Alsterpaullone

Alsterpaullone (9-Nitropaullone) is a potent CDK inhibitor, with IC50s of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also competes with ATP for binding to GSK-3alpha/GSK-3beta with IC50s of both 4 nM. Alsterpaullone has antitumor activity, and possesses potential for the study in neurodegenerative and proliferative disorders[1]. Alsterpaullone induces apoptosis in leukemia cell line[2].

Product Specifications

CAS Number

[237430-03-4]

Product Name Alternative

9-Nitropaullone; NSC 705701

UNSPSC

12352005

Hazard Statement

H315, H319, H335

Target

Apoptosis; CDK; GSK-3

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; PI3K/Akt/mTOR; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/alsterpaullone.html

Purity

99.85

Solubility

DMSO : 5 mg/mL (ultrasonic)

Smiles

O=C1NC2=CC=CC=C2C(NC3=C4C=C([N+]([O-])=O)C=C3)=C4C1

Molecular Formula

C16H11N3O3

Molecular Weight

293.28

Precautions

H315, H319, H335

References & Citations

[1]Leost M, et al. Paullones are potent inhibitors of glycogen synthase kinase-3beta and cyclin-dependent kinase 5/p25. Eur J Biochem. 2000 Oct;267 (19) :5983-94.|[2]Lahusen T, et al. Alsterpaullone, a novel cyclin-dependent kinase inhibitor, induces apoptosis by activation of caspase-9 due to perturbation in mitochondrial membrane potential. Mol Carcinog. 2003 Apr;36 (4) :183-94.|[3]Chunying Cui, et al. Alsterpaullone, a Cyclin-Dependent Kinase Inhibitor, Mediated Toxicity in HeLa Cells through Apoptosis-Inducing Effect. J Anal Methods Chem. 2013;2013:602091.|[4]Claudia C Faria, et al. Identification of alsterpaullone as a novel small molecule inhibitor to target group 3 medulloblastoma. Oncotarget. 2015 Aug 28;6 (25) :21718-29.