Product Name

SMI481

General description

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.

Synonym

(4-Chloro-3-nitrophenyl)(4-(2-fluorophenyl)piperazin-1-yl)methanone, 1-(4-Chloro-3-nitrobenzoyl)-4-(2-fluorophenyl)-piperazine, SID: 164348711

Purity

≥98.0%(HPLC)

CAS Number

432020-20-7

Formula

C¹⁷H¹⁵ClFN³O³

Molecular Weight

363.77

Suitability

BioReagent, suitable for cell culture, etc.

l  Physical and Chemical Information

Appearance

White to beige Solid

Solubility(25℃)

DMSO

~5mg/mL

l  Biological Information

Biochem/Physiol   Actions

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.

l  Storage

Storage temp.

-20℃

l  Precautions and Disclaimer

This product is for R&D use only, not for drug, household, or other uses.

l  References

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov