GDC-0152 is a potent inhibitor of IAPs and binds to the XIAP BIR3 domain, the BIR domain of ML-IAP, and the BIR3 domains of cIAP1 and cIAP2 with K (i) values of 28, 14, 17, and 43 nM, respectively.

SM-164 is a potent cell-permeable and bivalent Smac mimetic which bind to a XIAP protein with a Ki value of 0.56 nM, and binds to cIAP-1 and cIAP-2 proteins with Ki values of 0.31 and 1.1 nM, respectively.

Birinapant binds with XIAP and cIAP1 with K of 45 and <1 nM, respectively.

E3 ligase Ligand 9 is a Bestatin-based E3 ligase ligand.

AZD5582 is a class of dimeric Smac mimetics as potent IAP antagonist and binds potently to the BIR3 domains of cIAP1, cIAP2, and XIAP (IC50 = 15, 21, and 15 nM, respectively).

An orally bioavailable, non-peptidomimetic antagonist of both X chromosome-linked inhibitor of apoptosis protein (XIAP) and cellular IAP 1 (cIAP1), with potential antineoplastic and pro-apoptotic activities.

UC-112 is a potent IAP (Inhibitor of apoptosis) inhibitor, and potently inhibits cell growth in two human melanoma (A375 and M14) and two human prostate (PC-3 and DU145) cancer cell lines (IC50=0.7-3.4 μM).

AT406 is a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs), AT-406 binds to XIAP, cIAP1, and cIAP2 proteins with K (i) of 66.4, 1.9, and 5.1 nM, respectively.

BV6 is a small-molecule Smac mimetic, which antagonizes IAP and induces autoubiquitination and subsequent proteasomal degradation of cIAP1 and cIAP2.

Embelin, a quinone isolated from the Japanese Ardisia herb, is an inhibitor of X-linked inhibitor of apoptosis (XIAP) with IC50 of 4.1 μM in a cell-free assay.

Polygalacin D, a natural product isolated and purified from the roots of Polygala tenuifolia Willd, can inhibit the expression of lipopolysaccharide (LPS)-induced iNOS and COX-2 protein and mRNA without an appreciable cytotoxic effect on RAW 264.7 macrophages, suppress induction by LPS of pro-inflammatory cytokines such as prostaglandin E2 (PGE2), exhibit significant inhibition on the proliferation of five kinds of cultured human tumor cell lines, i.

LCL161 is an IAP inhibitor, inhibits XIAP activity in HEK293 cell with IC50 of 35 nM, also inhibits cIAP1 activity in MDA-MB-231 cell with IC50 of 0.4 nM.

MX69 is a dual inhibitor of MDM2 and XIAP which can induce MDM2 downregulation resulted not only in inhibition of XIAP expression, but also in activation of p53.