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-118522
    TP-110
    		Inhibitor
    TP-110 is a proteasome inhibitor. TP-110 specifically inhibits the protease-like activity of the 20S proteasome, but does not affect the trypsin-like or peptidyl-glutamyl peptide hydrolysis activity. TP-110 inhibits the NF-κB pathway, activates caspase-8, -9, and -3, and causes PARP cleavage, significantly reducing the levels of cIAP-1 and XIAP. TP-110 causes cell cycle arrest at the G2/M phase and promotes apoptosis of cancer cells. TP-110 can be used in cancer research of prostate cancer and multiple myeloma, etc.
    TP-110
  • HY-149978
    LSD1-IN-26
    		Inhibitor
    LSD1-IN-26 (compound 12u) is a potent LSD1 inhibitor, with an IC50 of 25.3 nM. LSD1-IN-26 also inhibits MAO-A (IC50=1234.57 nM) and MAO-B (IC50=3819.27 nM). LSD1-IN-26 significantly induces apoptosis in MGC-803 cells. LSD1-IN-26 can be used for gastric cancer research.
    LSD1-IN-26
  • HY-168739
    Topoisomerase I inhibitor 17
    		Inhibitor
    Topoisomerase I inhibitor 17 (Compound 7h) is a Topoisomerase I (Top1) inhibitor. Topoisomerase I inhibitor 17 reduces DDX5 and reverses the locking of Top1 activity by DDX5. Topoisomerase I inhibitor 17 induces Top1-mediated DNA damage and promotes reactive oxygen species (ROS) production. Topoisomerase I inhibitor 17 induces Apoptosis (reduces antiapoptotic proteins XIAP, Bcl-2, Survivin and up-regulates pro-apoptotic proteins Bax, γH2AX). Topoisomerase I inhibitor 17 also blocks the progression of the G2/M checkpoint and induces cell cycle arrest. Topoisomerase I inhibitor 17 significantly inhibits colony formation and cell migration in colorectal cancer cells. Topoisomerase I inhibitor 17 effectively reduces tumors in human PDX tumor mice.
    Topoisomerase I inhibitor 17
  • HY-W009141R
    1-Monopalmitin (Standard)
    		Inhibitor
    1-Monopalmitin (Glyceryl palmitate) (Standard) is the analytical standard of 1-Monopalmitin (HY-W009141). This product is intended for research and analytical applications. 1-Monopalmitin (Glyceryl palmitate) is an activator of the PI3K/Akt pathway and an inhibitor of P-glycoprotein (P-gp). 1-Monopalmitin can induce G2/M arrest and caspase-dependent apoptosis in cancer cells, while inhibiting IAPs protein expression. 1-Monopalmitin can increase drug accumulation by inhibiting P-gp activity in intestinal Caco-2 cells. 1-Monopalmitin has the ability to induce protective autophagy and apoptosis of lung cancer cells (IC50=50-58 μg/mL), with low toxicity to normal cells.
    1-Monopalmitin (Standard)
  • HY-W009141S
    1-Monopalmitin-d31
    1-Monopalmitin-d31 (Glyceryl palmitate-d31) is the deuterium labeled 1-Monopalmitin (HY-W009141). 1-Monopalmitin (Glyceryl palmitate) is an activator of the PI3K/Akt pathway and an inhibitor of P-glycoprotein (P-gp). 1-Monopalmitin can induce G2/M arrest and caspase-dependent apoptosis in cancer cells, while inhibiting IAPs protein expression. 1-Monopalmitin can increase drug accumulation by inhibiting P-gp activity in intestinal Caco-2 cells. 1-Monopalmitin has the ability to induce protective autophagy and apoptosis of lung cancer cells (IC50=50-58 μg/mL), with low toxicity to normal cells.
    1-Monopalmitin-d<sub>31</sub>
  • HY-175450
    XIAP ligand-Linker Conjugate 2
    		Antagonist
    XIAP ligand-Linker Conjugate 2 is an E3 ligase ligand-linker conjugate that incorporates the XIAP BIR2 ligand XB2M54 (HY-175348) and linker. XIAP ligand-Linker Conjugate 2 can be used for synthesis of PROTAC GNE-1567 (HY-175448).
    XIAP ligand-Linker Conjugate 2
  • HY-102051
    XIAP/cIAP1 antagonist-1
    		Inhibitor
    XIAP/cIAP1 antagonist-1 is a potent and orally active XIAP/cIAP1 antagonist with EC50s of 5.1 nM and 0.32 nM for XIAP and cIAP1, respectively. XIAP/cIAP1 antagonist-1 inhibits the tumor growth in dose-dependent manner in vivo.
    XIAP/cIAP1 antagonist-1
  • HY-17473R
    Embelin (Standard)
    		Antagonist
    Embelin (Standard) is the analytical standard of Embelin. This product is intended for research and analytical applications. 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 (Standard)
  • HY-181319
    PROTAC EZH2 Degrader-21
    		Ligand
    PROTAC EZH2 Degrader-21 is an EZH2 degrader developed based on PROTAC technology. PROTAC EZH2 Degrader-21 induces the degradation of the target protein EZH2 via specific recruitment of the cIAP E3 ligase. PROTAC EZH2 Degrader-21 exhibits significant inhibitory activity in a variety of lymphoma cell lines. PROTAC EZH2 Degrader-21 can be used for research on the pathogenesis of lymphoma.
