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.

• 동의어(들): 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
• 실험식(Hill 표기법): C₁₅H₁₆ClN₃O₃
• CAS Number: 383907-43-5
• Molecular Weight: 321.76
• MDL number: MFCD08276924
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• Quality Level: 100
• 분석: ≥98% (HPLC)
• 형태: solid
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: red
• solubility: DMSO: 5 mg/mL (Use only fresh, anhydrous DMSO.); ethanol: 5 mg/mL
• 배송 상태: ambient
• 저장 온도: 2-8°C
• 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

설명

일반 설명

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.

생화학적/생리학적 작용

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

포장

Packaged under inert gas

경고

Toxicity: Carcinogenic / Teratogenic (D)

재구성

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.

기타 정보

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.

법적 정보

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

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): 470.1 °F
• Flash Point (°C): 243.4 °C