GSK-A1 |
Catalog No.GC49284
One-Click Copy Product Info
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GSK-A1 is a selective phosphatidylinositol 4-kinase IIIα (PI4KIIIα/PI4KA) inhibitor (pIC50=8.5-9.8). GSK-A1 inhibits PtdIns(4,5)P2 resynthesis (IC50=3nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1416334-69-4
Sample solution is provided at 25 µL, 10mM.
GSK-A1 is a selective phosphatidylinositol 4-kinase IIIα (PI4KIIIα/PI4KA) inhibitor (pIC50=8.5-9.8). GSK-A1 inhibits PtdIns(4,5)P2 resynthesis (IC50=3nM). GSK-A1 downregulates phosphatidylinositol 4-phosphate (PtdIns(4)P) generation at the cell membrane. GSK-A1 interferes with hepatitis C virus replication and membrane signal transduction. GSK-A1 enhances antitumor effects by regulating the ERK/AMPK/OXPHOS axis and the Hippo/YAP pathway. GSK-A1 can be used for research on hepatitis C, drug-resistant leukemia, and membrane lipid signaling[1-4].
In vitro, HEK293 and HeLa cells were treated with 100nM GSK-A1 for 30 minutes. GSK-A1 significantly reduced heat shock protein HSPA1A plasma membrane localization in heat-shocked cells[5]. K562/Adr and HL-60/Adr doxorubicin-resistant leukemia cells were treated with 0-8μM GSK-A1 for 48 hours. GSK-A1 enhanced doxorubicin cytotoxicity against drug-resistant leukemia cells[6].
References:[1] Dornan GL, Dalwadi U, Hamelin DJ, et al. Probing the Architecture, Dynamics, and Inhibition of the PI4KIIIα/TTC7/FAM126 Complex. J Mol Biol. 2018 Sep 14;430(18 Pt B):3129-3142.
[2] Smulders L, Altman R, Briseno C, 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.
[3] Kučka M, Gonzalez-Iglesias AE, Tomić M, et al. Calcium-Prolactin Secretion Coupling in Rat Pituitary Lactotrophs Is Controlled by PI4-Kinase Alpha. Front Endocrinol (Lausanne). 2021 Dec 30;12:790441.
[4] Beebe SJ, Reimann EM, Schlender KK. Purification and characterization of a cAMP- and Ca2+-calmodulin-independent glycogen synthase kinase from porcine renal cortex. J Biol Chem. 1984 Feb 10;259(3):1415-22.
[5] Smulders L, Altman R, Briseno C, et al. Phosphatidylinositol Monophosphates Regulate the Membrane Localization of HSPA1A, a Stress-Inducible 70-kDa Heat Shock Protein. Biomolecules. 2022 Jun;12(6):856.
[6] Jiang X, Huang X, Zheng G, et al. Targeting PI4KA sensitizes refractory leukemia to chemotherapy by modulating the ERK/AMPK/OXPHOS axis. Theranostics. 2022;12(16):6972-6988.
| Cell experiment [1]: | |
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Cell lines |
HeLa cells (human epithelial immortal cell line) |
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Preparation Method |
HeLa cells were maintained in Minimum Essential Media supplemented with 10% fetal bovine serum, 2mM L-glutamine, penicillin-streptomycin, 0.1mM non-essential amino acids and sodium pyruvate at 37°C, 5% CO2. HeLa cells were transiently transfected with HSPA1A-GFP for 18h, then heat-shocked at 42°C for 1h and recovered at 37°C for 8h. After heat shock and during the 8h recovery period, cells were treated with 100nM GSK-A1 diluted in serum-free DMEM for 30min. HSPA1A's plasma membrane localization was quantified using confocal microscopy. |
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Reaction Conditions |
100nM; 30min |
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Applications |
GSK-A1 significantly decreased the plasma membrane localization of HSPA1A in heat-shocked HeLa cells. GSK-A1 also significantly decreased the plasma membrane localization of the PI(4)P biosensor P4M-SidMx2. GSK-A1 significantly decreased the plasma membrane localization of the PS biosensor Lact-C2. GSK-A1 slightly decreased the plasma membrane localization of the PI(4,5)P2 biosensor PLCδ-PH in control cells. GSK-A1 did not alter the endosomal localization of the PI(3)P biosensor EEA1. |
| References: [1] Smulders L, Altman R, Briseno C, et al. Phosphatidylinositol Monophosphates Regulate the Membrane Localization of HSPA1A, a Stress-Inducible 70-kDa Heat Shock Protein. Biomolecules. 2022 Jun;12(6):856. | |
| Cas No. | 1416334-69-4 | SDF | |
| Canonical SMILES | O=S(NC1=C(F)C=CC=C1)(C2=C(OC)N=CC(C3=CC4=C(N=C(N4C5=CC=C(N6CCOCC6)C=C5)N)C=C3)=C2)=O | ||
| Formula | C29H27FN6O4S | M.Wt | 574.6 |
| Solubility | DMSO: 2 mg/ml | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7403 mL | 8.7017 mL | 17.4034 mL |
| 5 mM | 348.1 μL | 1.7403 mL | 3.4807 mL |
| 10 mM | 174 μL | 870.2 μL | 1.7403 mL |
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 14 reference(s) in Google Scholar.)