2. Metabolic Enzyme/Protease Apoptosis
  3. Phospholipase Apoptosis
  4. FKGK18

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.

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

FKGK18 Chemical Structure

FKGK18 Chemical Structure

CAS No. : 1071001-09-6

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1 mg USD 150 In-stock
5 mg USD 480 In-stock
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Based on 1 publication(s) in Google Scholar

FKGK18 Related Antibodies

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1 Publications Citing Use of MCE FKGK18

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Description

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[1][2][3].

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.

FKGK18 Related Antibodies

Cell Viability Assay[2]

Cell Line: Human pancreatic islets
Concentration: 1 nM
Incubation Time: 1 h
Result: Inhibited GSIS from pancreatic islets, AA hydrolysis from beta-cells membranes and PGE2 generation. Penetrated islets and the beta-cells from islets.

Apoptosis Analysis[2]

Cell Line: INS-1 OE cells
Concentration: 0.1-10 nM
Incubation Time: 24 h
Result: Inhibited beta-cells apoptosis induced by ER-stress.

Cell Viability Assay[3]

Cell Line: CD4+ T-cell and B-cell from 8–12-week-old NOD female mice
Concentration: 0.1-10 μM/L
Incubation Time: 24 h
Result: Decreased TNF-α generation, reduced viability of B cell and antibody production.
In Vivo

FKGK18 (20 mg/kg; i.p. three times per week from 10 days until euthanasia) reduces diabetes incidence[3].

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

Animal Model: 10-day-old female NOD mice[3]
Dosage: 20 mg/kg
Administration: Intraperitoneal injection; 20 mg/kg three times per week; from 10 days until euthanasia
Result: Reduced diabetes incidence and maintained better glucose homeostasis.
Molecular Weight

280.28

Formula

C16H15F3O
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(CCCCC1=CC=C2C=CC=CC2=C1)C(F)(F)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.5679 mL 17.8393 mL 35.6786 mL
5 mM 0.7136 mL 3.5679 mL 7.1357 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, 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 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.
  • Protocol 2

    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:

Dosage

mg/kg

Animal weight
(per animal)

g

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: ≥99.0%

COA (243 KB)

Handling Instructions (2659 KB)
References

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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FKGK18 Related Classifications

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:

FKGK181071001-09-6FKGK 18FKGK-18PhospholipaseApoptosisdiabetesgroup VIAcalcium-independentfluoroketoneINS-1pancreatic isletsInhibitorinhibitorinhibit

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