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Cat. No. Product Name CAS No. Information
PC-60991

AS2677131

2171502-44-4

AS2677131(AS 2677131, AS-2677131) is a novel potent, oral PIKfyve inhibitor that selectively decreases c-Rel binding to gene promoters of IL-12p40 and IL-1β, regulates cytokine production through PIKfyve-c-Rel pathway ( IL-12p40 IC50=4 nM); inhibits the production of IL-12p40, IL-6 and IL-1β but not TNFα in activated macrophages or dendritic cells, and expression of IgM-induced MHC class II on B cells; reduces Akt phosphorylation in IFNγ/LPS-stimulated RAW264.7 cells, greatly increases cell size with many small vesicles in the cytoplasm.

PC-43409

YM-201636

371942-69-7 YM-201636 is a potent, selective PIKfyve inhibitor with IC50 of 33 nM, does not inhibits type Iiγ/Iα PtdInsP kinases even at 10 uM (p110α IC50=3.3 uM); shows insensitivity against yeast orthologue of PIKfyve, Fab1; significantly decreases the production of PtdIns(3,5)P2 by 80% in serum-starved NIH3T3 cells with no effect on serum-stimulated PKB Ser 473 phosphorylation at 0.8 uM; inhibits basal and insulin-activated 2-deoxyglucose uptake withIC50 of 54 nM; significantly reduces retroviruses budding from cells; blocks the continuous recycling of the tight junction proteins claudin-1 and claudin-2 in MDCK cells.
PC-60992

AS2795440

A novel potent, selective, oral PIKfyve inhibitor that selectively decreases c-Rel binding to gene promoters of IL-12p40 and IL-1β, regulates cytokine production through PIKfyve-c-Rel pathway ( IL-12p40 IC50=2 nM); inhibits the production of IL-12p40, IL-6 and IL-1β but not TNFα in activated macrophages or dendritic cells, and expression of IgM-induced MHC class II on B cells; reduces Akt phosphorylation in IFNγ/LPS-stimulated RAW264.7 cells, greatly increases cell size with many small vesicles in the cytoplasm; prevents the development of arthritis in rats.
PC-60412

Apilimod

541550-19-0 A potent IL-12/IL-23 inhibitor that down-regulates both IL-12 p35 and IL-12/IL-23 p40 at the transcriptional level, and inhibits the production of both IL-12 and IL-23 cytokines (IC50=2 nM); suppresses Th1 but not Th2 immune response in mice; binds to PIKfyve and blocks its phosphotransferase activity (IC50=14 nM), has no activity on PIP4K, PIP5K, mTOR, PI3K and PI4K isoforms; also potently blocks infections by EBOV and MARV in Huh 7, Vero E6 and primary human macrophage cells with IC50 of 10 nM.

Blood Cancer

Phase 2 Clinical

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