5.33965

IAP Antagonist, BV6

• 別名: IAP Antagonist, BV6, (S,S,2S,2ʹS)-N,Nʹ-((2S,2ʹS)-(hexane-1,6-diylbis(azanediyl))bis(3-oxo-1,1-diphenylpropane-3,2-diyl))bis(1-((S)-2-cyclohexyl-2-((S)-2-(methylamino)propanamido)acetyl)pyrrolidine-2-carboxamide)
• 実験式（ヒル表記法）: C₇₀H₉₆N₁₀O₈
• CAS番号: 1001600-56-1
• 分子量: 1205.57
• UNSPSCコード: 51111800
• NACRES: NA.77

特性

• アッセイ: ≥98% (HPLC)
• 品質水準: 100
• 形状: powder
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; desiccated (hygroscopic); protect from light
• 色: white
• 溶解性: DMSO: 50 mg/mL
• 保管温度: −20°C

詳細

詳細

A bivalent SMAC mimetic that antagonizes cIAP1 and XIAP interaction with initiator caspases and triggers their proteasomal degradation. Shown to rapidly deplete levels of cIAP1 and XIAP in HCC193 (at 1 µM) and H460 (at 5 µM) lung cancer cell lines. Levels of cIAP1 are reduced within an hour following treatment while XIAP depletion takes up to 24 h. Effectively reduces the viability of HCC193 (IC₅₀ = 7.2 µM) and H460 (IC₅₀ = 30 µM) cells and synergistically enhances their sensitivity to radiation treatment. Reported to increase apoptosis via caspase-8 activation in HCC193 cells (~ 1 µM) and via caspase-9 in H460 cells (~ 5 µM). Also shown to increase the secretion of TNFa in HCC193 cells in a dose-dependent manner. Also enhances cytokine-induced killer (CIK) cell-mediated cytotoxicity against multiple hematological (H9, THP-1, Tanoue) and solid malignant cells (RH1, RH30, and TE671).

A bivalent SMAC mimetic that antagonizes cIAP1 and XIAP interaction with initiator caspases and triggers their proteasomal degradation. Shown to rapidly deplete levels of cIAP1 and XIAP in HCC193 (at 1 µM) and H460 (at 5 µM) lung cancer cell lines. Levels of cIAP1 are reduced within an hour following treatment while XIAP depletion takes up to 24 h. Effectively reduces the viability of HCC193 (IC₅₀ = 7.2 µM) and H460 (IC₅₀ = 30 µM) cells and synergistically enhances their sensitivity to radiation treatment. Reported to increase apoptosis via caspase-8 activation in HCC193 cells (~ 1 µM) and via caspase-9 in H460 cells (~ 5 µM). Also shown to increase the secretion of TNFa in HCC193 cells in a dose-dependent manner. Also enhances cytokine-induced killer (CIK) cell-mediated cytotoxicity against multiple hematological (H9, THP-1, Tanoue) and solid malignant cells (RH1, RH30, and TE671).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
IAP

Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

物理的形状

Supplied as a trifluoroacetate salt.

再構成

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

その他情報

Rettinger, E., et al. 2014. Front in Pediatr.2, 75.
Li, W., et al. 2011. J. Thorac. Oncol.6, 1801.

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