SMI481

SKU: orb1305258

Description

SMI481 (NPPM6748481) is a novel, small-molecule inhibitor targeting Sec14-like phosphatidylinositol transfer proteins (PITPs). This compound is a valuable research tool for investigating PITP-mediated lipid signaling and membrane trafficking in cellular and biochemical studies, both in vitro and in vivo.

Key Properties

• CAS Number: 432020-20-7
• MW: 363.77
• Purity: 99.54% (May vary between batches)
• Formula: C₁₇H₁₅ClFN₃O₃
• SMILES: [O-][N+](=O)c1cc(ccc1Cl)C(=O)N1CCN(CC1)c1ccccc1F
• Target: Others
• Solubility: DMSO:55 mg/mL (151.19 mM)

Bioactivity

• In Vitro:
  Sec14-like phosphatidylinositol transfer proteins (PITPs) integrate diverse territories of intracellular lipid metabolism with stimulated phosphatidylinositol-4-phosphate production and are discriminating portals for interrogating phosphoinositide signaling. Yet, neither Sec14-like PITPs nor PITPs in general have been exploited as targets for chemical inhibition for such purposes. Herein, we validate what is to our knowledge the first small-molecule inhibitors (SMIs) of the yeast PITP Sec14. These SMIs are nitrophenyl(4-(2-methoxyphenyl)piperazin-1-yl)methanones (NPPMs) and are effective inhibitors in vitro and in vivo. We further establish that Sec14 is the sole essential NPPM target in yeast and that NPPMs exhibit exquisite targeting specificities for Sec14 (relative to related Sec14-like PITPs), propose a mechanism for how NPPMs exert their inhibitory effects and demonstrate that NPPMs exhibit exquisite pathway selectivity in inhibiting phosphoinositide signaling in cells. These data deliver proof of concept that PITP-directed SMIs offer new and generally applicable avenues for intervening with phosphoinositide signaling pathways with selectivities superior to those afforded by contemporary lipid kinase-directed strategies.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

NPPM 6748481, NPPM 6748-481, NPPM6748481, NPPM-6748481, NPPM-6748-481, SMI 481, SMI481, SMI-481, SMI-481 SMI 481, SMI-481 SMI481, SMI-481 SMI-481, phosphatidylinositol transfer proteins (PITPs)

Compound Identifiers

PubChem CID

1334619