5.33657

PI4KIIIβ Inhibitor, BF738735

• Synonyme(s) : PI4KIIIβ Inhibitor, BF738735, 2-Fluoro-4-(2-methyl-8-(3-(methylsulfonyl)benzylamino)imidazo[1,2-a]pyrazin-3-yl)phenol, Phosphatidylinositol-phosphate-4-Kinase III β Inhibitor, BF-738735
• Formule empirique (notation de Hill) : C₂₁H₁₉FN₄O₃S
• Numéro CAS: 1436383-95-7
• Poids moléculaire : 426.46
• MDL number: MFCD24702860
• NACRES: NA.77
• UNSPSC Code: 12352200
• Assay: ≥98% (HPLC)
• Form: powder
• Quality level: 100
• Storage condition: OK to freeze, protect from light

Propriétés

• assay: ≥98% (HPLC)
• Quality Level: 100
• form: powder
• potency: 5.7 nM IC₅₀
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: light gray
• solubility: DMSO: 50 mg/mL
• storage temp.: 2-8°C

Description

General description

A cell-permeable imidazo-pyrazine based compound that acts as a potent and reversible inhibitor of PI4KIIIβ (IC₅₀ = 5.7 nM). Displays excellent selectivity over PI4KIIIα (IC₅₀ = 1.7 µM) and several other lipid kinases (IC₅₀ >10 µM). Shown to dose-dependently decrease PI4P levels, reduce oxysterol-binding protein (OSBP) localization to replication organelles (ROs) and inhibit cholesterol shuttling to ROs (at 1 µM in BGM and HeLaR19 cells transfected with CVB3) at multiplicity of infection (MOI). Exhibits uniformly potent and broad spectrum antienteroviral activity across a wide range of species (EC₅₀ = 4-31 nM) and is inactive against RNA, DNA, and retroviruses.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
PI4KIII&beta

Reversible: yes

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Strating, J.R.P.M., et al. 2015. Cell Reports.10, 600.
MacLeod, A.M., et al. 2013. ACS Med. Chem. Lett.4, 585.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Informations sur la sécurité

• Classe de stockage: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable