GSK-A1
Based on 2 publication(s) in Google Scholar
GSK-A1 is a selective type III phosphatidylinositol 4-kinase PI4KA (PI4KIIIα) inhibitor with a pIC50 of 8.5-9.8. GSK-A1 inhibits PtdIns(4,5)P2 resynthesis with an IC50 of about 3 nM. GSK-A1 potently decreases the levels of PtdIns(4)P with a negligible effect on PtdIns(4,5)P2. GSK-A1 has the potential for anti-hepatitis C virus (HCV) research.
For research use only. We do not sell to patients.
- Purity: 99.04%
- CAS No.: 1416334-69-4
- Formula: C29H27FN6O4S
- Molecular Weight:574.63
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) GSK-A1
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Customer Validation & Images
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IF
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IF
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Cell Imaging/Staining
Biological Activity
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PI4KA 8.5-9.8 (pIC50) |
PI4KB 7.2-7.7 (pIC50) |
PI4K2A <5 (pIC50) |
PI4K2B <5 (pIC50) |
GSK-A1 (100 nM, 30 min) reduces HSPA1A localization at the plasma membrane in HeLa cells[2].
GSK-A1 (0-8 μM, 48 h) enhances Doxorubicin (HY-15142A) efficacy in resistant leukemia cells (K562/Adr and HL-60/Adr cells)[3].
GSK-A1 (0-50 nM) stimulates phosphorylation of LATS and YAP in HEK293A cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1416334-69-4
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Appearance Solid
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Molecular Weight 574.63
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Formula C29H27FN6O4S
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Color White to off-white
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SMILES
O=S(C1=CC(C2=CC=C3N=C(N)N(C4=CC=C(N5CCOCC5)C=C4)C3=C2)=CN=C1OC)(NC6=CC=CC=C6F)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
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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Curr Biol
2025 Apr 7;35(7):1612-1621.e3. PMID: 40049172
GSK-A1 purchased from MedChemExpress. Usage Cited in: Curr Biol. 2025 Apr 7;35(7):1612-1621.e3. [Abstract]
Injection of either the vehicle the PI4Kα inhibitor GSK-A1 (30 μM) into embryos expressing PH-mCherry. The plasma membrane signal levels are comparable immediately after injection (NC5). By NC9/budding in GSK-A1 injected embryos, PH-mCherry is lost from the cortex.
GSK-A1 purchased from MedChemExpress. Usage Cited in: Curr Biol. 2025 Apr 7;35(7):1612-1621.e3. [Abstract]
Injection of the PI4Kα inhibitor GSK-A1 (30 μM) into embryos expressing GFP-MoeABD. Scale bars: 10 μm. The results showed that PI4Kα inhibition disrupted F-actin dynamics at the posterior.
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bioRxiv
Membrane composition-dependent patterning of Rho and F-actin in an artificial cell cortex. [Abstract]2025 Jul 31:2025.07.31.667950. PMID: 40766503
GSK-A1 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Jul 31:2025.07.31.667950. [Abstract]
Quantification of normalized F-actin intensity over time after treatment with DMSO or PI4KIIIɑ inhibitor (GSK-A1) (60 μM; 10 min). Mean (solid line)) ± standard deviation (SD, shading) is shown. For both n = 3 videos from 3 extract preps on 2 experimental days.
Solvent & Solubility
DMSO : ≥ 2 mg/mL (3.48 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
* "≥" means soluble, but saturation unknown.
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)
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: ≥ 0.2 mg/mL (0.35 mM); Clear solution
This protocol yields a clear solution of ≥ 0.2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (2.0 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: ≥ 0.2 mg/mL (0.35 mM); Clear solution
This protocol yields a clear solution of ≥ 0.2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (2.0 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.
Purity & Documentation
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Data Sheet (279 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)
References
[1]. Naveen Bojjireddy, et al. Pharmacological and genetic targeting of the PI4KA enzyme reveals its important role in maintaining plasma membrane phosphatidylinositol 4-phosphate and phosphatidylinositol 4,5-bisphosphate levels. J Biol Chem. 2014 Feb 28;289(9):6120-32. [Content Brief]
[2]. Smulders L, et al. Phosphatidylinositol Monophosphates Regulate the Membrane Localization of HSPA1A, a Stress-Inducible 70-kDa Heat Shock Protein. Biomolecules. 2022 Jun 20;12(6):856. [Content Brief]
[3]. Jiang X, et al. Targeting PI4KA sensitizes refractory leukemia to chemotherapy by modulating the ERK/AMPK/OXPHOS axis. Theranostics. 2022 Oct 3;12(16):6972-6988. [Content Brief]
[4]. Li FL, et al. Hippo pathway regulation by phosphatidylinositol transfer protein and phosphoinositides. Nat Chem Biol. 2022 Oct;18(10):1076-1086. [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 | 1.7403 mL | 8.7013 mL | 17.4025 mL | 43.5063 mL |
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