| S6414 |
Apilimod (STA-5326)
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Apilimod is a potent and orally-available inhibitor of the cytokines interleukin-12 (IL-12) and interleukin-23 (IL-23) with the potential to treat certain autoimmune and inflammatory diseases. Apilimod (STA-5326) inhibits IL-12 with IC50 of 1 nM, 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs, human monocytes and mouse PBMCs, respectively. Apilimod (STA-5326) is also a cell permeable small molecule that specifically inhibits PIKfyve with IC50 of 14 nM.
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Nat Commun, 2025, 16(1):8123
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Nat Commun, 2025, 16(1):6397
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J Cell Biol, 2025, 224(6)e202408158
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| S1219 |
YM201636
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YM201636 is a selective PIKfyve inhibitor with IC50 of 33 nM, less potent to p110α and insensitive to Fabl (yeast orthologue). This compound suppresses the growth of liver cancer via the induction of autophagy.
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Mol Biol Cell, 2024, 35(5):ar70
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Nat Commun, 2022, 13(1):2136
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Blood Cancer J, 2022, 12(3):39
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| S6912 |
Vacuolin-1
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Vacuolin-1 is a potent and cell-permeable inhibitor that blocks the Ca(2+)-dependent exocytosis of lysosomes and prevents the release of lysosomal content without affecting the process of resealing. This compound is also a potent and selective PIKfyve inhibitor, and inhibits autophagy by impairing lysosomal maturation via PIKfyve inhibition.
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Autophagy, 2025, 1-15.
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Virulence, 2024, 15(1):2350893
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Nat Commun, 2023, 14(1):3997
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| E2933 |
MOMIPP
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MOMIPP, a macropinocytosis inducer, is a PIKfyve inhibitor. This compound readily penetrates the blood-brain barrier and is moderately effective in suppressing progression of intracerebral glioblastoma xenografts.
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| S0785 |
Apilimod mesylate
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Apilimod mesylate is a potent and orally-available inhibitor of the cytokines interleukin-12 (IL-12) and interleukin-23 (IL-23) with the potential to treat certain autoimmune and inflammatory diseases. This compound inhibits IL-12 with IC50 of 1 nM, 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs, human monocytes and mouse PBMCs, respectively. It is also a cell permeable small molecule that specifically inhibits PIKfyve with IC50 of 14 nM.
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Cancer Research, 2025, 1479-1495
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bioRxiv, 2024, 2024.02.28.582543
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Stem Cell Reports, 2022, 17(2):397-412
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