Alsterpaullone

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Cat.No. 6400 - Alsterpaullone | C16H11N3O3 | CAS No. 237430-03-4
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
Reviews
Literature

Biological Activity

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

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 14.66 50

Preparing Stock Solutions

The following data is based on the product molecular weight 293.28. Batch specific molecular weights may vary from batch to batch due to solvent 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

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References

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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Literature in this Area

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Cancer

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Cell Cycle & DNA Damage Repair

Cell Cycle & DNA Damage Repair Poster

In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.