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5.33657

Sigma-Aldrich

PI4KIIIβ Inhibitor, BF738735

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Synonym(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
Empirical Formula (Hill Notation):
C21H19FN4O3S
CAS Number:
Molecular Weight:
426.46
UNSPSC Code:
12352200
NACRES:
NA.77

Assay

≥98% (HPLC)

Quality Level

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

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

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

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