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ApoptosisIAP
IAP (Inhibitors of Apoptosis) is a family of functionally and structurally related proteins, which serve as endogenous inhibitors of programmed cell death (apoptosis). A common feature of all IAPs is the presence of a BIR in one to three copies. The human IAP family consists of 8 members, and IAP homologs have been identified in numerous organisms. The members of the IAPs included IAPs, Cp-IAP, Op-IAP, XIAP, c-IAPl, C-IAP2, NAIP, Livin and Survivin. The best characterized IAP is XIAP, which binds caspase-9, caspase-3 and caspase 7, thereby inhibiting their activation and preventing apoptosis. Also cIAP1 and cIAP2 have been shown to bind caspases, although how the IAPs inhibit apoptosis mechanistically at the molecular level is not completely understood.
SM-164
Cited
T12932L957135-43-2
SM-164 binds to XIAP protein containing both the BIR2 and BIR3 domains (IC50: 1.39 nM). It acts as an extremely potent antagonist of XIAP.
- $119
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CitedSe-Methylselenocysteine
T772726046-90-2
Se-Methylselenocysteine (Se-MSC) is a potent chemopreventive agent in many test systems and has been shown to inhibit tumor promotion and induce apoptosis.
- $39
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LCL161
Cited
T20801005342-46-0
LCL161 is a SMAC mimetic, an IAP antagonist with oral activity that inhibits XIAP (IC50=35 nM) in HEK293 cells and also inhibits cIAP1 (IC50=0.4 nM) in MDA-MB-231 cells. LCL161 has potential antitumor activity.
- $63
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CitedBirinapant Cited
T60071260251-31-7
Birinapant (TL32711) is a synthetic small molecule that is both a peptidomimetic of second mitochondrial-derived activator of caspases (SMAC) and inhibitor of IAP (Inhibitor of Apoptosis Protein) family proteins, with potential antineoplastic activity.
- $41
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CitedAcacetin Cited
T3981480-44-4
Acacetin (5,7-Dihydroxy-4'-methoxyflavone) is an O-methylated flavone found in various plants, exhibiting antinociceptive, anti-inflammatory, and antioxidant activities in different research models.
- $30
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CitedHM90822
T708681363145-46-3In house
HM90822 is a novel synthetic apoptotic protein (IAP) antagonist that induces apoptosis in human pancreatic cancer cells through proteasome-dependent degradation of IAPs containing the BIR2 3 structural domain.HM90822 inhibits the expression of XIAP and cIAP1 2 proteins in HM822-sensitive Panc-1 and BxPC-3 cells, induces ubiquitylation of IAPs and promotes induces IAP ubiquitination and promotes proteasome-dependent IAP degradation.
- $613
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Xevinapant
T67631071992-99-8
Xevinapant (Debio-1143) is a potent Smac mimetic and an antagonist of IAP (inhibitor of apoptosis protein via E3 ubiquitin ligase), binding to XIAP-BIR3, cIAP1-BIR3 and cIAP2-BIR3 with Ki of 66.4 nM, 1.9 nM, and 5.1 nM, 50- to 100-fold higher affinities than the Smac AVPI peptide. Phase 1.
- $36
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BV6 Cited
T64281001600-56-1
BV6 is an antagonist of c-IAP1 and XIAP, members of the inhibitors of apoptosis (IAP) family.
- $44
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CitedN-Deshydroxyethyl Dasatinib
T18750910297-51-7
N-Deshydroxyethyl Dasatinib (N-Deshydroxyethyl BMS-354825) is a metabolite of Dasatinib, a dasatinib-based molecule that degrades ABL by binding to the IAP ligand via a linker to form SNIPER. N-Deshydroxyethyl Dasatinib is used in the study of cancer and immune diseases.
- $84
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Polygalacin D Cited
TN209166663-91-0
Polygalacin D shows anti- proliferation, anti-inflammary, and hepatoprotective activities, it can inhibit the expression of lipopolysaccharide (LPS)-induced iNOS and COX-2 protein and mRNA without an appreciable cytotoxic effect on RAW 264.7 macrophages, and can suppress induction by LPS of pro-inflammatory cytokines such as prostaglandin E2 (PGE2).
