Apoptosis Activator VIII, TP421

A cell-permeable triphenylphosphonium compound that exhibits selective toxicity towards cancer cells and inhibits their proliferation (IC₅₀ = 400, 500, 800 nM and 1.1. µM for HPAC, MIA PaCa-2, BxPC-3, and PANC-1 pancreatic cancer cells, respectively). Arrests cell cycle at G0/G1 phase of the cell cycle in a time- and dose-dependent manner. It accumulates in mitochondria and induces mitochondrial and cytosolic accumulation of reactive oxygen species. Induces apoptosis by activating caspase-8 and 7 and by lowering the levels of Bcl-2 and survivin in cancer cells. Reduces autophagy as evidenced by a reduction in beclin-1 and increase in LC3B-II and p62 levels (at ~20 µM). Also shown to diminish Src phosphorylation (Tyr416) correspondingly reduce in Ser576 and Tyr861 phosphorylation in focal adhesion kinase (FAK).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Cell permeable: yes

Packaged under inert gas

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

Millard, M., et al. 2013. PLos One.5, e13131.

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

Toxicity: Standard Handling (A)