IAP Antagonist, BV6

Cell permeable: yes

Primary Target
IAP

Reversible: yes

Toxicity: Standard Handling (A)

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.

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

Packaged under inert gas

Supplied as a trifluoroacetate salt.

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

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