IAP

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IAP製品

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  • IAP阻害剤 (9)
  • IAP拮抗剤(5)
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製品コード 製品名称 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1130 Sepantronium Bromide (YM155) Sepantronium Bromide(YM155) is a potent survivin suppressant by inhibiting Survivin promoter activity with IC50 of 0.54 nM in HeLa-SURP-luc and CHO-SV40-luc cells; does not significantly inhibit SV40 promoter activity, but is observed to slightly inhibit the interaction of Survivin with XIAP. YM155 down-regulates survivin and XIAP, modulates autophagy and induces autophagy-dependent DNA damage in breast cancer cells. Phase 2.
Adv Sci (Weinh), 2023, 10(25):e2301753
Cell Rep Med, 2023, 4(12):101339
Proc Natl Acad Sci U S A, 2023, 120(4):e2218118120
S7015 Birinapant Birinapant is a SMAC mimetic antagonist, mostly to cIAP1 with Kd of <1 nM in a cell-free assay, less potent to XIAP. Birinapant helps to induce apoptosis in latent HIV-1-infected cells. Phase 2.
Cell Death Dis, 2024, 15(1):77
Cell Discov, 2023, 9(1):7
Cancer Res, 2023, 83(19):3284-3304
S7597 BV-6 BV-6 is a SMAC mimetic, dual cIAP and XIAP inhibitor.
Cell Rep Med, 2024, 5(1):101377
Viruses, 2024, 16(2)290
Nature, 2023, 619(7969):371-377
S7009 LCL161 LCL-161, a small molecule second mitochondrial activator of caspase (SMAC) mimetic, potently binds to and inhibits multiple IAPs (i.e. XIAP, c-IAP).
Nat Commun, 2023, 14(1):1461
Pharmacol Res, 2023, 189:106697
Int Immunopharmacol, 2023, 117:109974
S2754 Xevinapant (AT406) Xevinapant (AT406, ARRY-334543, Debio1143, SM-406) 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.
Cells, 2023, 12(12)1653
Cells, 2023, 12(12)1653
Heliyon, 2023, 9(10):e20655
S7010 GDC-0152 GDC-0152 is a potent antagonist of XIAP-BIR3, ML-IAP-BIR3, cIAP1-BIR3 and cIAP2-BIR3 with Ki of 28 nM, 14 nM, 17 nM and 43 nM in cell-free assays, respectively; less affinity shown to cIAP1-BIR2 and cIAP2-BIR2. Phase 1.
Nat Commun, 2023, 14(1):1461
Cell Rep, 2023, 42(1):111965
Cell Death Dis, 2020, 11(8):680
S7362 AZD5582 AZD5582, a novel small-molecule IAP inhibitor, binds potently to the BIR3 domains of cIAP1, cIAP2, and XIAP with IC50 values of 15, 21, and 15 nM. AZD5582 induces apoptosis.
Cell Death Dis, 2023, 14(9):599
Cell Death Dis, 2023, 14(9):599
Heliyon, 2023, 9(10):e20655
S7089 SM-164 SM-164 is a potent, non-peptide, cell-permeable antagonist of XIAP that targets both the BIR2 and BIR3 domains with IC50 of 1.39 nM. SM-164 induces apoptosis and tumor regression.
Microbiol Spectr, 2024, 12(1):e0275823
EMBO J, 2023, e113490.
Cell Death Dis, 2023, 14(9):599
S7025 Embelin Embelin (Embelic Acid, NSC 91874), a quinone isolated from the Japanese Ardisia herb, is an inhibitor of X-linked inhibitor of apoptosis (XIAP) with IC50 of 4.1 μM in a cell-free assay.
Heliyon, 2023, 9(3):e14006
Cancers (Basel), 2021, 13(14)3585
Cell Host Microbe, 2018, 24(5):689-702
S8681 Tolinapant (ASTX660) Tolinapant (ASTX660) is a potent, non-peptidomimetic antagonist of cIAP1/2 and XIAP that inhibits the interactions between a SMAC-derived peptide and the BIR3 domains of XIAP (BIR3-XIAP) and cIAP1 (BIR3-cIAP1) with IC50 values less than 40 and 12 nmol/L, respectively.
Heliyon, 2023, 9(10):e20655
Heliyon, 2023, 9(10):e20655
Biochem Biophys Res Commun, 2022, 602:8-14
S5967 Berberine chloride hydrate Berberine (Natural Yellow 18) chloride hydrate is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.
Front Biosci (Landmark Ed), 2022, 27(8):242
Front Pharmacol, 2021, 12:632201
S9634 Phenoxodiol (Haginin E) Phenoxodiol (Haginin E, Idronoxil, Dehydroequol, NV 06, PXD) is an isoflavone analog with antineoplastic activity that activates the caspase system, inhibits XIAP (X-linked inhibitor of apoptosis), and disrupts FLICE inhibitory protein (FLIP) expression, resulting in tumor cell apoptosis. Phenoxodiol also inhibits DNA topoisomerase II.
Anticancer Res, 2018, 38(10):5709-5716
S2271 Berberine chloride Berberine chloride is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.
Adv Healthc Mater, 2023, e2300591.
Transl Oncol, 2023, 35:101712
J Biomol Struct Dyn, 2022, 1-11
S5600 Flavokawain A Flavokawain A, extracted from kava, is an apoptotic inducers and anticarcinogenic agent. Flavokawain A can down-regulation of antiapoptotic proteins, such as XIAP, survivin, and Bcl-xL, thereby changing the balance between apoptotic and antiapoptotic molecules and then induce cell death in tumor cells.
