1. Signaling Pathways
  2. Apoptosis
  3. IAP

IAP

IAP (Inhibitor of apoptosis) proteins, a family of anti-apoptotic proteins, have an important role in evasion of apoptosis, as they can both block apoptosis-signaling pathways and promote survival. Eight members of this family have been described in humans (BIRC1/NAIP, BIRC2/cIAP1, BIRC3/cIAP2, BIRC4/XIAP, BIRC5/Survivin, BIRC6/Apollon, BIRC7/ML-IAP and BIRC8/ILP2).

IAP genes encode proteins that directly bind and inhibit caspases, and thus play a critical role in deciding cell fate. The IAPs are in turn regulated by endogenous proteins (second mitochondrial activator of caspases and Omi) that are released from the mitochondria during apoptosis. IAP protein family members are frequently overexpressed in cancer and contribute to tumor cell survival, chemo-resistance, disease progression, and poor prognosis. Targeting critical apoptosis regulators, like IAPs, is an attractive therapeutic way undertaken for the development of new classes of therapies for cancer.

Although best known for their ability to regulate caspases, IAPs also influence ubiquitin (Ub)-dependent pathways that modulate innate immune signaling via activation of NF-κB. Several members of the IAP family regulate innate and adaptive immunity through modulation of signal transduction pathways, cytokine production, and cell survival. The regulation of immunity by the IAPs is primarily mediated through the ubiquitin ligase function of cIAP1, cIAP2, and XIAP, the targets of which impact NF-κB and MAPK signalling pathways.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-16591
    Birinapant
    Antagonist 99.70%
    Birinapant (TL32711), a bivalent Smac mimetic, is a potent antagonist for XIAP and cIAP1 with Kds of 45 nM and less than 1 nM, respectively. Birinapant (TL32711) induces the autoubiquitylation and proteasomal degradation of cIAP1 and cIAP2 in intact cells, which results in formation of a RIPK1: caspase-8 complex, caspase-8 activation, and induction of tumor cell death. Birinapant (TL32711) targets TRAF2-associated cIAPs and abrogates TNF-induced NF-κB activation.
    Birinapant
  • HY-15518
    LCL161
    Inhibitor 99.91%
    LCL161 is a IAP inhibitor which inhibits XIAP in HEK293 cell and cIAP1 in MDA-MB-231 cell with IC50s of 35 and 0.4 nM, respectively.
    LCL161
  • HY-15989
    SM-164
    Antagonist 99.65%
    SM-164 is a cell-permeable Smac mimetic compound. SM-164 binds to XIAP protein containing both the BIR2 and BIR3 domains with an IC50 value of 1.39 nM and functions as an extremely potent antagonist of XIAP.
    SM-164
  • HY-12600
    AZD5582
    Antagonist 98.21%
    AZD5582 is an antagonist of the inhibitor of apoptosis proteins (IAPs), which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC50s of 15, 21, and 15 nM, respectively. AZD5582 induces apoptosis.
    AZD5582
  • HY-15454
    Xevinapant
    Antagonist 99.94%
    Xevinapant (AT-406) is a potent and orally bioavailable Smac mimetic and an antagonist of IAPs, and it binds to XIAP, cIAP1, and cIAP2 proteins with Ki of 66.4, 1.9, and 5.1 nM, respectively.
    Xevinapant
  • HY-160022
    XIAP BIR2/BIR2-3 inhibitor-1
    Inhibitor
    XIAP BIR2/BIR2-3 inhibitor-1 (compound 3) is a dual inhibitor of BIR2 and BIR2-3 with IC50s of 1.9 and 0.8 nM, respectively. XIAP BIR2/BIR2-3 inhibitor-1 can used in study cancers.
    XIAP BIR2/BIR2-3 inhibitor-1
  • HY-160030
    XIAP BIR2/BIR2-3 inhibitor-3
    Inhibitor
    XIAP BIR2/BIR2-3 inhibitor-3 is a dual inhibitor of BIR2 and BIR2-3 with IC50s less than 1 nM. XIAP BIR2/BIR2-3 inhibitor-3 can used in study cancers.
    XIAP BIR2/BIR2-3 inhibitor-3
  • HY-16701
    BV6
    Antagonist 99.50%
    BV6 is an antagonist of cIAP1 and XIAP, members of the inhibitors of apoptosis (IAP) family.
    BV6
  • HY-17473
    Embelin
    Antagonist 98.75%
