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CD45 Inhibitor VI-Calbiochem

品牌
Sigma-Aldrich
货号
5.30197
规格纯度
A cell-permeable, potent, irreversible, non-substrate competitive inhibitor of CD45/PTPRC tyrosine phosphatase activity (IC50= 290 nM).
价格
2289.97 *本价格含增值税费
促销
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数量
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半岛bd体育手机客户端 名称:
CD45 Inhibitor VI-Calbiochem
2-(4-Acetylanilino)-3-chloronaphthoquinone, Compound 211, Protein Tyrosine Phosphatase CD45 Inhibitor VI, PTP Inhibitor XXXII
半岛bd体育手机客户端 介绍:

半岛bd体育手机客户端 说明

一般描述

A cell-permeable chloronaphthoquinone compound that potently inhibits CD45/PTPRC tyrosine phosphatase activity (IC50= 290 nM) in a non-substrate-competitive and irreversible manner via targeting an allosteric pocket at the D1-D2 domains interface. Exhibits good selectivity over MKPX, PRL-2, PTP1B/PTPN1, TC-PTP/PTPN2, SHP-1/PTPN6, PEP/PTPN22, LAR/PTPRF, and PTP-Sigma/PTPRS (IC50>40 ?M). Shown to reduce T cell receptor-mediated activation of Lck, Zap-70, MAPK, and IL-2 production in primary T cells and effectively block human Lck pY-394 dephosphorylation in Jurkat, but not CD45-deficient J45.01 line, reducing cellular metabolic activity without affecting viability. Displays immunosuppressive properties against footpad swelling in a murine modle of delayed type hypersensitivity among C57/BL6 mice even when administered (3 mg/kg, i.p) after early onset of inflammation. However, it does not clear existing edema when applied to mice with fully developed inflammation.
A cell-permeable chloronaphthoquinone that potently inhibits CD45/PTPRC tyrosine phosphatase activity (IC50= 290 nM; substrate = 1 mM pp60-src pY-527 peptide) in a non-substrate-competitive, irreversible, and selective manner via targeting an allosteric pocket at the D1-D2 domains interface away from the substrate-binding/catalytic site, exhibiting little potency toward murine PEST or eight human phosphatases (IC50>40 ?M against pNPP hydrolysis by MKPX, PRL-2, PTP1B/PTPN1, TC-PTP/PTPN2, SHP-1/PTPN6, PEP/PTPN22, LAR/PTPRF, and PTP-Sigma/PTPRS). Shown to increase human Lck pY394 phosphorylation level in Jurkat cells (by 40% in 24 h; 0.5 ?M), but not CD45-deficient J45.01 line. Likewise, drug treatment effectively suppresses induction of Lck pY394, Zap-70 pY319, pErk1/2 phosphorylations and IL-2 release in primary murine splenocyte cultures upon T-cell activation (0.5 ?M for 48 h) via TCR cross-linking with concomitant reduced metabolic activity (by MTT assay), but not cell death (by Trypan Blue exclusion). Single intraperitoneal injection (3 mg/kg) administered either 1 h or 3 d post Ovalbumin-/OVA-challenge (1 ?g /footpad) among OVA-sensitized mice effectively prevents footpad swelling 6 d post challenge (<0.05 mm vs. >0.3 mm, respectively, with or without treatment) in delayed type hypersensitivity (DTH) testsin vivo. Exhibits no detectable cytotoxicity in KB or HEK293 cultures (0.5 ?M for 24 h), while a 50% lymphocytes reduction is reported in mice 24 h post 3 mg/kg i.p. dosage with no other apparent adverse effects.

生化/生理作用

Cell permeable: yes
Reversible: no
Primary Target
CD45

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Use only fresh DMSO for reconstitution.

其他说明

Perron, M., et al. 2014.Mol. Pharmacol.85,553.

法律信息

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

基本信息

经验(实验)分子式 C18H12ClNO3
分子量 325.75

半岛bd体育手机客户端 性质

质量水平 100
测定 ≥98% (HPLC)
形式 powder
manufacturer/tradename Calbiochem?
储存条件 OK to freeze
protect from light
颜色 orange
溶解性 DMSO: 25 mg/mL
储存温度 2-8℃

安全信息

象形图 GHS07GHS09
警示用语: Warning
危险声明 H315 - H319 - H335 - H400
预防措施声明 P261 - P264 - P271 - P273 - P302 + P352 - P305 + P351 + P338
危险分类 Aquatic Acute 1 - Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
靶器官 Respiratory system
储存分类代码 11 - Combustible Solids
WGK WGK 3
闪点(F) Not applicable
闪点(C) Not applicable

Sigma-Aldrich

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