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MOMIPP is an inhibitor of PIKfyve (IC50 = 5.05 nM).1 It selectively binds to PIKfyve over phosphatidylinositol 4-phosphate 5-kinase type-1 γ (PIP5K1C; Kds = 5.3 and >15,000 nM, respectively). MOMIPP (10 µM) induces vacuolization and cell lysis, markers of methuosis, and decreases the extracellular acidification rate (ECAR), indicating inhibition of glycolytic flux, but not the oxygen consumption rate (OCR), in U251 glioblastoma cells.2 Intraperitoneal administration of MOMIPP (80 mg/kg) decreases tumor growth in a U251 orthotopic mouse xenograft model.
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1. Indolyl-
2. The JNK signaling pathway plays a key role in methuosis (non-