| S7009 |
LCL161
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LCL-161, a small molecule second mitochondrial activator of caspase (SMAC) mimetic, potently binds to and inhibits multiple IAPs (i.e. XIAP, c-IAP).
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Immunity, 2025, 58(4):961-979.e8
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Nat Commun, 2025, 16(1):4919
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EMBO Mol Med, 2025, 10.1038/s44321-025-00201-x
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| S1130 |
Sepantronium Bromide (YM155)
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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. It does not significantly inhibit SV40 promoter activity, but is observed to slightly inhibit the interaction of Survivin with XIAP. This compound down-regulates survivin and XIAP, modulates autophagy and induces autophagy-dependent DNA damage in breast cancer cells. Phase 2.
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Cell Rep Med, 2025, S2666-3791(25)00102-8
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Biochim Biophys Acta Mol Basis Dis, 2025, 1871(3):167693
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Cancer Res Commun, 2025, 5(6):1018-1033
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| S2271 |
Berberine chloride
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Berberine chloride is a quaternary ammonium salt from the group of isoquinoline alkaloids. This compound activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. It decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. This chemical induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. It is a dual topoisomerase I and II inhibitor. It is also a potential autophagy modulator.
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J Cardiovasc Dev Dis, 2025, 12(7)278
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Adv Healthc Mater, 2023, e2300591.
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Transl Oncol, 2023, 35:101712
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| S7025 |
Embelin
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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.
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Heliyon, 2023, 9(3):e14006
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Cancers (Basel), 2021, 13(14)3585
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Cell Host Microbe, 2018, 24(5):689-702
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| S5967 |
Berberine chloride hydrate
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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.
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Front Biosci (Landmark Ed), 2022, 27(8):242
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Front Pharmacol, 2021, 12:632201
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| S9634 |
Phenoxodiol (Haginin E)
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Phenoxodiol (Haginin E, Idronoxil, Dehydroequol, NV 06, PXD) is an isoflavone analog with antineoplastic activity. It activates the caspase system, inhibits XIAP (X-linked inhibitor of apoptosis), and disrupts FLICE inhibitory protein (FLIP) expression, resulting in tumor cell apoptosis. This compound also inhibits DNA topoisomerase II.
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Anticancer Res, 2018, 38(10):5709-5716
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| S5600 |
Flavokawain A
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Flavokawain A, extracted from kava, is an apoptotic inducers and anticarcinogenic agent. This compound 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.
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