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Description

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 µ,M) and H460 (at 5 µ,M) 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 µ,M) and H460 (IC50 = 30 µ,M) cells and synergistically enhances their sensitivity to radiation treatment. Reported to increase apoptosis via caspase-8 activation in HCC193 cells (~ 1 µ,M) and via caspase-9 in H460 cells (~ 5 µ,M). 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 µ,M) and H460 (at 5 µ,M) 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 µ,M) and H460 (IC50 = 30 µ,M) cells and synergistically enhances their sensitivity to radiation treatment. Reported to increase apoptosis via caspase-8 activation in HCC193 cells (~ 1 µ,M) and via caspase-9 in H460 cells (~ 5 µ,M). 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.