2. Apoptosis
  3. IAP

IAP

IAP

Related Products

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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 Related Products (49):

Cat. No. Product Name Effect Purity
  • HY-12600
    AZD5582 Antagonist 98.75%
    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[1].
  • 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.
  • HY-15989
    SM-164 Antagonist 99.49%
    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.
  • HY-16591
    Birinapant Antagonist
    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.
  • HY-15454
    Xevinapant Antagonist 99.91%
    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.
  • 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[1].
  • 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[1].
  • HY-155019
    Anticancer agent 128 Inhibitor
    Anticancer agent 128 (compound 1) is an IAP inhibitor that covalently targets the BIR3 domains of XIAP, cIAP1, and cIAP2. Anticancer agent 128 targets the BIR3 domains of XIAP, cIAP1, and cIAP2 with IC50s of 24.9 nM, 19.3 nM, and 10.3 nM, respectively[1].
  • 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[1][2][3].
  • HY-155018
    Anticancer agent 127 Inhibitor
    Anticancer agent 127 (142D6) is an IAP inhibitor that covalently targets the BIR3 domains of XIAP, cIAP1, and cIAP2. Anticancer agent 127 targets the BIR3 domains of XIAP, cIAP1, and cIAP2 with IC50s of 12 nM, 14 nM, and 9 nM, respectively. Anticancer agent 127 has anticancer effects[1].
  • HY-138059
    SM-433 Inhibitor 99.01%
    SM-433, a Smac mimetic, function as inhibitor of inhibitor of apoptosis proteins (IAPs). SM-433 exhibits strong binding affinity XIAP BIR3 protein with an IC50<1 μM (patent WO2008128171A2)[1].
  • HY-126166
    NOC-5 Activator 98.50%
    NOC-5 is a diazeniumdiolate compound that belongs to the same family of NO donors. NOC-5 is able to increase intracellular XIAP and Aven levels, potentially leading to the inhibition of caspase-9 activity following increased mitochondrial permeability[1][2].
  • HY-109565
    Tolinapant Antagonist 99.81%
    Tolinapant (ASTX660) is an orally bioavailable dual antagonist of cellular inhibitor of apoptosis protein (cIAP) and X-linked inhibitor of apoptosis protein (XIAP).
  • HY-12842
    UC-112 Inhibitor
    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).
  • 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[1].
  • HY-15519
    LBW242 Inhibitor
    LBW242, a 3-mer and Smac mimetic, is a potent and orally active proapoptotic IAP inhibitor. LBW242 shows effects on mutant FLT3-expressing cells. LBW242 has activity against multiple myeloma, and potentiates TRAIL- and anticancer agent-mediated cell death of ovarian cancer cells[1][2].
  • 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.
  • HY-125378A
    (7R)-SBP-0636457 Control 98.36%
    (7R)-SBP-0636457 is the isomer of SBP-0636457 (HY-125378), and can be used as an experimental control. SBP-0636457 (SB1-0636457) is a SMAC mimetic, and as an IAP antagonist. SBP-0636457 binds to the BIR-domains of the IAP proteins, with a Ki of 0.27 μM. SBP-0636457 can be used for the research of solid tumors and hematologic cancers[1][2].
  • HY-160024
    XIAP BIR2/BIR2-3 inhibitor-2 Inhibitor
    XIAP BIR2/BIR2-3 inhibitor-2 is a dual inhibitor of BIR2 and BIR2-3 with IC 50s less than 1 nM. XIAP BIR2/BIR2-3 inhibitor-2 can used in study cancers[1].
  • HY-138059A
    SM-433 hydrochloride Inhibitor 98.57%
    SM-433 hydrochlorid, a Smac mimetic, function as inhibitor of inhibitor of apoptosis proteins (IAPs). SM-433 hydrochlorid exhibits strong binding affinity XIAP BIR3 protein with an IC50<1 μM (patent WO2008128171A2)[1].