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BF738735

Catalog No. T16530   CAS 1436383-95-7

BF738735 is a selective inhibitor of phosphatidylinositol 4-kinase III beta (PI4KIIIβ, IC50 = 5.7 nM) showing higher activity over α(IC50 = 1.7 μM). BF738735 exhibits a broad spectrum of antiviral activity.

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BF738735 Chemical Structure
BF738735, CAS 1436383-95-7
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2 mg In stock $ 57.00
5 mg In stock $ 89.00
10 mg In stock $ 155.00
25 mg In stock $ 339.00
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1 mL * 10 mM (in DMSO) In stock $ 97.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description BF738735 is a selective inhibitor of phosphatidylinositol 4-kinase III beta (PI4KIIIβ, IC50 = 5.7 nM) showing higher activity over α(IC50 = 1.7 μM). BF738735 exhibits a broad spectrum of antiviral activity.
Targets&IC50 PI4KIIIα:1.7 μM, PI4KIIIβ:5.7 nM
In vitro BF738735 effectively inhibits all viruses tested, with EC50s ranging between 4 and 71 nM. The cytotoxicity of BF738735, determined in parallel with the EC50 and using the same culture conditions for 3 to 4 days, is low, with CC50 values ranging from 11 to 65 μM, resulting in high selectivity indices. BF738735 exhibits a broad spectrum of antiviral activity, as it inhibits all tested species of enteroviruses and rhinoviruses, with 50% effective concentrations ranging between 4 and 71 nM. BF738735 also impairs PI4KIIIα, but only at an ~300-fold-higher concentration (IC50 of 1.7 μM). The activity of BF738735 is analyzed on a set of 150 cellular kinases, including 13 lipid kinases at a concentration of 10 μM. For all kinases, the inhibition is less than 10%, indicating that BF738735 specifically inhibits PI4KIIIβ in vitro. Low concentrations of BF738735 decrease the amount of luciferase to GuaHCl-treated levels, suggesting that the BF738735 blocks viral RNA replication. The EC50 of BF738735 in this assay is 77 nM, which is comparable to the inhibition observed in the multicycle assay for coxsackievirus serotype B3 (CVB3)[1].
In vivo BF738735 demonstrates favorable tolerability in test subjects, achieving effective plasma concentrations of the antiviral. Notably, a complete inhibition of the target activity is achieved at a dosage of 25 mg/kg, while a partial inhibition is observed with a 5 mg/kg dose[2].
Molecular Weight 426.46
Formula C21H19FN4O3S
CAS No. 1436383-95-7

Storage

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

Solubility Information

DMSO: 125 mg/mL (293.11 mM), Sonication is recommended.

TargetMolReferences and Literature

1. V Saarnio. Antiviral Molecules of Enteroviruses. 13.1.2017. 2. van der Schaar HM, et al. A novel, broad-spectrum inhibitor of enterovirus replication that targets host cell factor phosphatidylinositol 4-kinase IIIβ. Antimicrob Agents Chemother. 2013 Oct;57(10):4971-81.

Related compound libraries

This product is contained In the following compound libraries:
Kinase Inhibitor Library Inhibitor Library Anti-Liver Cancer Compound Library Anti-Cancer Compound Library Neuronal Differentiation Compound Library Anti-Prostate Cancer Compound Library Anti-Lung Cancer Compound Library Metabolism Compound Library Glycolysis Compound Library Anti-Obesity Compound Library

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Keywords

BF738735 1436383-95-7 Immunology/Inflammation PI3K/Akt/mTOR signaling Antiviral PI4K Phosphatidylinositol 4 kinases Inhibitor PI4 kinases BF-738735 inhibit Reverse Transcriptase BF 738735 inhibitor

 

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