Signaling Pathway

IAP

IAP

Related Products

PDF File 0.25MB

IAP (Inhibitors of Apoptosis) is a family of functionally and structurally related proteins, which serve as endogenous inhibitors of programmed cell death (apoptosis). A common feature of all IAPs is the presence of a BIR in one to three copies. The human IAP family consists of 8 members, and IAP homologs have been identified in numerous organisms. The members of the IAPs included IAPs, Cp-IAP, Op-IAP, XIAP, c-IAPl, C-IAP2, NAIP, Livin and Survivin. The best characterized IAP is XIAP, which binds caspase-9, caspase-3 and caspase 7, thereby inhibiting their activation and preventing apoptosis. Also cIAP1 and cIAP2 have been shown to bind caspases, although how the IAPs inhibit apoptosis mechanistically at the molecular level is not completely understood.

IAP Inhibitors & Modulators (10)

Product Name Catalog No. Brief Description
AZD5582

HY-12600

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

Birinapant

HY-16591

Birinapant, a bivalent Smac mimetic, is a potent antagonist for XIAP and cIAP1(Kd value are 45 nM and <1 nM respectively).

BV6

HY-16701

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

CUDC-427

HY-15835

CUDC-427(GDC-0917) is a small-molecule peptide mimetic of SMAC/DIABLO; directly antagonize inhibitors of apoptosis proteins (IAPs).

Embelin

HY-17473

Embelin is a cell-permeable benzoquinone compound that exhibits antitumor properties.

GDC-0152

HY-13638

GDC-0152 is a potent inhibitor of IAPs; 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

HY-15518

LCL161 is an orally bioavailable SMAC mimetic and inhibitor of Inhibitor of Apoptosis Protein (IAP) family of proteins, with antineoplastic activity.

MX69

HY-100892

MX69 is the MDM2/XIAP inhibitor, used for cancer treatment.

SM-164

HY-15989

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.

UC-112

HY-12842

UC-112 is a novel potent IAP(Inhibitor of apoptosis) inhibitor; potently inhibit 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 uM).