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-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-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-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-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-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-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-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-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-123870
    MX107
    		Degrader
    MX107 is a selective and potent survivin inhibitor that suppresses triple-negative breast cancer (TNBC) cell proliferation. MX107 induces degradation of survivin and inhibitor-of-apoptosis proteins (IAPs), which inhibits nuclear factor κB (NF-κB) activation induced by DNA damage. MX107 enhances tumoricidal efficacy of genotoxic treatments synergized with chemotherapeutic drugs.
    MX107
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
IAP Isoform Comparison

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