    Embelin (Embelic acid), a potent, nonpeptidic XIAP inhibitor (IC50=4.1 μM), inhibits cell growth, induces apoptosis, and activates caspase-9 in prostate cancer cells with high levels of XIAP. Embelin blocks NF-kappaB signaling pathway leading to suppression of NF-kappaB-regulated antiapoptotic and metastatic gene products. Embelin also induces autophagic and apoptotic cell death in human oral squamous cell carcinoma cells.
    Embelin
  • HY-109565
    Tolinapant
    Antagonist 99.60%
    Tolinapant (ASTX660) is an orally bioavailable dual antagonist of cellular inhibitor of apoptosis protein (cIAP) and X-linked inhibitor of apoptosis protein (XIAP).
    Tolinapant
  • HY-12486
    FL118
    Inhibitor 99.14%
    FL118 (10,11-(Methylenedioxy)-20(S)-camptothecin), a Camptothecin (HY-16560) analogue, is a potent and orally active survivin inhibitor. FL118 binds to oncoprotein DDX5 (p68) to dephosphorylates and degrades DDX5. FL118 can be used for the research of cancer.
    FL118
  • HY-13638
    GDC-0152
    Inhibitor 99.67%
    GDC-0152 is a potent IAPs inhibitor, and binds to the BIR3 domains of XIAP, cIAP1, cIAP2 and the BIR domain of ML-IAP with Ki values of 28 nM, 17 nM, 43 nM and 14 nM, respectively.
    GDC-0152
  • HY-125593
    Dasminapant
    Antagonist 99.36%
    Dasminapant (APG-1387), a bivalent SMAC mimetic and an IAP antagonist, blocks the activity of IAPs family proteins (XIAP, cIAP-1, cIAP-2, and ML-IAP). Dasminapant induces degradation of cIAP-1 and XIAP proteins, as well as caspase-3 activation and PARP cleavage, which leads to apoptosis. Dasminapant can be used for the research of hepatocellular carcinoma, ovarian cancer, and nasopharyngeal carcinoma.
    Dasminapant
  • HY-13208
    Xevinapant hydrochloride
    Antagonist 98.80%
    Xevinapant (AT-406) hydrochloride is a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs). Xevinapant hydrochloride binds to XIAP, cIAP1, and cIAP2 proteins with Kis of 66.4, 1.9, and 5.1 nM, respectively. Xevinapant hydrochloride effectively antagonizes XIAP BIR3 protein in a cell-free functional assay, induces rapid degradation of cellular cIAP1 protein, and inhibits cancer cell growth in various human cancer cell lines. Xevinapant hydrochloride is highly effective in induction of apoptosis in xenograft tumors.
    Xevinapant hydrochloride
  • HY-110346
    AZD5582 dihydrochloride
    Antagonist 98.67%
    AZD5582 dihydrochloride is an antagonist of the inhibitor of apoptosis proteins (IAPs), which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC50s of 15, 21, and 15 nM, respectively. AZD5582 induces apoptosis.
    AZD5582 dihydrochloride
  • HY-15835
    CUDC-427
    Inhibitor 99.01%
    CUDC-427 is a potent second-generation pan-selective IAP antagonist, used for treatment of various cancers.
    CUDC-427
  • HY-15989A
    SM-164 Hydrochloride
    Antagonist 98.10%
    SM-164 Hydrochloride is a cell-permeable Smac mimetic compound. SM-164 binds to XIAP protein containing both the BIR2 and BIR3 domains with an IC50 value of 1.39 nM and functions as an extremely potent antagonist of XIAP.
    SM-164 Hydrochloride
  • HY-100892
    MX69
    Inhibitor 99.60%
    MX69 is an inhibitor of MDM2/XIAP, used for cancer treatment.
    MX69
  • HY-113534
    MV1
    Antagonist 99.10%
    MV1 is an antagonist of IAP (inhibitor of apoptosis protein), leads to protein knockdown of HaloTag-fused proteins when combined with HaloTag ligand.
    MV1
  • HY-N3001
    Isolinderalactone
    Inhibitor 98.79%
    Isolinderalactone suppresses human glioblastoma growth and angiogenic activity through the inhibition of VEGFR2/KDR/Flk-1 activation in endothelial cells. Isolinderalactone suppresses the expression of B-cell lymphoma 2 (Bcl-2), survi
    Isolinderalactone
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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