FKGK18
Based on 2 publication(s) in Google Scholar
FKGK18 is a selective group VIA calcium-independent phospholipase A2 (GVIA iPLA2) inhibitor. FKGK18 is a fluoroketone (FK)-based compound with IC50s of 50 nM and 3 μM for iPLA2β and iPLA2γ. FKGK18 can be used for the research of beta-cell apoptosis and diabetes.
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- Pureza : 99.9%
- No. CAS: 1071001-09-6
- Fòrmula: C16H15F3O
- Peso molecular:280.28
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) FKGK18
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Actividad biológica
Descripciòn
IC50 & Target
IC50: 50 nM (iPLA2β), 3 μM (iPLA2γ)[2]
In Vitro
FKGK18 (1 nM; 1 h) inhibits glucose-stimulated insulin secretion (GSIS) and prostaglandin E2 (PGE2) generation[2]. FKGK18 (0.1-10 nM; 24 h) inhibits beta-cell apoptosis[3]. FKGK18 (0.1-10 μM; 24 h) affects immune cells function and influences B-cell survival[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human pancreatic islets
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Concentration:1 nM
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Incubation Time:1 h
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Result:Inhibited GSIS from pancreatic islets, AA hydrolysis from beta-cells membranes and PGE2 generation. Penetrated islets and the beta-cells from islets.
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Cell Line:INS-1 OE cells
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Concentration:0.1-10 nM
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Incubation Time:24 h
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Result:Inhibited beta-cells apoptosis induced by ER-stress.
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Cell Line:CD4+ T-cell and B-cell from 8–12-week-old NOD female mice
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Concentration:0.1-10 μM/L
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Incubation Time:24 h
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Result:Decreased TNF-α generation, reduced viability of B cell and antibody production.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:10-day-old female NOD mice[3]
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Dosage:20 mg/kg
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Administration:Intraperitoneal injection; 20 mg/kg three times per week; from 10 days until euthanasia
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Result:Reduced diabetes incidence and maintained better glucose homeostasis.
Chemical Information
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No. CAS 1071001-09-6
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Appearance Solid
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Peso molecular 280.28
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Fòrmula C16H15F3O
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Color Off-white to yellow
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SMILES
O=C(CCCCC1=CC=C2C=CC=CC2=C1)C(F)(F)F
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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iScience
Phospholipase PLA2G7 is complementary to GPX4 in mitigating punicic-acid-induced ferroptosis in prostate cancer cells. [Abstract]2024 Apr 18;27(5):109774. PMID: 38711443
Solvente y solubilidad
In Vitro:
DMSO : 20 mg/mL (71.36 mM; Need ultrasonic and warming; 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (4.46 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (4.46 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
In Vivo Dissolution Calculator
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.
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Kokotos G, et al. Potent and selective fluoroketone inhibitors of group VIA calcium-independent phospholipase A2. J Med Chem. 2010 May 13;53(9):3602-10. [Content Brief]
[2]. Ali T, et al. Characterization of FKGK18 as inhibitor of group VIA Ca2+-independent phospholipase A2 (iPLA2β): candidate drug for preventing beta-cell apoptosis and diabetes. PLoS One. 2013 Aug 20;8(8):e71748. [Content Brief]
[3]. Bone RN, et al. Inhibition of Ca2+-independent phospholipase A2β (iPLA2β) ameliorates islet infiltration and incidence of diabetes in NOD mice. Diabetes. 2015 Feb;64(2):541-54. [Content Brief]
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.5679 mL | 17.8393 mL | 35.6786 mL | 89.1965 mL |
| 5 mM | 0.7136 mL | 3.5679 mL | 7.1357 mL | 17.8393 mL | |
| 10 mM | 0.3568 mL | 1.7839 mL | 3.5679 mL | 8.9197 mL | |
| 15 mM | 0.2379 mL | 1.1893 mL | 2.3786 mL | 5.9464 mL | |
| 20 mM | 0.1784 mL | 0.8920 mL | 1.7839 mL | 4.4598 mL | |
| 25 mM | 0.1427 mL | 0.7136 mL | 1.4271 mL | 3.5679 mL | |
| 30 mM | 0.1189 mL | 0.5946 mL | 1.1893 mL | 2.9732 mL | |
| 40 mM | 0.0892 mL | 0.4460 mL | 0.8920 mL | 2.2299 mL | |
| 50 mM | 0.0714 mL | 0.3568 mL | 0.7136 mL | 1.7839 mL | |
| 60 mM | 0.0595 mL | 0.2973 mL | 0.5946 mL | 1.4866 mL |
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