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			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

375240 Sigma-AldrichHNF4 Antagonist, BI6015 - CAS 93987-29-2 - Calbiochem

The HNF4 Antagonist, BI6, also referenced under CAS 93987-29-2, controls the biological activity of HNF4.

HNF4 Antagonist, BI6015 - CAS 93987-29-2 - 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
試験成績書（CoA）
参考資料
Data Sheet

同義語: Hepatocyte Nuclear Factor4 Antagonist, 2-Methyl-1-(2-methyl-5-nitrophenylsulfonyl)-1H-benzo[d]imidazole

Primary Target: HNFα & γ

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概要

Replacement Information

主要スペック表

CAS #	Empirical Formula
93987-29-2	C₁₅H₁₃N₃O₄S

価格＆在庫状況

カタログ番号	在庫状況	包装	Qty/Pk	価格	数量
375240-25MGCN	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	25 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 phenylsulfonylbenzimidazole that is shown to dock in the ligand-binding pocket of both HNF4α and HNF4γ and antagonize HNF4α DNA binding activity in HepG2 cells (by 93%; 10 µM overnight), effectively inhibiting HNF4α-dependent cellular activities (Effective conc. 1 to 5 µM). HNF4γ inhibition by BI6015 can also lead to decreased insulin promoter binding by transactivators E47 & PDX-1 in T6PNE cells (5 µM 48 h). Although BI6015 is found to exhibit cancer-selective cytotoxicity toward a panel of 58 human cancer cells and Hep3B-Luc (Effective conc. 1 to 10 µM), but not primary murine hepatocytes, it does cause hepatic steatosis both in vitro and in mice in vivo, limiting its use in animal studies. BI6015 also inhibits Human CYP450 2C19 and rat L-type calcium channel (by 94% and 83%, respectively, at 10 µM), but not PPARγ or a panel of 41 receptors/enzymes of human, mouse, and rat origin.
Catalogue Number	375240
Brand Family	Calbiochem®
Synonyms	Hepatocyte Nuclear Factor4 Antagonist, 2-Methyl-1-(2-methyl-5-nitrophenylsulfonyl)-1H-benzo[d]imidazole

References
References	Kiselyuk, A., et al. 2012. Chem. Biol. 19, 806.

Product Information
CAS number	93987-29-2
Form	Beige powder
Hill Formula	C₁₅H₁₃N₃O₄S
Reversible	Y
Structure formula Image
Quality Level	MQ100

Applications

Biological Information
Primary Target	HNFα & γ
Purity	≥99% 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 6 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
375240-25MGCN	04055977212891

Documentation

HNF4 Antagonist, BI6015 - CAS 93987-29-2 - Calbiochem (M)SDS

タイトル
英語版製品安全データシート（(M)SDS）

HNF4 Antagonist, BI6015 - CAS 93987-29-2 - Calbiochem 試験成績書（CoA）

タイトル	ロット番号
375240	ロット番号を入力

参考資料

参考資料の概要
Kiselyuk, A., et al. 2012. Chem. Biol. 19, 806.

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	11-October-2012 JSW
Synonyms	Hepatocyte Nuclear Factor4 Antagonist, 2-Methyl-1-(2-methyl-5-nitrophenylsulfonyl)-1H-benzo[d]imidazole
Description	A cell-permeable phenylsulfonylbenzimidazole compound that is shown to dock in the ligand-binding pocket of both HNF4α and HNF4γ via in silico structural analyses and antagonizes HNF4α DNA binding activity (by 93% after 10 µM overnight treatment of HepG2 cells), effectively inhibiting HNF4α-dependent cellular activities, including HNF4α mRNA transcription (by 62% in murine insulinoma MIN6 and 84% in human hepatoma HepG2 cultures after 5 h and 48 h 5 µM inhibitor treatment, respectively) and OTC (omithine transcarbamoylase) promoter transcription (by 85% & >95% in human HNF4α-transfected HepG2 & CV-1 cells, respectively; 48 hr 1 µM treatment). HNF4γ inhibition by BI6015 is also reported to indirectly lead to decreased binding of transactivators, E47 & PDX-1, to insulin promoter in T6PNE cells (48 h 5 µM treatment). Although BI6015 is found to exhibit cancer-selective cytotoxicity toward a panel of 58 human cancer cells and Hep3B-Luc (Effective conc. 1 to 10 µM), but not primary murine hepatocytes, it does cause hepatic steatosis both in vitro (primary murine hepatocytes; 5 µM for 3 days) and in mice in vivo (10 to 30 mg/kg/day for 5 days via i.p.) and is effectively metabolized by liver enzymes, limiting its in vivo efficacy in treating human Hep3B-derived liver tumor in mice. BI6015 also inhibits Human CYP450 2C19 and rat L-type calcium channel (by 94% and 83%, respectively, at 10 µM), but not PPARγ or a panel of 41 receptors/enzymes of human, mouse, and rat origin.
Form	Beige powder
Intert gas (Yes/No)	Packaged under inert gas
CAS number	93987-29-2
Structure formula
Purity	≥99% by HPLC
Solubility	DMSO (10 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 6 months at -20°C.
Toxicity	Standard Handling
References	Kiselyuk, A., et al. 2012. Chem. Biol. 19, 806.

カテゴリー

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

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