Birinapant（TL32711）是一种双价Smac模拟物和有效的XIAP和cIAP1拮抗剂，Kd值分别为45 nM和小于1 nM。Birinapant诱导cIAP1和cIAP2在细胞中的自泛素化和蛋白酶体降解，导致RIPK1复合物的形成、caspase-8的激活和肿瘤细胞死亡。它靶向与TRAF2相关的cIAP，并消除TNF诱导的NF-κB激活。

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.

Xevinapant (AT-406) 是一种有效的口服生物可利用的 Smac 模拟物，作为 IAPs 的拮抗剂，能够抑制 XIAP、cIAP1 和 cIAP2 蛋白，其 Ki 值分别为 66.4、1.9 和 5.1 nM。

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).

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.