5.33965

IAP Antagonist, BV6

• Synonim(y): 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)
• Wzór empiryczny (zapis Hilla): C₇₀H₉₆N₁₀O₈
• Numer CAS: 1001600-56-1
• Masa cząsteczkowa: 1205.57
• Kod UNSPSC: 51111800
• NACRES: NA.77

Właściwości

• Próba: ≥98% (HPLC)
• Poziom jakości: 100
• Postać: powder
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; desiccated (hygroscopic); protect from light
• kolor: white
• rozpuszczalność: DMSO: 50 mg/mL
• temp. przechowywania: −20°C

Opis

Opis ogólny

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.

Działania biochem./fizjol.

Cell permeable: yes

Primary Target
IAP

Reversible: yes

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Standard Handling (A)

Postać fizyczna

Supplied as a trifluoroacetate salt.

Rekonstytucja

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

Inne uwagi

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

Informacje prawne

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

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable