GA-017 |
رقم الكتالوجGC65116
One-Click Copy Product Info
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GA-017 هو مثبط قوي وانتقائي LATS1 و LATS2 (مثبط كبير للورم كيناز 1/2) ، بقيم IC50 تبلغ 4.10 و 3.92 نانومتر ، على التواليGA-017 هو منشط لتكاثر الخلاياGA-017 تروج لتفعيل YAP / TAZ والانتقال النووييعزز GA-017 نمو الخلايا في ظل ظروف الثقافة ثلاثية الأبعادGA-017 يعزز تكوين الكائنات الحية المعوية خارج الجسم
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 |
| الذوبان | 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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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.)