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Alsterpaullone

Cat. No. 6400 Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
Description: Potent CDK1 and CDK2 inhibitor; also inhibits GSK-3β and Lck
Chemical Name: 7,12-Dihydro-9-nitroindolo[3,2-d][1]benzazepin-6(5H)-one
Purity: ≥98% (HPLC)
Datasheet
Citations
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Biological Activity Technical Data Solubility Calculators Datasheets References

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

M. Wt 293.28
Formula C16H11N3O3
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 237430-03-4
PubChem ID 5005498
InChI Key OLUKILHGKRVDCT-UHFFFAOYSA-N
Smiles O=C1CC2=C(C3=CC=CC=C3N1)NC4=C2C=C([N+]([O-])=O)C=C4

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
Solubility
DMSO 14.66 50

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.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets for Alsterpaullone

Certificate of Analysis / Product Datasheet
Safety Datasheet

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

If you know of a relevant reference for Alsterpaullone, please let us know.

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Citations for Alsterpaullone

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