| S9706 |
OT-82
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OT-82 is a novel nicotinamide phosphoribosyltransferase (NAMPT) inhibitor with average IC50s of 13.03 nM in non-HP cancer cells and 2.89 nM in HP cancer cells, respectively.
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Molecular Cancer, May 16, 2024, 105
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Nat Commun, 2025, 16(1):2513
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bioRxiv, 2025, 2025.07.28.667284
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| S2799 |
FK866 (Daporinad)
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FK866 (Daporinad) effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase; Nampt) with IC50 of 0.09 nM in a cell-free assay. This compound triggers autophagy. Phase 1/2.
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Adv Sci (Weinh), 2025, 12(33):e06599
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J Neuroinflammation, 2025, 22(1):113
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Cell Commun Signal, 2025, 23(1):348
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| S8444 |
Padnarsertib (KPT-9274, ATG-019)
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Padnarsertib (KPT 9274) is an orally bioavailable small molecule that is a non-competitive dual inhibitor of PAK4 and NAMPT. It shows an IC50 of ~120 nM for NAMPT in a cell-free enzymatic assay.
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Cell Reports Medicine, January 08 2026, 102540
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Blood Advances, December 22 2025, Online ahead of print
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Clinical Cancer Research, April 15 2021, 2352-2366
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| S8117 |
GMX1778
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GMX1778 is a potent and specific inhibitor of nicotinamide phosphoribosyltransferase (NAMPT) with IC50 and Kd of < 25 nM and 120 nM, respectively. This compound induces programmed cell death with apoptotic features. Phase 1.
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Nat Commun, 2025, 16(1):2513
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Nature Communications, 2025, 2513
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bioRxiv, 2025, 2025.04.25.650475
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| S7316 |
STF-118804
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STF-118804 is a highly specific NAMPT inhibitor.
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Nat Commun, 2025, 16(1):2513
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PLoS One, 2025, 20(6):e0324443
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Cell Metab, 2022, S1550-4131(22)00453-3
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| S7968 |
P7C3
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P7C3 is a potent proneurogenic and neuroprotective chemical that targets NAMPT enzyme.
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Nat Commun, 2025, 16(1):2513
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Front Oncol, 2023, 13:1225220
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Frontiers in Oncology, 2023, 1225220
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| S6629 |
GNE-617
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GNE-617 is a highly potent inhibitor of NAMPT activity with an IC50 of 5 nM.
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Nat Commun, 2025, 16(1):2513
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Nature Communications, 2025, 2513
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Molecular Cancer Research, 2024, 973-988
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| S8980 |
SBI-797812
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SBI-797812 is a NAMPT activator which is structurally similar to active-site directed NAMPT inhibitors and blocks binding of these inhibitors to NAMPT. This compound turns NAMPT into a "super catalyst" that more efficiently generates nicotinamide mononucleotide.
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Biotechnol Prog, 2023, e3365.
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