BF738735
Based on 6 publication(s) in Google Scholar
BF738735 is a phosphatidylinositol 4-kinase III beta (PI4KIIIβ) inhibitor with an IC50 of 5.7 nM.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.26%
- CAS. Nr.: 1436383-95-7
- Formel: C21H19FN4O3S
- Molecular Weight:426.46
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Publications Citing Use of MedChemExpress (MCE) BF738735
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Biologische Aktivität
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PI4KIIIβ 5.7 nM (IC50) |
PI4KIIIα 1.7 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | EC50 |
31 nM
Compound: 5, BF738735
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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
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[PMID: 24900715] |
| HeLa | CC50 |
61 μM
Compound: 5, BF738735
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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
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[PMID: 24900715] |
| Huh-7 | CC50 |
>30 μM
Compound: 92; BF738735
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Cytotoxicity against human Huh-7 cells
Cytotoxicity against human Huh-7 cells
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[PMID: 33539089] |
| RD | EC50 |
11 nM
Compound: 5, BF738735
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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
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[PMID: 24900715] |
| Vero | EC50 |
13 nM
Compound: 5, BF738735
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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
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[PMID: 24900715] |
| Vero | EC50 |
15 nM
Compound: 5, BF738735
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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
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[PMID: 24900715] |
| Vero | EC50 |
19 nM
Compound: 5, BF738735
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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
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[PMID: 24900715] |
| Vero | EC50 |
21 nM
Compound: 5, BF738735
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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
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[PMID: 24900715] |
| Vero | EC50 |
5 nM
Compound: 5, BF738735
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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
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[PMID: 24900715] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1436383-95-7
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Appearance Solid
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Molecular Weight 426.46
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Formel C21H19FN4O3S
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Color White to off-white
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SMILES
OC1=CC=C(C2=C(C)N=C3C(NCC4=CC=CC(S(=O)(C)=O)=C4)=NC=CN32)C=C1F
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (6)
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Journal Impact Factor
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Most Recent
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Immunity
A chemical agonist and the Golgi-resident lipid PI4P activate STING by inducing transmembrane helix rearrangement. [Abstract]2025 Dec 5:S1074-7613(25)00506-0. PMID: 41352342 -
Int J Biol Macromol
PI4KB is an essential host factor for duck hepatitis a virus 1 replication and translation. [Abstract]2024 Nov;281(Pt 3):136480. PMID: 39393728 -
PLoS Pathog
IFITM1 enhances nonenveloped viral RNA replication by facilitating cholesterol transport to the Golgi. [Abstract]2023 May 30;19(5):e1011383. PMID: 37252940 -
Npj Viruses
A robust cell-based infection model for Rhinovirus C research and antiviral drug discovery. [Abstract]2026 May 11. PMID: 42108281 -
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Lösungsmittel & Löslichkeit
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)
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protokoll
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (281 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
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.
| 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
HY-U00426 Related Classifications
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