecular weight 293.28. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.5 mM||6.82 mL||34.1 mL||68.19 mL|
|2.5 mM||1.36 mL||6.82 mL||13.64 mL|
|5 mM||0.68 mL||3.41 mL||6.82 mL|
|25 mM||0.14 mL||0.68 mL||1.36 mL|
References for Alsterpaullone
References are publications that support the biological activity of the product.
Schulz et al (1999) Paullones, a series of cyclin-dependent kinase inhibitors: synthesis, evaluation of CDK1/cyclin B inhibition, and in vitro antitumor activity. J.Med.Chem. 42 2909 PMID: 10425100
Bain et al (2003) The specificities of protein kinase inhibitors: an update. Biochem.J. 371 199 PMID: 12534346
Lahusen et al (2003) Alsterpaullone, a novel cyclin-dependent kinase inhibitor, induces apoptosis by activation of caspase-9 due to perturbation in mitochondrial membrane potential. Mol.Carcinog. 36 183 PMID: 12669310
Jiang et al (2017) A high-throughput chemical screen identifies novel inhibitors and enhancers of anti-inflammatory functions of the glucocorticoid receptor. Sci.Rep. 7 6405 PMID: 28785063
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Citations for Alsterpaullone
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