数量	カタログ番号	注文内容	Qty/Pk	価格
			96-Well Plate

数量	カタログ番号	注文内容	Qty/Pk	価格
	48-602MAG	Buffer Detection Kit for Magnetic Beads	1 Kit

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).

IκB Ubiquitination Inhibitor, GS143 - CAS 916232-21-8 - Calbiochem: のSDS（安全データシート）、CoA（試験成績書）およびCoQ（品質証明書）、カタログなど製品関連の技術資料を入手いただけます。

(M)SDS
参考資料
Data Sheet

同義語: 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

View This Product on Sigma-Aldrich

お勧めの製品

概要

Replacement Information

主要スペック表

CAS #	Empirical Formula
916232-21-8	C₂₈H₁₉FN₂O₄

価格＆在庫状況

カタログ番号	在庫状況	包装	Qty/Pk	価格	数量
5.30588.0001	在庫状況検索中… — 現在国内在庫なし現在国内在庫有り販売中止在庫僅少現在国内在庫あり在庫を照会するにはログインしてください現在国内在庫有り現在国内在庫なし現在国内在庫有り Remaining : Will advise Remaining : Will advise 注文対象外お問合せください Contact Customer Service お問合せくださいお問合せください	ｶﾞﾗｽﾋﾞﾝ	10 mg	価格を検索中… 価格が見つかりません Minimum Quantity needs to be mulitiple of Maximum Quantity is 弊社照会詳細を表示　値引 () — 弊社照会納入価格を閲覧するにはログインしてください	在庫状況を照会 —	お気に入り/ショッピングリストに追加お気に入り/ショッピングリストに追加お気に入りに追加されました

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
カタログ番号	GTIN
5.30588.0001	04055977260939

Documentation

IκB Ubiquitination Inhibitor, GS143 - CAS 916232-21-8 - Calbiochem (M)SDS

タイトル
英語版製品安全データシート（(M)SDS）

参考資料

参考資料の概要
Hirose, K., et al. 2008. Biochem. Biophys. Res. Commun. 374, 507. Nakajima, H., et al. 2008. Biochem. Biophys. Res. Commun. 368, 1007.

データシート

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.

カテゴリー

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

製品がカートに追加されました