- $123
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CitedEmbelin Cited
T6485550-24-3
Embelin (Embelic acid), isolated from the Japanese Ardisia herb, is an inhibitor of the X-linked inhibitor of apoptosis (IC50: 4.1 uM).
- $50
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CitedPhenoxodiol
T1652281267-65-4
Phenoxodiol (Idronoxil) activates the mitochondrial caspase system, inhibits X-linked inhibitor of apoptosis(XIAP), disrupts FLICE inhibitory protein(FLIP) expression, and sensitizes the cancer cells to Fas-mediated apoptosis. Phenoxodiol induces cell cycle arrest in the G1 S phase of the cell cycle and upregulates p21WAF1 via a p53 independent manner. Phenoxodiol also inhibits DNA topoisomerase II.
- $60
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CUDC-427
T150181446182-94-0
CUDC-427 (GDC-0917) is an orally bioactive and pan antagonist of inhibitor of apoptosis proteins(IAPs). CUDC-427 can be used in research on cancers.
- $42
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AZD5582 TFA
T36201L
AZD5582 TFA is a potent IAP antagonist that binds to the BIR3 domain of cIAP1, cIAP2, and XIAP with IC50 values of 15, 21, and 15 nM, respectively.AZD5582 TFA induces apoptosis.
- $50
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ASTX660
TQ00291799328-86-1
Tolinapant (ASTX660) is an orally bioavailable cIAP1 2 and XIAP antagonist that induces expression of immunogenic cell death (ICD) markers in sensitive HNSCC cell lines in vitro.
- $76
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AZD5582
T143781258392-53-8
AZD5582 is an inhibitor of IAPs, which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC50s of 15, 21, and 15 nM, respectively. It induces apoptosis.
- $49
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MX69
T36531005264-47-0
MX69 is the MDM2 XIAP inhibitor, blocking the MDM2 protein-XIAP RNA interaction, leading to MDM2 degradation.
- $31
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1-[2,4-Dihydroxy-6-methoxy-3-(3-methyl-2-buten-1-yl)phenyl]-3-(4-hydroxyphenyl)-2-propen-1-one
TN5263569-83-5
1-[2,4-Dihydroxy-6-methoxy-3-(3-methyl-2-buten-1-yl)phenyl]-3-(4-hydroxyphenyl)-2-propen-1-one (Xanthohumol) , prenylchacone flavonoid, is a natural product with multi-biofunctions purified from Hops Humulus lupulus,is effective against HIV-1 and might serve as an interesting lead compound. It may represent a novel chemotherapeutic agent for HIV-1 infection.
- $36
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AZD5582 acetate (1258392-53-8 free base) Cited
T14378L
AZD5582 acetate is an inhibitor of IAPs, which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC50s of 15, 21, and 15 nM, respectively. AZD5582 induces apoptosis.
- $89
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CitedSM-164 Hydrochloride (957135-43-2 free base)
T12932
SM-164 Hydrochloride is a cell-permeable Smac mimetic compound. SM-164 binds to XIAP protein containing both the BIR2 and BIR3 domains(IC50 value of 1.39 nM) and functions as an extremely potent antagonist of XIAP.
- $266
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Anticancer agent 127
T792472410953-19-2
Anticancer agent 127 (142D6), an IAP inhibitor, covalently binds to the BIR3 domains of XIAP, cIAP1, and cIAP2, with IC50 values of 12 nM, 14 nM, and 9 nM, respectively, demonstrating anticancer effects [1].
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Xevinapant hydrochloride
T32991071992-57-8
Xevinapant hydrochloride (AT-406 HCl) , an orally active antagonist of multiple inhibitor of apoptosis proteins(IAP), inhibits progression of human ovarian Y binding to XIAP-BIR3, cIAP1-BIR3 and cIAP2-BIR3 with Ki of 66.4 nM, 1.9 nM, and 5.1 nM, 50- to 100-fold higher affinities than the Smac AVPI peptide.
- $35
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Anticancer agent 128
T792482941243-62-3
Anticancer agent 128 (compound 1) is an IAP inhibitor that covalently binds to the BIR3 domains of XIAP, cIAP1, and cIAP2, showing IC50 values of 24.9 nM, 19.3 nM, and 10.3 nM, respectively [1].
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