    PROTAC EZH2 Degrader-21
  • HY-175446
    GDC-0152-acetamide
    		Antagonist
    GDC-0152-acetamide is a pan-inhibitor of apoptosis protein (IAP) antagonist. GDC-0152-acetamide induces cIAP1/2 autoubiquitination and degradation, activating the non-canonical NF-κB pathway to promote TNF-α secretion and tumor cell apoptosis. GDC-0152-acetamide is promising for research of ERα-positive breast cancer.
    GDC-0152-acetamide
  • HY-153199
    MDM2/XIAP-IN-1
    		Inhibitor
    MDM2/XIAP-IN-1 (compound 14) is an orally active inhibitor of dual MDM2/XIAP. MDM2/XIAP-IN-1 has anti-cancer activity with an IC50 value of 0.3 μM, which can be used in cance rescrch.
    MDM2/XIAP-IN-1
  • HY-181410
    PROTAC EZH2 Degrader-41
    PROTAC EZH2 Degrader-41 is an EZH2-targeting PROTAC and cIAP E3 ubiquitin ligase recruiter. PROTAC EZH2 Degrader-41 induces EZH2 degradation via ubiquitination and proteasomal breakdown. PROTAC EZH2 Degrader-41 exerts antiproliferative effects in lymphoma cells. PROTAC EZH2 Degrader-41 can be used for the research of lymphoma.
    PROTAC EZH2 Degrader-41
  • HY-168893
    K882
    		Inhibitor
    K882 (Compound 4e) is a Src inhibitor, with KD of 0.315 μM. K882 induces Apoptosis. K882 inhibits XIAP and Survivin. K882 inhibits the activation of PI3K/Akt/mTOR, Jak1/Stat3, Ras/MAPK signaling pathways. K882 shows anti-tumor activity against non-small cell lung cancer.
    K882
  • 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-180948
    PZ-11
    PZ-11 is a derivative of thiazolidinedione with anti-tumor activity. PZ-11 can induce cancer cells apoptosis by downregulating anti-apoptotic gene AIFM1, BAG3 and BIRC3 and regulating pro-apoptotic gene BAD, HRK, CASP10 and CASP10. PZ-11 can be used for research of breast cancer.
    PZ-11
  • HY-182002
    Apoptosis inducer 61
    		Inhibitor
    Apoptosis inducer 61 (Compound 4E) is an Apoptosis inducer. Apoptosis inducer 61 significantly downregulates the expression of BIRC3 and activates Apoptosis. Anticancer agent 313 exhibits anticancer activity against ER+ breast cancer cells, triple-negative breast cancer cells, and gastric cancer cells.
    Apoptosis inducer 61
  • HY-157230
    XIAP antagonist 1
    		Degrader
    XIAP antagonist 1 degrades rather than inhibits XIAP, catalyzing rapid degradation of XIAP through the ubiquitin-proteasome pathway[2].
    XIAP antagonist 1
  • HY-123925
    CSLP43
    		Inhibitor
    CSLP43 is a selective RIPK2 and XIAP inhibitor with an IC50 of 19.9 nM against human RIPK2. CSLP43 binds to the ATP-binding pocket of RIPK2 and disrupts the interaction between RIPK2 and the BIR2 domain of XIAP or cIAP1. CSLP43 inhibits RIPK2 ubiquitination, NOD1-dependent inflammatory signaling pathways, NOD2-dependent inflammatory signaling pathways, as well as NF-κB activation associated with NOD agonists. CSLP43 is selective for the NOD1/NOD2 signaling pathway and does not inhibit the kinase activity of RIPK1 or RIPK3. CSLP43 is applicable to research related to Crohn's disease, Blau syndrome, early-onset sarcoidosis and early-onset inflammatory bowel disease.
    CSLP43
  • HY-N18315
    (2''S)-2'',3''-Dihydrodelicaflavone
    		Modulator
    (2''S)-2'',3''-Dihydrodelicaflavone is a biflavonoid compound present in the whole herb of Selaginella doederleinii, which exhibits antiproliferative and apoptosis-inducing activities against non-small cell lung cancer cells. (2''S)-2'',3''-Dihydrodelicaflavone can be used in the research of non-small cell lung cancer.
    (2''S)-2'',3''-Dihydrodelicaflavone
  • HY-181533
    IAP ligand 9
    		Ligand
    IAP ligand 9 is an ASX-series, non-peptidic SMAC mimetic and IAP binder with high cell permeability. IAP ligand 9 selectively targets cIAP1-BIR3, XIAP-BIR3, exhibits extremely weak binding affinity for XIAP-BIR2, with a KD of 100 nM for cIAP1-BIR3 and 10 nM for XIAP-BIR2. IAP ligand 9 can be used to synthesize IAP-recruiting protein degraders (IPD), and can calibrate the cell permeability and cellular-level target binding assays of the IPD molecule SNIPER (TEAD)-1 (HY-181607). IAP ligand 9 and its series of degraders can be used in the research of solid tumors such as malignant pleural mesothelioma associated with abnormal activation of the Hippo pathway.
    IAP ligand 9
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
IAP Isoform Comparison

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