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ProRS Inhibitor, Halofuginone-CAS 64924-67-0-Calbiochem

品牌
Sigma-Aldrich
CAS
64924-67-0
货号
5.05763
规格纯度
A cell-permeable racemic mixture of Halofuginone that inhibits of prolyl-tRNA synthetase.
参考价格
2579.1 *本价格含增值税费
促销
数量
-+
产品介绍:

产品说明

一般描述

A cell-permeable racemic mixture of Halofuginone, a halogenated derivative of the Dichroa febriguga alkaloid Febrifugine, whose D-(+)/(2R, 3S) enantiomer serves as the active inhibitor against ProRS- (prolyl-tRNA synthetase) mediated aminoacylation by simultaneously targeting/blocking ProRS Proline-binding pocket with its hydroxypiperidine and tRNA 3′ end adenosine-binding site with its halogenated 4-quinazolinone, preventing not only ProRS-catalyzed prolyl adenylation (Pro-AMP formation), but also the subsequent Pro transfer from Pro-AMP to tRNAPro. Consistently, only proline, but not other NEAA, is able to reverse the inhibitory effect of HF in in vitro rabbit reticulocyte lysate translations (1 µM HF; 1 mM Pro) and prevent HF-induced cellular AAR (amino acid response) pathway activation (100 nM HF/2 mM Pro/MEF; 10 nM HF/1 mM Pro/Murine CD4+ CD25- T cells). Shown to inhibit bFGF-induced neovascularization in a murine corneal angiogenesis model (5 mg/kg/day via food intake) and significantly reduce the severity of myelin antigen MOG33-55-induced autoimmune EAE/encephalomyelitis in mice (2 µg/mouse/day i.p.) in vivo. Unlike AA-AMP mimetics, HF does not compete against ATP for ProRS binding. ATP, in its ProRS bound state, actually helps stabilize HF via hydrogen bond interactions.
A cell-permeable racemic mixture of Halofuginone whose D-(+)/(2R, 3S) enantiomer serves as the active inhibitor against ProRS-mediated aminoacylation by simultaneously preventing ProRS-catalyzed Pro-AMP formation and the subsequent Pro transfer from Pro-AMP to tRNAPro. Proline, but not other NEAA, is able to reverse the inhibitory effect of HF in in vitro rabbit reticulocyte lysate translations (1 µM HF; 1 mM Pro) and prevent HF-induced cellular AAR pathway activation (100 nM HF/2 mM Pro/MEF; 10 nM HF/1 mM Pro/Murine CD4+ CD25- T cells). Shown to inhibit bFGF-induced neovascularization in a murine corneal angiogenesis model (5 mg/kg/d via food intake) and significantly reduce the severity of MOG33-55-induced EAE in mice (2 µg/mouse/d i.p.) in vivo. Unlike AA-AMP mimetics, HF does not compete against ATP for ProRS binding.

生化/生理作用

Primary Target
prolyl-tRNA synthetase

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.

其他说明

Zhou, H., et al. 2013, Nature494, 121.

Keller, T.L., et al. 2012, Nat. Chem. Biol.12, 311.

Sundrud, M.S., et al. 2009, Science324, 1334.
Elkin, M., et al. 2000, FASEB J.14, 2477.
Elkin, M., et al. 1999, Clin. Cancer Res.5, 1982.

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C16H17BrClN3O3 · xHBr
分子量414.68 (free base basis)
MDL编号MFCD23843776

产品性质

质量水平100
测定≥98% (HPLC)
形式powder
效能18 nM IC50
manufacturer/tradenameCalbiochem®
储存条件OK to freeze
protect from light
颜色 white
溶解性DMSO: 100 mg/mL
储存温度2-8℃
InChI1S/C16H17BrClN3O3.BrH/c17-11-6-13-10(5-12(11)18)16(24)21(8-20-13)7-9(22)4-14-15(23)2-1-3-19-14;/h5-6,8,14-15,19,23H,1-4,7H2;1H/t14?,15-;/m1./s1
InChI keySJUWEPZBTXEUMU-NUNOUFIPSA-N

安全信息

象形图GHS06GHS09
警示用语:Danger
危险声明H300 + H310 + H330 - H315 - H319 - H410
预防措施声明P262 - P273 - P280 - P302 + P352 + P310 - P304 + P340 + P310 - P305 + P351 + P338
危险分类Acute Tox. 1 Dermal - Acute Tox. 2 Inhalation - Acute Tox. 2 Oral - Aquatic Acute 1 - Aquatic Chronic 1 - Eye Irrit. 2 - Skin Irrit. 2
储存分类代码6.1A - Combustible, acute toxic Cat. 1 and 2 / very toxic hazardous materials
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable

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