S1130 Sepantronium Bromide (YM155) Sepantronium Bromide(YM155) is a potent survivin suppressant by inhibiting Survivin promoter activity with IC50 of 0.54 nM in HeLa-SURP-luc and CHO-SV40-luc cells; does not significantly inhibit SV40 promoter activity, but is observed to slightly inhibit the interaction of Survivin with XIAP. YM155 down-regulates survivin and XIAP, modulates autophagy and induces autophagy-dependent DNA damage in breast cancer cells. Phase 2.
Adv Sci (Weinh), 2023, 10(25):e2301753
Cell Rep Med, 2023, 4(12):101339
Proc Natl Acad Sci U S A, 2023, 120(4):e2218118120
S7597 BV-6 BV-6 is a SMAC mimetic, dual cIAP and XIAP inhibitor.
Cell Rep Med, 2024, 5(1):101377
Viruses, 2024, 16(2)290
Nature, 2023, 619(7969):371-377
S7009 LCL161 LCL-161, a small molecule second mitochondrial activator of caspase (SMAC) mimetic, potently binds to and inhibits multiple IAPs (i.e. XIAP, c-IAP).
Nat Commun, 2023, 14(1):1461
Pharmacol Res, 2023, 189:106697
Int Immunopharmacol, 2023, 117:109974
S7362 AZD5582 AZD5582, a novel small-molecule IAP inhibitor, binds potently to the BIR3 domains of cIAP1, cIAP2, and XIAP with IC50 values of 15, 21, and 15 nM. AZD5582 induces apoptosis.
Cell Death Dis, 2023, 14(9):599
Cell Death Dis, 2023, 14(9):599
Heliyon, 2023, 9(10):e20655
S7025 Embelin Embelin (Embelic Acid, NSC 91874), a quinone isolated from the Japanese Ardisia herb, is an inhibitor of X-linked inhibitor of apoptosis (XIAP) with IC50 of 4.1 μM in a cell-free assay.
Heliyon, 2023, 9(3):e14006
Cancers (Basel), 2021, 13(14)3585
Cell Host Microbe, 2018, 24(5):689-702
S5967 Berberine chloride hydrate Berberine (Natural Yellow 18) chloride hydrate is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.
Front Biosci (Landmark Ed), 2022, 27(8):242
Front Pharmacol, 2021, 12:632201
S9634 Phenoxodiol (Haginin E) Phenoxodiol (Haginin E, Idronoxil, Dehydroequol, NV 06, PXD) is an isoflavone analog with antineoplastic activity that activates the caspase system, inhibits XIAP (X-linked inhibitor of apoptosis), and disrupts FLICE inhibitory protein (FLIP) expression, resulting in tumor cell apoptosis. Phenoxodiol also inhibits DNA topoisomerase II.
Anticancer Res, 2018, 38(10):5709-5716
S2271 Berberine chloride Berberine chloride is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.
Adv Healthc Mater, 2023, e2300591.
Transl Oncol, 2023, 35:101712
J Biomol Struct Dyn, 2022, 1-11
S5600 Flavokawain A Flavokawain A, extracted from kava, is an apoptotic inducers and anticarcinogenic agent. Flavokawain A can down-regulation of antiapoptotic proteins, such as XIAP, survivin, and Bcl-xL, thereby changing the balance between apoptotic and antiapoptotic molecules and then induce cell death in tumor cells.
S7015 Birinapant Birinapant is a SMAC mimetic antagonist, mostly to cIAP1 with Kd of <1 nM in a cell-free assay, less potent to XIAP. Birinapant helps to induce apoptosis in latent HIV-1-infected cells. Phase 2.
Cell Death Dis, 2024, 15(1):77
Cell Discov, 2023, 9(1):7
Cancer Res, 2023, 83(19):3284-3304
S2754 Xevinapant (AT406) Xevinapant (AT406, ARRY-334543, Debio1143, SM-406) 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.
Cells, 2023, 12(12)1653
Cells, 2023, 12(12)1653
Heliyon, 2023, 9(10):e20655
S7010 GDC-0152 GDC-0152 is a potent antagonist of XIAP-BIR3, ML-IAP-BIR3, cIAP1-BIR3 and cIAP2-BIR3 with Ki of 28 nM, 14 nM, 17 nM and 43 nM in cell-free assays, respectively; less affinity shown to cIAP1-BIR2 and cIAP2-BIR2. Phase 1.
Nat Commun, 2023, 14(1):1461
Cell Rep, 2023, 42(1):111965
Cell Death Dis, 2020, 11(8):680
S7089 SM-164 SM-164 is a potent, non-peptide, cell-permeable antagonist of XIAP that targets both the BIR2 and BIR3 domains with IC50 of 1.39 nM. SM-164 induces apoptosis and tumor regression.
Microbiol Spectr, 2024, 12(1):e0275823
EMBO J, 2023, e113490.
Cell Death Dis, 2023, 14(9):599
S8681 Tolinapant (ASTX660) Tolinapant (ASTX660) is a potent, non-peptidomimetic antagonist of cIAP1/2 and XIAP that inhibits the interactions between a SMAC-derived peptide and the BIR3 domains of XIAP (BIR3-XIAP) and cIAP1 (BIR3-cIAP1) with IC50 values less than 40 and 12 nmol/L, respectively.
Heliyon, 2023, 9(10):e20655
Heliyon, 2023, 9(10):e20655
Biochem Biophys Res Commun, 2022, 602:8-14

IAP阻害剤の選択性比較

Tags: IAP inhibitor|IAP agonist|IAP activator|IAP inducer|IAP antagonist|IAP signaling pathway|IAP assay kit