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505763 Sigma-AldrichProRS Inhibitor, Halofuginone - CAS 64924-67-0 - Calbiochem

A cell-permeable racemic mixture of Halofuginone that inhibits of prolyl-tRNA synthetase.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

MSDS
参考
Data Sheet

同义词: prolyl-tRNA synthetase Inhibitor, STENOROL, HF, Hydrobromide, trans-(±)-7-Bromo-6-chloro-3-[3-(3-hydroxy-2-piperidinyl)-2-oxopropyl]-4(3H)-quinazolinone hydrobromide

Primary Target: prolyl-tRNA synthetase

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概述

Replacement Information

重要规格表

CAS #	Empirical Formula
64924-67-0	C₁₆H₁₇BrClN₃O₃•HBr

价格及供货情况

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Description
Overview	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 tRNA^Pro. 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.
Catalogue Number	505763
Brand Family	Calbiochem®
Synonyms	prolyl-tRNA synthetase Inhibitor, STENOROL, HF, Hydrobromide, trans-(±)-7-Bromo-6-chloro-3-[3-(3-hydroxy-2-piperidinyl)-2-oxopropyl]-4(3H)-quinazolinone hydrobromide

References
References	Zhou, H., et al. 2013, Nature 494, 121. Keller, T.L., et al. 2012, Nat. Chem. Biol. 12, 311. Sundrud, M.S., et al. 2009, Science 324, 1334. Elkin, M., et al. 2000, FASEB J. 14, 2477. Elkin, M., et al. 1999, Clin. Cancer Res. 5, 1982.

Product Information
CAS number	64924-67-0
Form	White powder
Hill Formula	C₁₆H₁₇BrClN₃O₃•HBr
Chemical formula	C₁₆H₁₇BrClN₃O₃•HBr
Structure formula Image
Quality Level	MQ100

Applications

Biological Information
Primary Target	prolyl-tRNA synthetase
Primary Target IC<sub>50</sub>	18 nM
Purity	≥98% by HPLC

Physicochemical Information

Dimensions

Materials Information

Toxicological Information

Safety Information according to GHS

Safety Information

Product Usage Statements

Storage and Shipping Information
Ship Code	Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity	Standard Handling
Storage	+2°C to +8°C
Protect from Light	Protect from light
Do not freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Packaging Information
Packaged under inert gas	Packaged under inert gas

Transport Information

Supplemental Information

Specifications

Global Trade Item Number
产品目录编号	GTIN
5.05763.0001	04055977243536

Documentation

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

职位
物料安全数据表 (MSDS)

参考

参考信息概述
Zhou, H., et al. 2013, Nature 494, 121. Keller, T.L., et al. 2012, Nat. Chem. Biol. 12, 311. Sundrud, M.S., et al. 2009, Science 324, 1334. Elkin, M., et al. 2000, FASEB J. 14, 2477. Elkin, M., et al. 1999, Clin. Cancer Res. 5, 1982.

数据表

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision	28-March-2014 JSW
Synonyms	prolyl-tRNA synthetase Inhibitor, STENOROL, HF, Hydrobromide, trans-(±)-7-Bromo-6-chloro-3-[3-(3-hydroxy-2-piperidinyl)-2-oxopropyl]-4(3H)-quinazolinone hydrobromide
Description	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 tRNA^Pro. 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.
Form	White powder
Intert gas (Yes/No)	Packaged under inert gas
CAS number	64924-67-0
Chemical formula	C₁₆H₁₇BrClN₃O₃•HBr
Structure formula
Purity	≥98% by HPLC
Solubility	DMSO (100 mg/ml)
Storage	Protect from light +2°C to +8°C
Do Not Freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity	Standard Handling
References	Zhou, H., et al. 2013, Nature 494, 121. Keller, T.L., et al. 2012, Nat. Chem. Biol. 12, 311. Sundrud, M.S., et al. 2009, Science 324, 1334. Elkin, M., et al. 2000, FASEB J. 14, 2477. Elkin, M., et al. 1999, Clin. Cancer Res. 5, 1982.

种类

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Other Inhibitors of Biological Interest > Protein Synthesis Inhibitors

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