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530588 Sigma-AldrichIκB Ubiquitination Inhibitor, GS143 - CAS 916232-21-8 - Calbiochem

A cell-permeable, selective inhibitor of E3 ligase complex SCFβTrCP1-mediated ubiquitination of phosphorylated IκBα (IC₅₀ = 5.2 µM).

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

MSDS
参考
Data Sheet

同义词: 4-(3-Benzyl-4-(5-(2-fluoro-phenyl)-furan-2-ylmethylene)-5-oxo-4,5-dihydropyrazol-1-yl)-benzoic acid, 4-(3-Benzyl-4-((5-(2-fluorophenyl)furan-2-yl)methylene)-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid, GS 143

Primary Target: phosphorylated IκBα

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概述

Replacement Information

重要规格表

CAS #	Empirical Formula
916232-21-8	C₂₈H₁₉FN₂O₄

价格及供货情况

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Description
Overview	A cell-permeable trisubstituted oxo-dihydropyrazolyl-benzoic acid that selectively inhibits the E3 ligase complex SCF^βTrCP1-mediated ubiquitination of phosphorylated IκBα (IC₅₀ = 5.2 µM), displaying little inhibitory potency against IKKβ-catalyzed IκBα phosphorylation, MDM2-mediated p53 ubiquitination, or the protease activities of cathepsin B, chymotrypsin, 20S & 26S proteasome (IC₅₀ >100 µM). Effectively inhibits TNFα- and LPS-stimulated NF-κB transcription in HEK293, HT-29, and THP-1 cultures (IC₅₀ from 2.1 to 10.5 µM). Intranasal administration (32 µg/20 µL/mouse) among OVA-sensitized mice 2 h prior to OVA challenge via inhalation greatly suppress NF-κB activation in lung tissue and airway inflammation in vivo. GS143 most likely prevents SCF^βTrCP1 from interacting with phosphorylated IκBα without inhibiting SCF^βTrCP1 E3 ligase activity directly.
Catalogue Number	530588
Brand Family	Calbiochem®
Synonyms	4-(3-Benzyl-4-(5-(2-fluoro-phenyl)-furan-2-ylmethylene)-5-oxo-4,5-dihydropyrazol-1-yl)-benzoic acid, 4-(3-Benzyl-4-((5-(2-fluorophenyl)furan-2-yl)methylene)-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid, GS 143

References
References	Hirose, K., et al. 2008. Biochem. Biophys. Res. Commun. 374, 507. Nakajima, H., et al. 2008. Biochem. Biophys. Res. Commun. 368, 1007.

Product Information
CAS number	916232-21-8
Form	Dark red powder
Hill Formula	C₂₈H₁₉FN₂O₄
Chemical formula	C₂₈H₁₉FN₂O₄
Structure formula Image
Quality Level	MQ100

Applications

Biological Information
Primary Target	phosphorylated IκBα
Purity	≥97% by HPLC

Physicochemical Information
Cell permeable	Y

Dimensions

Materials Information

Toxicological Information

Safety Information according to GHS

Safety Information

Product Usage Statements

Storage and Shipping Information
Ship Code	Ambient Temperature Only
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
5.30588.0001	04055977260939

Documentation

IκB Ubiquitination Inhibitor, GS143 - CAS 916232-21-8 - Calbiochem MSDS

职位
物料安全数据表 (MSDS)

参考

参考信息概述
Hirose, K., et al. 2008. Biochem. Biophys. Res. Commun. 374, 507. Nakajima, H., et al. 2008. Biochem. Biophys. Res. Commun. 368, 1007.

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	13-June-2014 JSW
Synonyms	4-(3-Benzyl-4-(5-(2-fluoro-phenyl)-furan-2-ylmethylene)-5-oxo-4,5-dihydropyrazol-1-yl)-benzoic acid, 4-(3-Benzyl-4-((5-(2-fluorophenyl)furan-2-yl)methylene)-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid, GS 143
Description	A cell-permeable trisubstituted oxo-dihydropyrazolyl-benzoic acid that selectively inhibits the E3 ligase complex SCF^βTrCP1-mediated ubiquitination of phosphorylated IκBα (IC₅₀ = 5.2 µM), displaying little inhibitory potency against IKKβ-catalyzed IκBα phosphorylation, MDM2-mediated p53 ubiquitination, or the protease activities of cathepsin B, chymotrypsin, 20S & 26S proteasome (IC₅₀ >100 µM). Cellular IκBα degradation blockage by GS143 treatment (complete inhibition against TNFα-induced degradation with 30 min 20 µM drug pretreatment in in HeLa S3 and HT29 cultures) effectively inhibits TNFα- and LPS-stimulated NF-κB transcription in HEK293, HT-29, and THP-1 cultures (IC₅₀ from 2.1 to 10.5 µM). Intranasal administration (32 µg/20 µL/mouse) among OVA-sensitized mice 2 h prior to OVA challenge via inhalation greatly suppress OVA challenge-induced NF-κB activation in lung tissue (> 90% inhibition of nuclear NF-κB p65 DNA-binding activity 2 h post challenge) and airway inflammation (>80% reduction in eosinophils & lymphocytes in BALF 48 h post challenge) in vivo. GS143 most likely prevents SCF^βTrCP1 from interacting with phosphorylated IκBα without inhibiting SCF^βTrCP1 E3 ligase activity directly, as no apparent accumulation of another known SCF^βTrCP1 substrate β-catenin is seen in HeLa S3 cells upon GS143 treatment (up to 20 µM for 3 h).
Form	Dark red powder
Intert gas (Yes/No)	Packaged under inert gas
CAS number	916232-21-8
Chemical formula	C₂₈H₁₉FN₂O₄
Structure formula
Purity	≥97% by HPLC
Solubility	DMSO (25 mg/ml). Use only fresh DMSO for reconstitution.
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	Hirose, K., et al. 2008. Biochem. Biophys. Res. Commun. 374, 507. Nakajima, H., et al. 2008. Biochem. Biophys. Res. Commun. 368, 1007.

种类

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > NF-κB Activation > NF-κB Activation Inhibitors

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