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NSC 95397

(Synonyms: Cdc25 Inhibitor IV, PTP Inhibitor XXIX) 目录号 : GC11561

An irreversible inhibitor of Cdc25 isoforms

NSC 95397 Chemical Structure

Cas No.:93718-83-3

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产品描述

NSC 95397 is a potent, selective Cdc25 dual specificity phosphatase inhibitor (Ki=32 nM (Cdc25A), 96 nM (Cdc25B), 40 nM (Cdc25C); IC50=22.3 nM (human Cdc25A), 56.9 nM (human Cdc25C), 125 nM (Cdc25B))[1]. NSC 95397 inhibits mitogen-activated protein kinase phosphatase-1 (MKP-1) and suppresses proliferation and induces apoptosis in colon cancer cells through MKP-1 and ERK1/2 pathway[2].

NSC 95397 (0, 10, and 20 µM; 24 hour) decreases the cell viability of three colon cancer cell lines SW480, SW620, and DLD-1 in a concentration-dependent manner[2].NSC 95397(10 μM; 24 hour) upregulates p21 while downregulates CDK4 and CDK6 were d in all three colon cancer cell lines SW480, SW620, and DLD-1 cells[2]. NSC 95397 (10 μM; 24 hour) reduces the phosphorylation of retinoblastoma protein (Rb) on Ser795 and Ser807/811[2]. NSC 95397 (20 μM; 24 hours) significantly increases cleaved caspase-9, -3, -7 and PARP levels[2]. NSC 95397 (10 μM; 6 hours) enhances the phosphorylation of its downstream ERK1/2 at Thr202/Tyr 204[2].

References:
[1]. Lazo JS, et al. Identification of a potent and selective pharmacophore for Cdc25 dual specificity phosphatase inhibitors. Mol Pharmacol. 2002 Apr;61(4):720-8.
[2]. Dubey NK, et al. NSC 95397 Suppresses Proliferation and Induces Apoptosis in Colon Cancer Cells through MKP-1 and the ERK1/2 Pathway. Int J Mol Sci. 2018 May 31;19(6). pii: E1625.

Chemical Properties

Cas No. 93718-83-3 SDF
别名 Cdc25 Inhibitor IV, PTP Inhibitor XXIX
化学名 2,3-bis((2-hydroxyethyl)thio)naphthalene-1,4-dione
Canonical SMILES O=C1C2=CC=CC=C2C(C(SCCO)=C1SCCO)=O
分子式 C14H14O4S2 分子量 310.38
溶解度 DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2)(1:5): 0.16 mg/ml,Ethanol: 0.33 mg/ml 储存条件 Desiccate at -20°C
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1 mM 3.2219 mL 16.1093 mL 32.2186 mL
5 mM 0.6444 mL 3.2219 mL 6.4437 mL
10 mM 0.3222 mL 1.6109 mL 3.2219 mL
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