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SMI481 is a selective small-molecule inhibitor (SMI) of the yeast phosphatidylinositol transfer protein (PITP) Sec14, a key regulator of phosphoinositide signaling, regulating membrane trafficking through the trans-Golgi network and endosomal systems. SMI481 has an IC50 value of 211 ± 19 nM in vitro against S. cerevisiae Sec14 (WT) in a phosphatidylinositol (PtdIns) transfer assay measuring exchange of PtdIns and phosphatidylcholine between membranes and inhibited Sec14-dependent growth of WT yeast with an IC50 of 2.87 ± 0.55 μM. SMI481′s activity is believed to involve binding in the Sec14 hydrophobic cavity, a new target for studying phosphoinositide signaling with more selectivity than that afforded by lipid kinase–directed strategies.
| Molecular Weight | 363.77 |
| Formula | C17H15ClFN3O3 |
| CAS Number | 432020-20-7 |
| Solubility (25°C) | DMSO: 5 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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