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. |
-
Cell Commun Signal, 2024, 22(1):440
-
Sci Rep, 2024, 14(1):7604
-
Adv Sci (Weinh), 2023, 10(25):e2301753
|
|
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 Differ, 2024, 31(10):1318-1332
-
Cell Death Differ, 2024, 10.1038/s41418-024-01316-3
-
Cancer Res, 2024, 84(15):2432-2449
|
|
S7597 |
BV-6
|
BV-6 is a SMAC mimetic, dual cIAP and XIAP inhibitor.
|
-
Cell Rep Med, 2024, 5(1):101377
-
Cell Death Differ, 2024, 10.1038/s41418-024-01301-w
-
Cell Rep, 2024, 43(9):114728
|
|
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). |
-
Cell Death Dis, 2024, 15(8):592
-
Cell Death Dis, 2024, 15(4):255
-
Cell Death Dis, 2024, 15(11):855
|
|
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. |
-
Cell Death Dis, 2024, 15(11):855
-
Cells, 2023, 12(12)1653
-
Cells, 2023, 12(12)1653
|
|
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 |
-
Cell Rep, 2024, 43(7):114400
-
Cell Death Dis, 2023, 14(9):599
-
Cell Death Dis, 2023, 14(9):599
|
|
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
-
J Biochem, 2024, mvae067
-
EMBO J, 2023, 42(9):e113490
|
|
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. |
-
Cell Death Differ, 2024, 31(10):1318-1332
-
Cell Death Differ, 2024, 10.1038/s41418-024-01316-3
-
Heliyon, 2023, 9(10):e20655
|
|
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. |
- Cell Commun Signal, 2024, 22(1):440
- Sci Rep, 2024, 14(1):7604
- Adv Sci (Weinh), 2023, 10(25):e2301753
|
|
S7597 |
BV-6
|
BV-6 is a SMAC mimetic, dual cIAP and XIAP inhibitor.
|
- Cell Rep Med, 2024, 5(1):101377
- Cell Death Differ, 2024, 10.1038/s41418-024-01301-w
- Cell Rep, 2024, 43(9):114728
|
|
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). |
- Cell Death Dis, 2024, 15(8):592
- Cell Death Dis, 2024, 15(4):255
- Cell Death Dis, 2024, 15(11):855
|
|
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 |
- Cell Rep, 2024, 43(7):114400
- Cell Death Dis, 2023, 14(9):599
- 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
|
|
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 Differ, 2024, 31(10):1318-1332
- Cell Death Differ, 2024, 10.1038/s41418-024-01316-3
- Cancer Res, 2024, 84(15):2432-2449
|
|
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. |
- Cell Death Dis, 2024, 15(11):855
- Cells, 2023, 12(12)1653
- Cells, 2023, 12(12)1653
|
|
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
- J Biochem, 2024, mvae067
- EMBO J, 2023, 42(9):e113490
|
|
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. |
- Cell Death Differ, 2024, 31(10):1318-1332
- Cell Death Differ, 2024, 10.1038/s41418-024-01316-3
- Heliyon, 2023, 9(10):e20655
|
|