217692

CDC25 Phosphatase Inhibitor II, NSC 663284

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.

• 別名: CDC25 Phosphatase Inhibitor II, NSC 663284, 6-Chloro-7-(2-morpholin-4-yl-ethylamino)quinoline-5,8-dione, DA3003-1, PTP Inhibitor XXI, VHR Inhibitor II
• 実験式（ヒル表記法）: C₁₅H₁₆ClN₃O₃
• CAS番号: 383907-43-5
• 分子量: 321.76
• MDL番号: MFCD08276924
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥98% (HPLC)
• フォーム: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: red
• 溶解性: DMSO: 5 mg/mL (Use only fresh, anhydrous DMSO.); ethanol: 5 mg/mL
• 輸送温度: ambient
• 保管温度: 2-8°C
• SMILES記法: ClC1=C(C(=O)c3ncccc3C1=O)NCCN2CCOCC2
• 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

詳細

詳細

A cell-permable, potent, irreversible, and competitive inhibitor of the Cdc25 phosphatase family (K_i = 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 (K_i = 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.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
CD25A

Product does not compete with ATP.

Reversible: no

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

包装

Packaged under inert gas

警告

Toxicity: Carcinogenic / Teratogenic (D)

再構成

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.

その他情報

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.

法的情報

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): 470.1 °F
• 引火点(℃): 243.4 °C