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-175352
    Nurr1 agonist 14
    		Inducer 99.42%
    Nurr1 agonist 14 (Compound 32) is a Nurr1 agonist with an EC50 of 0.09  μM for Nurr1. Nurr1 agonist 14 has significant neuroprotective activity with no influence of residual DHODH inhibition. Nurr1 agonist 14 upregulates neuroprotective genes including SOD2, SESN3, BIRC5, XIAP, FLRT2 and CRMP4 in dopaminergic neurons. Nurr1 agonist 14 can be used for neurodegenerative diseases such as Alzheimer′s disease (AD), Parkinson′s disease (PD) and multiple sclerosis (MS) research.
    Nurr1 agonist 14
  • HY-12372
    Sanggenon G
    		Inhibitor
    Sanggenon G is a cell-permeable and potent inhibitor of X-linked inhibitor of apoptosis protein (XIAP). Sanggenon G binds specifically to the BIR3 domain of XIAP with a binding affinity of 34.26 μM. Sanggenon G enhances caspase activation.
    Sanggenon G
  • 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).
    SM-433 hydrochloride
  • 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.
    Anticancer agent 128
  • HY-179023
    CDK9-IN-45
    		Inhibitor
    CDK9-IN-45 (Compound B11) is a highly selective CDK9 inhibitor with IC50 values for CDK9 and CDK1 of 7.13 and 489.5 nM respectively. CDK9-IN-45 exhibits a potent inhibitory effect on colorectal cancer cells. CDK9-IN-45 induces cell apoptosis and leads to significant accumulation of ROS. CDK9-IN-45 activates Caspase-3, downregulates Mcl-1, XIAP, and c-Myc. CDK9-IN-45 can be used for research on colorectal cancer.
    CDK9-IN-45
  • HY-111886
    KHS108-MV1
    		Antagonist
    KHS108-MV1 is a conjugate of KHS108 and MV1. KHS108 is a ligand for TACC3. MV1 is an IAP antagonist that binds to cIAP1, cIAP2, and XIAP. KHS108-MV1 can be used in the research of breast cancer and fibrosarcoma.
    KHS108-MV1
  • HY-12440
    HM90822
    		Antagonist
    HM90822 is an orally active IAP antagonist. HM90822 induces ubiquitination and proteasome-dependent degradation of XIAP, cIAP1 and cIAP2 in sensitive pancreatic cancer cells. HM90822 induces Apoptotic cell death. HM90822 inhibits tumor growth in Panc-1 pancreatic cancer xenograft and orthotopic mouse models. HM90822 can be used for the research of pancreatic cancer.
    HM90822
  • HY-179633
    ZLMT-72
    		Inhibitor
    ZLMT-72 is an orally active dual CDK2 and CDK9 inhibitor with IC50s of 0.741 nM and 1.03 nM, respectively. ZLMT-72 shows good selectivity in kinase profiling andcholinesterase inhibition activity. ZLMT-72 has strong antiproliferative effects in the colorectal cancer (CRC) cell line HCT116 (GI50 < 0.1 nM). ZLMT-72 induces apoptosis by inhibiting thephosphorylation of retinoblastoma and RNA polymerase II, resulting in downregulation of antiapoptotic proteins (Mcl-1 and XIAP). ZLMT-72 can be used for the study of colorectal cancer (CRC).
    ZLMT-72
  • HY-181531
    IAP ligand 7
    		Ligand
    IAP ligand 7 is an E3 ligase ligand. IAP ligand 7 can be conjugated with TEAD ligand (HY-181595) and linker (HY-181608) to synthesize PROTAC TEAD/IAP degrader-1 (HY-181594) .
    IAP ligand 7
  • 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.
    Anticancer agent 127
  • HY-181534
    PROTAC TEAD1/IAP degrader-1
    		Degrader
    PROTAC TEAD1/IAP degrader-1 (Compound A232) is a selective TEAD1 and cIAP1 PROTAC degrader, with DC50 values of 14 nM and 270 nM, respectively. PROTAC TEAD1/IAP degrader-1 promotes the ubiquitination and degradation of TEAD1 and cIAP1. PROTAC TEAD1/IAP degrader-1 downregulates the expression of the TEAD-dependent gene CTGF. PROTAC TEAD1/IAP degrader-1 exhibits anticancer activity against mesothelioma.
    PROTAC TEAD1/IAP degrader-1
  • HY-155294
    SM-122
    		Degrader
    SM-122 is a monovalent Smac mimetic targeting cellular inhibitor of apoptosis protein (cIAP)-1/2. SM-122 can induce cIAP-1/2 degradation and weakly induce apoptosis in tumor cells. SM-122 can be used for the research of cancer, such as breast cancer.
    SM-122
  • HY-181018
    Topo I/DDX5-IN-1
    		Inhibitor
    Topo I/DDX5-IN-1 (Compound A10) is a Topo I and DDX5 inhibitor. Topo I/DDX5-IN-1 inhibits Topo I activity, binds to DDX5, and suppresses DDX5 function. Topo I/DDX5-IN-1 increases expression of γ-H2AX and p21, suppresses the expression of antiapoptotic proteins (Bcl-2 and XIAP), stimulates ROS generation, and triggers Apoptosis. Topo I/DDX5-IN-1 exhibits anticancer activity against pancreatic cancer, non-small cell lung cancer, skin cancer, and colorectal cancer.
    Topo I/DDX5-IN-1
  • HY-175445
    GNE-5472
    		Antagonist
    GNE-5472 is a potent bifunctional ERα PRRTAC degrader, with its E3 ligand being a pan-IAP antagonist. GNE-5472 antagonizes cIAP1/2, activating the non-classical NF-κB pathway, resulting in a significant upregulation of TNFα expression. GNE-5472 inhibits the proliferation of breast cancer cells and induces cell apoptosis. GNE-5472 can be used for the study of breast cancer.
    GNE-5472
  • 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-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.
    LBW242
  • HY-175444
    XIAP ligand-Linker Conjugate 1
    		Antagonist
    XIAP ligand-Linker Conjugate 1 is an E3 ligase ligand-linker conjugate that incorporates the XIAP BIR2 ligand XB2M54 (HY-175348) and linker. XIAP ligand-Linker Conjugate 1 can be used for synthesis of PROTAC ERα Degrader-1 (HY-112098).
    XIAP ligand-Linker Conjugate 1
  • HY-181590
    PROTAC TEAD1/IAP degrader-3
    		Degrader
    PROTAC TEAD1/IAP degrader-3 is a TEAD1/IAP PROTAC degrader. PROTAC TEAD1/IAP degrader-3 recruits the cIAP1 and XIAP E3 ligases to form a ternary complex, drives proteasomal degradation of TEAD1, and triggers autoubiquitination and proteasomal degradation of cIAP1. PROTAC TEAD1/IAP degrader-3 inhibits cell proliferation. PROTAC TEAD1/IAP degrader-3 regulates Hippo pathway activity by downregulating CTGF gene expression in a TEAD-dependent manner. PROTAC TEAD1/IAP degrader-3 is applicable to the research of mesothelioma.
    PROTAC TEAD1/IAP degrader-3
  • 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-134844
    Ciapavir
    		Degrader
    Ciapavir (SBI-0953294) is a HIV-1 latency-reversing agent. Ciapavir reverses latent HIV-1 reservoir in vitro and in vivo without inducing systemic T cell activation or broad cytokine release. Ciapavir degrades cIAP1 and activates non-canonical NF-κB pathway. Ciapavir can be used for the research of HIV-1 infection.
    Ciapavir
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
IAP Isoform Comparison

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