NSC 663284

Three genes encode dual specificity phosphatases that are Cdc25 homologs. The phosphatases, Cdc25A through C, are proto-oncogenes and are often over-expressed in cancers. NSC 663284 is a potent, cell-permeable, and irreversible inhibitor of all Cdc25 isoforms, with preference for Cdc25A (IC50 = 29, 95, and 89 nM for Cdc25A, Cdc25B2, and Cdc25C, respectively). NSC 663284 poorly inhibits other phosphatases, including Vaccinia virus VH1-related (IC50 = 4.0 µM), PTP1B (no inhibition), and the mitogen-activated protein kinase phosphatases (MKP) MKP-1 or -3 (no inhibition). By inhibiting Cdc25 isoforms, NSC 663284 prevents the dephosphorylation and activation of Cdk1 and Cdk2, arrests cells at both G1 and G2/M phases, and prevents the proliferation of several human tumor cell lines.Formal Name: 6-chloro-7-[[2-(4-morpholinyl)ethyl]amino]-5,8-quinolinedione. CAS Number: 383907-43-5. Synonyms: Cdc25 Phosphatase Inhibitor II, DA-3003-1, SPS8I1. Molecular Formula: C15H16ClN3O3. Formula Weight: 321.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 10 mg/ml, Ethanol: 0.5 mg/ml, PBS (pH 7.2): 0.15 mg/ml. lambdamax: 236, 274, 477 nm. SMILES: ClC1=C(NCCN2CCOCC2)C(=O)c2ncccc2C1=O. InChi Code: InChI=1S/C15H16ClN3O3/c16-11-13(18-4-5-19-6-8-22-9-7-19)15(21)12-10(14(11)20)2-1-3-17-12/h1-3,18H,4-9H2. InChi Key: BMKPVDQDJQWBPD-UHFFFAOYSA-N.