GLPBio

GA-017

Catalog No.: GC65116Purity:>98.00%
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.

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GA-017
Cas No.: 2351906-74-4
10mM (in 1mL DMSO)In Stock
$116.00
1
1mgIn Stock
$62.00
1
5mgIn Stock
$154.00
1
10mgIn Stock
$238.00
1
25mgIn Stock
$398.00
1

Citations

2 publicationsPublications from researchers using this product

Description

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.

Protocol

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:
[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] 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.

Product Documents

Purity:>98.00%Appearance:A solid

Chemical Properties

CAS No.
2351906-74-4
Molecular Formula
C18H21N3O4
Molecular Weight
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
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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