at-iap

AT-IAP is an effective dual antagonist of XIAP and cIAP1.

PROTAC ERα Degrader-2 is composed of a cIAP1 ligand binding group, a linker, and an estrogen receptor α (ERα) binding group, serving as an ERα degrader. It achieves maximal ERα degradation in human mammary tumor MCF7 cells at a concentration of 30 μM. Degradation inducers that utilize cIAP1 are referred to as specific and non-genetic IAP-dependent protein erasers (SNIPERs)[1].

PROTAC RAR Degrader-1, an RAR degrader, consists of a cIAP1 ligand binding group, a linker, and an RAR ligand binding group. It achieves maximal RAR degradation at a concentration of 30 μM in HT1080 cells. Degradation inducers that utilize cIAP1 are known as specific and non-genetic IAP-dependent protein erasers (SNIPERs)[1].

CST 530 is a monovalent IAP antagonist. It induces cIAP1 and cIAP2 autodegradation in MM.1S cells (cIAP1 degradation at 0.1 μM and cIAP2 degradation at 1 μM after 16 hours). CST 530 reduces cell viability in multiple cancer cell lines including SUDHL6, MOLM13, and HEL (IC50 values ​​of 170 nM, 420 nM, and 450 nM, respectively).

EP4 receptor agonist 3 prodrug (Compound 9) serves as a prodrug for the EP4 receptor agonist (Compound 1a). This prodrug exhibits no intrinsic agonistic activity at the EP4 receptor and requires specific hydrolysis by intestinal alkaline phosphatase (IAP) within the gut to release the active molecule, thereby exerting localized EP4 receptor activation. EP4 receptor agonist 3 prodrug demonstrates targeted action in the colon and significantly alleviates colitis symptoms in mice.

Xevinapant hydrochloride (AT-406 HCl) , an orally active antagonist of multiple inhibitor of apoptosis proteins(IAP), inhibits progression of human ovarian Y binding to XIAP-BIR3, cIAP1-BIR3 and cIAP2-BIR3 with Ki of 66.4 nM, 1.9 nM, and 5.1 nM, 50- to 100-fold higher affinities than the Smac AVPI peptide.

Xevinapant (Debio-1143) is a potent Smac mimetic and an antagonist of IAP (inhibitor of apoptosis protein via E3 ubiquitin ligase), binding to XIAP-BIR3, cIAP1-BIR3 and cIAP2-BIR3 with Ki of 66.4 nM, 1.9 nM, and 5.1 nM, 50- to 100-fold higher affinities than the Smac AVPI peptide. Phase 1.