Birinapant

Description

Birinapant TL32711 , a bivalent Smac mimetic, is a potent antagonist for XIAP and cIAP1 with Kds of 45 nM and less than 1 nM, respectively. Birinapant TL32711 induces the autoubiquitylation and proteasomal degradation of cIAP1 and cIAP2 in intact cells, which results in formation of a RIPK1: caspase-8 complex, caspase-8 activation, and induction of tumor cell death. Birinapant TL32711 targets TRAF2-associated cIAPs and abrogates TNF-induced NF-?B activation.