BF738735

Name: BF738735
Brand: MedChemExpress
SKU: HY-U00426
Rating: 5.0 (3 reviews)

Cat. No.: HY-U00426 Purity: 99.10%: FAQs
Data Sheet SDS COA Handling Instructions

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BF738735 is a phosphatidylinositol 4-kinase III beta (PI4KIIIβ) inhibitor with an IC₅₀ of 5.7 nM.

For research use only. We do not sell to patients.

BF738735 Chemical Structure

CAS No. : 1436383-95-7

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 121	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 121	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 52	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 110	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 190	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 410	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Customer Review

Based on 3 publication(s) in Google Scholar

3 Publications Citing Use of MCE BF738735

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PI4KIIIβ PI4KIIIα PI4K PI4KII

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

BF738735 is a phosphatidylinositol 4-kinase III beta (PI4KIIIβ) inhibitor with an IC₅₀ of 5.7 nM.

IC₅₀ & Target^[1]

PI4KIIIβ

5.7 nM (IC₅₀)

PI4KIIIα

1.7 μM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	EC₅₀	31 nM Compound: 5, BF738735	Antienteroviral activity against Human rhinovirus 14 infected in human HeLa cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay Antienteroviral activity against Human rhinovirus 14 infected in human HeLa cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay	[PMID: 24900715]
HeLa	CC₅₀	61000 nM Compound: 5, BF738735	Cytotoxicity against human HeLa cells after 2 to 3 days by MTS assay Cytotoxicity against human HeLa cells after 2 to 3 days by MTS assay	[PMID: 24900715]
RD	EC₅₀	11 nM Compound: 5, BF738735	Antienteroviral activity against Enterovirus 71 infected in human RD cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay Antienteroviral activity against Enterovirus 71 infected in human RD cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay	[PMID: 24900715]
Vero	EC₅₀	13 nM Compound: 5, BF738735	Antienteroviral activity against poliovirus 2 infected in african green monkey Vero cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay Antienteroviral activity against poliovirus 2 infected in african green monkey Vero cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay	[PMID: 24900715]
Vero	EC₅₀	15 nM Compound: 5, BF738735	Antienteroviral activity against Coxsackievirus B3 infected in african green monkey Vero cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay Antienteroviral activity against Coxsackievirus B3 infected in african green monkey Vero cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay	[PMID: 24900715]
Vero	EC₅₀	19 nM Compound: 5, BF738735	Antienteroviral activity against poliovirus 1 infected in african green monkey Vero cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay Antienteroviral activity against poliovirus 1 infected in african green monkey Vero cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay	[PMID: 24900715]
Vero	EC₅₀	21 nM Compound: 5, BF738735	Antienteroviral activity against Coxsackievirus A9 infected in african green monkey Vero cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay Antienteroviral activity against Coxsackievirus A9 infected in african green monkey Vero cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay	[PMID: 24900715]
Vero	EC₅₀	5 nM Compound: 5, BF738735	Antienteroviral activity against poliovirus 3 infected in african green monkey Vero cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay Antienteroviral activity against poliovirus 3 infected in african green monkey Vero cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay	[PMID: 24900715]

In Vitro

BF738735 (Compound 1) strongly inhibits PI4KIIIβ activity in vitro, with an IC₅₀ of 5.7 nM. BF738735 also impairs PI4KIIIα, but only at an ~300-fold-higher concentration (IC₅₀ of 1.7 μM). In addition, 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. 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 potently 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. Low concentrations of BF738735 reduce 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

BF738735 is well tolerated by specimens with good plasma levels of the antiviral in circulation and a complete inhibition with 25 mg/kg and some inhibition with 5 mg/kg dose is observed^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

426.46

Formula

C₂₁H₁₉FN₄O₃S

CAS No.

