Background
NSC-95397 is a quinone-containing inhibitor of the cdc25 dual-specificity phosphatases responsible for regulating eukaryotic cell entry into mitosis. The primary substrate of cdc25A is CDK2, which allows progression through the G1/S and intra-S checkpoints; cdc25C activates CDK1 to overcome the G2/M checkpoint and allow mitotic entry (1). cdc25 phosphatase inhibition by NSC-95397 varies, with dissociation constants for cdc25A, -B, and -C of Ki = 32 nM, 96 nM, and 40 nM, respectively (2). NSC-95397 treatment of cancer cell lines leads to cell growth inhibition and cell cycle arrest at G2/M (1). Similar growth inhibition was seen in human hepatoma and breast cancer cells (3). Exposure of human erythrocytes to NSC-95397 triggers cell shrinkage, cell membrane scrambling, and eryptosis (4). The dual-specificity phosphatases MAP Kinase phosphatase 1 (MKP1) and MKP3 are likewise inhibited by NSC-95397, with NSC-95397 treatment followed by inhibited proliferation and reduced cell viability in a number of colon cancer cell lines (5,6).
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Molecular Formula
C14H14O4S2
Molecular Weight
310.4 g/mol
Purity
>98%
CAS
93718-83-3
Solubility
Soluble in DMSO at 15 mg/mL or ethanol at 1 mg/mL.
Storage
Directions for Use
Background References
Cross-Reactivity Key
H: human M: mouse R: rat Hm: hamster Mk: monkey Vir: virus Mi: mink C: chicken Dm: D. melanogaster X: Xenopus Z: zebrafish B: bovine Dg: dog Pg: pig Sc: S. cerevisiae Ce: C. elegans Hr: horse GP: Guinea Pig Rab: rabbit All: all species expected
Trademarks and Patents
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