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SMI481

Catalog No. T26195   CAS 432020-20-7
Synonyms: NPPM-6748-481, NPPM 6748-481, NPPM6748481, SMI-481 SMI 481, NPPM 6748481

SMI481 (NPPM6748481) is the first small-molecule Sec14-like phosphatidylinositol transfer proteins (PITPs) inhibitor.

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SMI481 Chemical Structure
SMI481, CAS 432020-20-7
Pack Size Availability Price/USD Quantity
5 mg In stock $ 39.00
10 mg In stock $ 64.00
25 mg In stock $ 98.00
50 mg In stock $ 155.00
100 mg In stock $ 228.00
500 mg In stock $ 573.00
1 mL * 10 mM (in DMSO) In stock $ 51.00
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Purity: 99.54%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description SMI481 (NPPM6748481) is the first small-molecule Sec14-like phosphatidylinositol transfer proteins (PITPs) inhibitor.
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.
Synonyms NPPM-6748-481, NPPM 6748-481, NPPM6748481, SMI-481 SMI 481, NPPM 6748481
Molecular Weight 363.77
Formula C17H15ClFN3O3
CAS No. 432020-20-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 55 mg/mL (151.19 mM), Sonication is recommended.

TargetMolReferences and Literature

1. Nile AH, Tripathi A, Yuan P, Mousley CJ, Suresh S, Wallace IM, Shah SD, Pohlhaus DT, Temple B, Nislow C, Giaever G, Tropsha A, Davis RW, St Onge RP, Bankaitis VA. PITPs as targets for selectively interfering with phosphoinositide signaling in cells. Nat Chem Biol. 2014 Jan;10(1):76-84. doi: 10.1038/nchembio.1389. Epub 2013 Nov 24. PubMed PMID: 24292071; PubMed Central PMCID: PMC4059020.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Bioactive Compounds Library Max NO PAINS Compound Library Bioactive Compound Library

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Keywords

SMI481 432020-20-7 Others NPPM-6748-481 NPPM 6748-481 Inhibitor NPPM6748481 SMI-481 SMI481 SMI-481 SMI 481 SMI-481 SMI-481 NPPM-6748481 SMI-481 NPPM 6748481 SMI 481 inhibit inhibitor

 

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