1436383-95-7

Appearance

Solid

Color

White to off-white

SMILES

OC1=CC=C(C2=C(C)N=C3C(NCC4=CC=CC(S(=O)(C)=O)=C4)=NC=CN32)C=C1F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (293.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3449 mL	11.7244 mL	23.4489 mL
5 mM	0.4690 mL	2.3449 mL	4.6898 mL
10 mM	0.2345 mL	1.1724 mL	2.3449 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.10%

Select Batch:

Data Sheet (281 KB) SDS (252 KB)

COA (251 KB) RP-HPLC (244 KB)

Handling Instructions (2659 KB)

References

[1]. 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. [Content Brief]

[2]. V Saarnio. Antiviral Molecules of Enteroviruses. 13.1.2017.

Kinase Assay ^[1]	The PI4K in vitro activity assay is performed. Briefly, recombinant PI4KIIIβ or PI4KIIIα and their substrate, phosphatidylinositol (PI)-phosphatidylserine (PS), are diluted in buffer containing Triton X-100. The reaction is started by addition of a mixture of ATP and 0.25 μCi of [γ-³³P]ATP. After 75 to 90 min of incubation at 30°C, the reaction is terminated by addition of phosphoric acid. The incorporated radioactivity is measured by using a TopCount NXT microplate scintillation counter. Data are converted to the percent inhibition relative to controls^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	Buffalo green monkey (BGM) kidney cells, HeLa R19 cells, and HeLa Rh cells are grown at 37°C, 5% CO₂ in minimal essential medium (MEM) supplemented with 10% fetal bovine serum, penicillin, and streptomycin. The assays to determine the 50% effective concentration (EC₅₀) and 50% cytotoxic concentration (CC₅₀) of BF738735 are performed. Briefly, cells are infected with 100 CCID₅₀ for 2 h, after which the virus is removed and serial dilutions of BF738735 (0.01, 0.033, 0.1, 0.33, 1, 3.33, 10, 33.33 and 100 μM) are added. For determination of the CC₅₀, serial dilutions of BF738735 are added to the cells. Following 3 to 4 days of incubation, the medium is replaced with CellTiter 96 AQueous One solution reagent. Optical densities at 490 nm are corrected for background absorbance, which is determined from wells that lack cells. The resulting values for untreated cells are set to 100%^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Mice^[2] BF738735 is used to study the bioavailability and antiviral effect in vivo. BF738735 is administrated in mice, 1 mg/kg intravenously or 5 mg/kg orally to treat coxsackievirus serotype B4 (CVB4) induced pancreatitis. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. 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. [Content Brief] [2]. V Saarnio. Antiviral Molecules of Enteroviruses. 13.1.2017.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.3449 mL	11.7244 mL	23.4489 mL	58.6221 mL
	5 mM	0.4690 mL	2.3449 mL	4.6898 mL	11.7244 mL
	10 mM	0.2345 mL	1.1724 mL	2.3449 mL	5.8622 mL
	15 mM	0.1563 mL	0.7816 mL	1.5633 mL	3.9081 mL
	20 mM	0.1172 mL	0.5862 mL	1.1724 mL	2.9311 mL
	25 mM	0.0938 mL	0.4690 mL	0.9380 mL	2.3449 mL
	30 mM	0.0782 mL	0.3908 mL	0.7816 mL	1.9541 mL
	40 mM	0.0586 mL	0.2931 mL	0.5862 mL	1.4656 mL
	50 mM	0.0469 mL	0.2345 mL	0.4690 mL	1.1724 mL
	60 mM	0.0391 mL	0.1954 mL	0.3908 mL	0.9770 mL
	80 mM	0.0293 mL	0.1466 mL	0.2931 mL	0.7328 mL
	100 mM	0.0234 mL	0.1172 mL	0.2345 mL	0.5862 mL

BF738735 Related Classifications

Infection

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BF7387351436383-95-7BF 738735BF-738735PI4KReverse TranscriptasePhosphatidylinositol 4 kinasesPI4 kinasesInhibitorinhibitorinhibit

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BF738735

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BF738735 Related Antibodies

3 Publications Citing Use of MCE BF738735

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Customer Review

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Complete Stock Solution Preparation Table

BF738735 Related Classifications

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