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.

• 同義詞: 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
• 經驗公式（希爾表示法）: C₁₅H₁₆ClN₃O₃
• CAS號碼: 383907-43-5
• 分子量：: 321.76
• MDL號碼: MFCD08276924
• 分類程式碼代碼: 12352200
• NACRES: NA.77

屬性

• 品質等級: 100
• 化驗: ≥98% (HPLC)
• 形狀: solid
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: red
• 溶解度: DMSO: 5 mg/mL (Use only fresh, anhydrous DMSO.); ethanol: 5 mg/mL
• 運輸包裝: ambient
• 儲存溫度: 2-8°C
• SMILES 字串: 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 密鑰: BMKPVDQDJQWBPD-UHFFFAOYSA-N

描述

一般說明

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.

生化／生理作用

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

包裝

Packaged under inert gas

警告

Toxicity: Carcinogenic / Teratogenic (D)

重構

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.

其他說明

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.

法律資訊

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

安全資訊

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: 470.1 °F
• 閃點（°C）: 243.4 °C