GA-017 |
Catalog No.GC65116
One-Click Copy Product Info
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GA-017 is a selective and potent small-molecule inhibitor of LATS1 and LATS2 kinases, with IC50 values of 4.10 ± 0.79nM for LATS1 and 3.92 ± 0.42nM for LATS2, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2351906-74-4
Sample solution is provided at 25 µL, 10mM.
GA-017 is a selective and potent small-molecule inhibitor of LATS1 and LATS2 kinases, with IC50 values of 4.10 ± 0.79nM for LATS1 and 3.92 ± 0.42nM for LATS2, respectively[1]. GA-017 is typically used for research in 3D cell culture systems, organoid expansion, and Hippo signaling pathway modulation[1][2].
GA-017 (1 - 20μM, 1 - 6h) inhibited the phosphorylation of YAP/TAZ in a dose-dependent manner under both 2D and 3D culture conditions and the inhibitory effect of GA-017 continued for 6h in SKOV3 cells[1]. GA-017 (10μM, 7 days) visibly increased both cell aggregate size and total cell number in the BCE C/D-1b cells[3].
GA-017 (2.5mg/kg/day, 4 weeks, i.p.) significantly decreased the body weight of mice while notably increasing tumor weight and size in the Ferredoxin 1 (FDX1)-knockdown colorectal cancer mouse model. GA-017 (2.5mg/kg/day, 4 weeks, i.p.) significantly increased the number of Ki67-positive cells in the FDX1-knockdown colorectal cancer mouse model. GA-017 (2.5mg/kg/day, 4 weeks, i.p.) significantly suppressed the production of pyruvate and α-ketoglutarate in the FDX1-knockdown colorectal cancer mouse model[4].
References:
[1] Aihara A, Iwawaki T, Abe-Fukasawa N, et al. Small molecule LATS kinase inhibitors block the Hippo signaling pathway and promote cell growth under 3D culture conditions[J]. Journal of Biological Chemistry, 2022, 298(4): 101779.
[2] Xu Z, Xu X, Mi Y, et al. Identifying the Role of YAP in the Development of Rumen Epithelium Using 3D Organoid[J]. Stem Cells International, 2025, 2025(1): 5105796.
[3] Abe-Fukasawa N, Hayashi R, Morita M, et al. Ex vivo expansion of corneal endothelial cells enabled by small molecule inhibitors of LATS kinase[J]. Regenerative Therapy, 2025, 30: 730-739.
[4] Hu Y, Liu H, Tan X, et al. Knocking down ferredoxin 1 inhibits the progression of colorectal Cancer and regulates Cuproptosis via mediating the Hippo signaling pathway[J]. Molecular Carcinogenesis, 2025, 64(5): 911-922.
| Cell experiment [1]: | |
Cell lines | Human ovarian adenocarcinoma cell line SKOV3 |
Preparation Method | SKOV3 cells were seeded in a medium supplemented with (3D) or without (2D) 0.015% gellan gum and treated with GA-017 or DMSO for the indicated time. Cells were then lysed with RIPA buffer containing Halt Protease and Phosphatase Inhibitors. Samples were separated by SDS-PAGE, and the proteins in the gel were electrophoretically transferred onto a PVDF membrane. The blot was then blocked and incubated with antibodies. Next, the blot was incubated with peroxidase-conjugated anti-immunoglobulin. Sites of antibody binding were visualized using the ECL Western blotting detection system and were subjected to densitometry analysis using ImageJ and normalized to β-Actin expression. |
Reaction Conditions | 1 - 20μM, 1 - 6h |
Applications | GA-017 inhibited the phosphorylation of YAP/TAZ in a dose-dependent manner under both 2D and 3D culture conditions and the inhibitory effect of GA-017 continued for 6h. |
| Animal experiment [2]: | |
Animal models | Ferredoxin 1 (FDX1)-knockdown colorectal cancer mouse model |
Preparation Method | Eighteen female nude BALB/c mice (5 - 6 weeks, 18 - 20g) were kept at 24°C - 25°C and 50% - 60% humidity, with free access of standard food and water. Animals were randomly divided into LV-NC group, LV-FDX1 group and LV-FDX1+GA-017 group (n = 6 per group). To induce the tumor-bearing model, 0.1mL of cell suspension was subcutaneously inoculated (2×106 cells per mouse) in nude mice. LV-NC and LV-FDX1 were used for gene knockdown. To inhibit Hippo pathway, GA-017 (2.5mg/kg) was intraperitoneally injected into LV-FDX1-treated mice. Mouse body weights were recorded weekly. Four weeks after injection, tumor weight and size were measured. |
Dosage form | 2.5mg/kg/day, 4 weeks, i.p. |
Applications | GA-017 significantly decreased the body weight of mice while notably increasing tumor weight and size. |
References: | |
| Cas No. | 2351906-74-4 | SDF | |
| Formula | C18H21N3O4 | M.Wt | 343.38 |
| Solubility | DMSO : 20.83 mg/mL (60.66 mM; ultrasonic and warming and heat to 80°C) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| 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 | 2.9122 mL | 14.5611 mL | 29.1223 mL |
| 5 mM | 582.4 μL | 2.9122 mL | 5.8245 mL |
| 10 mM | 291.2 μL | 1.4561 mL | 2.9122 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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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 30 reference(s) in Google Scholar.)