385570

Heat Shock Factor 1 Inhibitor, KRIBB11

The Heat Shock Factor 1 Inhibitor, KRIBB11 controls the biological activity of Heat Shock Factor 1.

• 別名: Heat Shock Factor 1 Inhibitor, KRIBB11, Hsp70 Induction Inhibitor II, N²-(1H-Indazol-5-yl)-N⁶-methyl-3-nitropyridine-2,6-diamine, HSF1 Inhibitor, KRIBB11, Heat Shock Protein Inhibitor III, p-TEFb hsp70 Promoter Recruitment Inhibitor
• 実験式（ヒル表記法）: C₁₃H₁₂N₆O₂
• CAS番号: 342639-96-7
• 分子量: 284.27
• MDL番号: MFCD30182306
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 品質水準: 200
• アッセイ: ≥98% (HPLC)
• 形状: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: orange-yellow
• 溶解性: DMSO: 50 mg/mL, brown
• 輸送温度: ambient
• 保管温度: −20°C
• SMILES記法: CNC(C=C1)=NC(NC2=CC3=C(NN=C3)C=C2)=C1[N+]([O-])=O

詳細

詳細

A cell-permeable 2,6-diaminopyridine compound that interacts with HSF1 (heat shock factor 1) in a reversible manner and prevents HSF1 from recruiting p-TEFb (positive transcription elongation factor b) to the hsp70 promoter site (IC₅₀ ≤3 µM in HCT-116 ChIP assays), a critical step for the p-TEFb CDK9 subunit-catalyzed pol II CTD (RNA polymerase II c-terminal domain) Ser-2 phosphorylation and transcription activation upon heat shock induction (IC₅₀<1, <3, <5, and <10 µM, respectively, against reporter, HSP47, HSP27, and HSP70 transcription in HCT-116 cultures). Reported to exhibit antiproliferation activity against several cancer cultures in vitro (IC₅₀ ranges from 3 to 8 µM) and effectively suppress HCT-116-derived tumor growth in mice in vivo (by 47.4% on day 31; single i.p. dosage of 50 mg/kg on day 13 after cancer implantation). Does not affect TNF-α-induced NF-κB activity in HeLa or heat shock-induced HSF1 ser230 phosphorylation and promoter association in HCT-116 even at concentrations as high as 10 µM.

A cell-permeable 2,6-diaminopyridine compound that interacts with HSF1 in a reversible manner and prevents HSF1 from recruiting p-TEFb to the hsp70 promoter site (IC₅₀ ≤3 µM in HCT-116 ChIP assays), a critical step for heat shock-induced transcription activation (IC₅₀<1, <3, <5, and <10 µM, respectively, against reporter, HSP47, HSP27, and HSP70 transcription in HCT-116 cultures). Reported to exhibit antiproliferation activity against several cancer cultures in vitro (IC₅₀ from 3 to 8 µM) and effectively suppress HCT-116-derived tumor growth in mice in vivo (50 mg/kg i.p.).

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

再構成

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

その他情報

Yoon, Y.J., et al. 2010. J. Biol. Chem.286, 1737.

法的情報

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable