GA-017
目录号 : GC65116
GA-017是一种选择性、强效的LATS1和LATS2激酶小分子抑制剂，其对LATS1和LATS2的IC50值分别为4.10 ± 0.79nM和3.92 ± 0.42nM。
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.
GA-017是一种选择性、强效的LATS1和LATS2激酶小分子抑制剂，其对LATS1和LATS2的IC50值分别为4.10 ± 0.79nM和3.92 ± 0.42nM[1]。GA-017通常用于3D细胞培养系统、类器官扩增和Hippo信号通路调节的研究[1][2]。
在2D和3D培养条件下，GA-017（1 - 20μM，1 - 6h）以剂量依赖性方式抑制YAP/TAZ的磷酸化，并且GA-017在SKOV3细胞中的抑制作用持续6h[1]。GA-017（10μM，7天）明显增加了BCE C/D-1b细胞中的细胞聚集体大小和细胞总数[3]。
在铁氧还蛋白1（FDX1）敲低结直肠癌小鼠模型中，GA-017（2.5mg/kg/天，4周，腹腔注射）显著降低小鼠体重，同时显著增加肿瘤重量和大小。GA-017（2.5mg/kg/天，4周，腹腔注射）显著增加了FDX1敲低结直肠癌小鼠模型中Ki67阳性细胞的数量。GA-017（2.5mg/kg/天，4周，腹腔注射）显著抑制FDX1敲低结直肠癌小鼠模型中丙酮酸和α-酮戊二酸的产生[4]。
| 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 | Download SDF |
| 分子式 | C18H21N3O4 | 分子量 | 343.38 |
| 溶解度 | DMSO : 20.83 mg/mL (60.66 mM; ultrasonic and warming and heat to 80°C) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet