Description
NSC 95397 (93718-83-3) is a potent and selective inhibitor of Cdc25 phosphatase (Ki? = 32, 96 and 40 nM for Cdc25A, B and C respectively). NSC-95397 inhibits the growth of several human tumor cell lines and blocks G2/M cell cycle transition.1 Induces cell cycle arrest, phosphorylation of EGFR and activation of ERK-1 and -2.2 Inhibits carboxyl-terminal binding protein a transcriptional corepressor that suppresses multiple pro-apoptotic and epithelial genes.3 Induces eryptosis in human erythrocytes.4
Uses
NSC 95397 is a quinone-based Cdc25 inhibitor, caspase-3 activator, ERK activator, and MKP inhibitor.
Definition
ChEBI: 2,3-bis(2-hydroxyethylthio)naphthalene-1,4-dione is a member of 1,4-naphthoquinones.
Biological Activity
Potent and selective irreversible inhibitor of Cdc25 dual specificity phosphatases (K i values are 32, 96 and 40 nM for inhibition of Cdc25A, -B and -C respectively). Displays 125-180-fold selectivity over VH1-related dual-specificity phosphatase and protein tyrosine phosphatase 1b. Inhibits carcinoma cell growth and blocks G 2 /M phase transition in vitro .
Biochem/physiol Actions
Irreversible Cdc25 dual specificity phosphatase inhibitor.
storage
Desiccate at -20°C
References
1) Lazo et al. (2002), Identification of a potent and selective pharmacophore for Cdc25 dual specificity phosphatase inhibitors; Mol. Pharmacol., 61 720
2) Melchheier et al. (2005), Quinone-induced Cdc25A inhibition causes ERK-dependent connexin phosphorylation; Biochem. Biophys. Res. Commun., 327 1016
3) Blevins et al. (2015), Small Molecule, NSC95397, inhibits the CtBP1-Protein Partner Interaction and CtBP1-Mediated Transcriptional Repression; J. Biomol. Screen., 20 663
4) Jemaa et al. (2016), Stimulation of Suicidal Erythrocyte Death by the CDC25 Inhibitor NSC-95397; Cell. Physiol. Biochem., 40 597
