2. Signaling Pathways
  3. Apoptosis
  4. IAP

IAP

IAP

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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.

IAP Isoform Specific Products:

IAP Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-175449
    XIAP ligand 5
    		Antagonist
    XIAP ligand 5 is a XIAP antagonist. XIAP ligand 5 is an E3 ligase ligand. XIAP ligand 5 can be used for synthesis of PROTAC GNE-1567 (HY-175448).
    XIAP ligand 5
  • HY-181532
    IAP ligand 8
    		Ligand
    IAP ligand 8 is an ASX-series, non-peptidic SMAC mimetic and IAP binder with high cell permeability. IAP ligand 8 selectively targets cIAP1-BIR3, XIAP-BIR2 (with a KD of 15.8 nM for both). IAP ligand 8 serves as an IAP ligand moiety to synthesize IAP-recruiting protein degrader (IPD) (HY-181590). This IPD simultaneously forms two ternary complexes, cIAP1-A538-TEAD1 and XIAP-A538-TEAD1, and efficiently degrades TEAD1 via a dual E3 recruitment mechanism, while inducing the autodegradation of cIAP1. IAP ligand 8 and its series of degraders are applicable to targeted research on Hippo pathway-dysregulated cancers such as NF2-mutant mesothelioma.
    IAP ligand 8
  • HY-158076
    S2/IAPinh
    		Inhibitor
    S2/IAPinh is a conjugate, which consist of an inhibitor for the apoptosis protein inhibitor (IAPinh) and a ligand for sigma 2 SW43. S2/IAPinh exhibits an anti-proliferative and apoptotic-inducing effect through degradation of the cellular inhibitor for apoptosis protein (clAP-1).
    S2/IAPinh
  • HY-175448
    GNE-1567
    		Antagonist
    GNE-1567 is a potent ERα PROTAC degrader and a selective XIAP antagonist with a Kd value of 0.03 μM. GNE-1567 is indicated for breast cancer research. (Pink: ligand for target protein (HY-18719); Black: linker; Blue: ligand for E3 ligase (HY-175449)).
    GNE-1567
  • HY-100682
    T-3256336
    		Inhibitor
    T-3256336 is a potent and orally active cIAP1 and XIAP inhibitor with IC50s of 1.3, 200 nM, respectively. T-3256336 shows anti-tumor activity.
    T-3256336
  • HY-N0732R
    Jolkinolide B (Standard)
    		Inhibitor
    Jolkinolide B (Standard) is the analytical standard of Jolkinolide B (HY-N0732). This product is intended for research and analytical applications. Jolkinolide B is a bioactive diterpene isolated from the roots of Euphorbia fischeriana Steud with oral activity. Jolkinolide B downregulates XIAP, cIAP1, cIAP2, and phosphorylated Akt, upregulates Smac, activates caspase-3 and caspase-9, and inhibits NF-κB, TGFβ/smad3 and JAK/STAT3 pathways. Jolkinolide B exerts comprehensive biological effects including inducing cancer cell apoptosis, suppressing inflammatory responses, improving lung function, alleviating hepatic steatosis and eliminating intracellular Mycobacterium tuberculosis. Jolkinolide B can be used for the research of leukemia, histiocytic lymphoma, asthma, metabolic dysfunction-associated steatotic liver disease and tuberculosis.
    Jolkinolide B (Standard)
  • HY-175348
    XB2M54
    		Antagonist
    XB2M54 is a selective XIAP antagonist. XB2M54 inhibits NOD2-mediated inflammatory signaling. XB2M54 is an E3 ligase ligand. XB2M54 can be used for synthesis of PROTAC ERα Degrader-1 (HY-112098).
    XB2M54
  • HY-120434
    AEG40826
    		Inhibitor
    AEG40826 (HGS1029), a second mitochondria-derived activator of caspases (SMAC) mimetic, is an inhibitor of apoptosis (IAP) inhibitor. AEG40826 degrades cellular IAP1 (cIAP1) and blocks TNF-α pro-survival signaling. AEG40826 can be used for cancer research.
    AEG40826
  • HY-181537
    PROTAC TEAD1/IAP degrader-2
    		Ligand
    PROTAC TEAD1/IAP degrader-2 is an IAP-harnessing TEAD1 PROTAC degrader, with a DC50 of 170 nM against TEAD1 in NCI-H2052 cells. PROTAC TEAD1/IAP degrader-2 exhibits moderate antiproliferative activity in Hippo pathway-dependent mesothelioma cells. PROTAC TEAD1/IAP degrader-2 inhibits the expression of CTGF, but with a weaker effect than the TEAD inhibitor VT-107 (HY-134957). PROTAC TEAD1/IAP degrader-2 can be used in mesothelioma-related research.
    PROTAC TEAD1/IAP degrader-2
  • HY-N2420R
    Flavokawain A (Standard)
    		Inhibitor
    Flavokawain A is a chalcone compound and an orally active inhibitor of PRMT5 and cytochrome P450. Flavokawain A has anti-inflammatory, anti-tumor, and immunomodulatory effects. Flavokawain A can inhibit the proliferation of tumor cells and induce apoptosis. Flavokawain A can be used in the research of diseases such as bladder cancer.
    Flavokawain A (Standard)
  • HY-N15378
    β-Carotene-15,15'-epoxide
    		Antagonist
    β-carotene-15,15ʹ-epoxide is a XIAP antagonist with apoptosis-inducing and antitumor activity, found in the leaves of Spondias mombin. In a DMBA (HY-W011845)-induced rat model of breast cancer, β-carotene-15,15ʹ-epoxide binds to the BIR3 domain of the anti-apoptotic protein XIAP, blocking its interaction with caspase-9 and thereby promoting tumor cell apoptosis. In addition, β-carotene-15,15ʹ-epoxide significantly downregulates the expression of BCL-2, COX-2, and TNF-α in tumor tissues, reduces MDA levels, increases catalase activity, and modulates serum levels of LDH, ALP, and ALT, demonstrating strong antioxidant, anti-inflammatory, and metabolic protective effects. β-carotene-15,15ʹ-epoxide may be used in research on inflammation-related conditions and cancers such as breast cancer.
    β-Carotene-15,15'-epoxide
  • HY-181535
    IAP ligand-Linker Conjugate 1
    		Ligand
    IAP ligand-Linker Conjugate 1 is a ligand-linker conjugate targeting IAP, which can be used in the synthesis of PROTAC TEAD1/IAP degrader-1 (HY-181534).
    IAP ligand-Linker Conjugate 1
  • HY-100892R
    MX69 (Standard)
    		Inhibitor
    MX69 (Standard) is the analytical standard of MX69 (HY-100892). This product is intended for research and analytical applications. MX69 is an inhibitor of MDM2/XIAP, used for cancer treatment.
    MX69 (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
IAP Isoform Comparison

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