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.

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.

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.

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.

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.

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.

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.

CUDC-427 is a small-molecule peptide mimetic of SMAC/DIABLO and directly antagonizes inhibitors of apoptosis proteins (IAPs).