| S7015 |
Birinapant (TL32711)
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Birinapant is a SMAC mimetic antagonist, mostly to cIAP1 with Kd of <1 nM in a cell-free assay, less potent to XIAP. This compound helps to induce apoptosis in latent HIV-1-infected cells. Phase 2.
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Cell, 2025, S0092-8674(25)01233-4
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Nat Commun, 2025, 16(1):7360
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EMBO Mol Med, 2025, 10.1038/s44321-025-00201-x
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| S7597 |
BV6
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BV-6 is a SMAC mimetic, dual cIAP and XIAP inhibitor.
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Nature, 2025, 647(8090):735-746
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Nat Commun, 2025, 16(1):4919
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EMBO J, 2025, 10.1038/s44318-025-00561-7
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| S2754 |
Xevinapant (AT406)
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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.
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Nat Commun, 2025, 16(1):2572
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Cell Death Dis, 2025, 16(1):476
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bioRxiv, 2025, 2025.09.22.677496
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| S7010 |
GDC-0152
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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.
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J Exp Clin Cancer Res, 2024, 43(1):311
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Nat Commun, 2023, 14(1):1461
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Cell Rep, 2023, 42(1):111965
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| S7089 |
SM-164
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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. This compound induces apoptosis and tumor regression.
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Nature, 2025, 10.1038/s41586-025-09741-1
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EMBO J, 2025, 10.1038/s44318-025-00412-5
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J Virol, 2025, 99(3):e0198024
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| S7362 |
AZD5582
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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
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EMBO J, 2025, 10.1038/s44318-025-00412-5
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Cell Rep, 2024, 43(7):114400
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Cell Death Dis, 2023, 14(9):599
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| S8681 |
Tolinapant (ASTX660)
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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.
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Cell Death Differ, 2024, 31(10):1318-1332
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Cell Death Differ, 2024, 10.1038/s41418-024-01316-3
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bioRxiv, 2024, 2024.12.12.628190
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