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CDC25 Phosphatase Inhibitor II, NSC 663284 - CAS 383907-43-5 - Calbiochem

The CDC25 Phosphatase Inhibitor II, NSC 663284, also referenced under CAS 383907-43-5, controls the biological activity of CDC25 Phosphatase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Synonym: 6-Chloro-7-(2-morpholin-4-yl-ethylamino)quinoline-5,8-dione, DA3003-1, PTP Inhibitor XXI, VHR Inhibitor II, CDC25 Phosphatase Inhibitor II, NSC 663284 - CAS 383907-43-5 - Calbiochem

  • CAS Number 383907-43-5

  • Empirical Formula (Hill Notation) C15H16ClN3O3

  • Molecular Weight 321.76

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Properties

assay   ≥98% (HPLC)
form   solid
mfr. no.   Calbiochem®
storage condition   OK to freeze
  protect from light
storage conditions   +2C to +8C
color   red
solubility   DMSO: 5 mg/mL (Use only fresh, anhydrous DMSO.)
  ethanol: 5 mg/mL
shipped in   ambient

Description

General description

A cell-permable, potent, irreversible, and competitive inhibitor of the Cdc25 phosphatase family (Ki = 29 nM, 95 nM, and 89 nM for Cdc25A, Cdc25B2, and Cdc25C, respectively) with anti-proliferative properties. Displays nearly 20- and 450-fold greater selectivity over VHR and PTP1B (IC50 = 4.0 µM and > 100 µM, respectively). Reported to arrest cell cycle progression, inhibit Cdk dephosphorylation, and delay tumor growth (mean IC50 = 1.5 µM in NCI-60 tumor cell panel). Also shown to block ERK dephosphorylation caused by ectopic Cdc25A expression.

A cell-permeable 7-substituted quinolinedione compound that displays antiproliferative properties. Acts as a potent, irreversible and mixed competitive inhibitor of the CDC25 phosphatase family (Ki = 29 nM, 95 nM and 89 nM for CDC25A, CDC25B2 and CDC25C, respectively; IC50 = 210 nM for CDC25B2) and displays nearly 20- and 450-fold greater selectivity for the CDC252 phosphatases over VHR and PTP1B (IC50 = 4.0 µM and > 100 µM, respectively). Reported to arrest cell cycle progression, inhibit Cdk dephosphorylation and delay tumor growth (IC50 = ~1.5 µM in NCI-60 tumor cell panel). Shown to modify CDC25A catalytic domain and to block cellular ERK dephosphorylation in HeLa-CDC25A cells.

Packaging

5 mg in Plastic ampoule

Biochem/physiol Actions

Cell permeable: yes

Primary Target
CD25A

Product does not compete with ATP.

Reversible: no

Target Ki: 29 nM, 95 nM and 89 nM for CDC25A, CDC25B2 and CDC25C, respectively; 210 nM for CDC25B2

Packaging

Packaged under inert gas

Warning

Toxicity: Carcinogenic / Teratogenic (D)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 1 month at -20°C. Ethanol stock solutions are stable for up to 6 months at -20°C.

Other Notes

Chao, J. I., et al. 2004. J. Biol. Chem.279, 20267.
Han, Y., et al. 2004. J. Pharmacol. Exp. Ther.309, 64.
Pu, L., et al. 2002. J. Biol. Chem.277, 46877.
Lazo, J.S., et al. 2001. J. Med. Chem.44, 4042.

Safety & Documentation

Safety Information

Safety Information for this product is unavailable at this time.

Documents

Certificate of Analysis (COA)

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