GB1107 |
Catalog No.GC18279
One-Click Copy Product Info
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GB1107 is an orally active inhibitor of galectin-3 (Gal-3; Kd=37nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1978336-61-6
Sample solution is provided at 25 µL, 10mM.
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GB1107 is an orally active inhibitor of galectin-3 (Gal-3; Kd=37nM)[1-2]. GB1107 possesses antiviral and anticancer properties, and is applicable in research related to various tumors such as lung, gastric, and liver cancers and intervertebral disc degeneration[3-4].
In vitro, FTC-133 and 8505C thyroid cancer cells were treated with GB1107 (10–100μM) for 24 hours. By attenuating AKT phosphorylation and downregulating the expression of β-catenin and MMP2, GB1107 significantly inhibited cell adhesion and induced anoikis, while also reducing cell migration and invasion in a dose-dependent manner[5]. Wild-type mouse bone marrow-derived macrophages (WT BMDMs) were pretreated with GB1107 (5μM) for 24 hours, followed by stimulation with LLC tumor cell-conditioned medium (LLC CM). GB1107 enhanced the phagocytic ability of macrophages against tumor cells and suppressed their polarization towards the immunosuppressive M2-like phenotype[6].
In vivo, myeloid cell-specific TIM-3 knock-in mice (FSF-TIM3/LysM-Cre+/-) received intraperitoneal injections of GB1107 (5mg/kg) every other day from 7 weeks of age until 10 weeks of age. GB1107 significantly alleviated lung inflammation and downregulated the transcriptional levels of pulmonary pro-inflammatory cytokines IL-1β and TNF-α[7]. In a CCl₄-induced liver fibrosis model in C57BL/6J mice, GB1107 (10mg/kg) was administered once daily by oral gavage during the final 4 weeks of the model. GB1107 significantly reduced liver fibrosis, evidenced by decreased picrosirius red-stained areas, and lowered plasma markers of liver injury such as ALT and AST[8].
References:
[1] Vuong L, Kouverianou E, Rooney CM, et al. An Orally Active Galectin-3 Antagonist Inhibits Lung Adenocarcinoma Growth and Augments Response to PD-L1 Blockade. Cancer Res. 2019 Apr 1;79(7):1480-1492.
[2] Zetterberg FR, Diehl C, Håkansson M, et al. Discovery of Selective and Orally Available Galectin-1 Inhibitors. J Med Chem. 2023 Dec 28;66(24):16980-16990.
[3] Liu WC, Lin CS, Luo CL, et al. Intracellular Galectin-3 as a Crucial Regulator of Foam Cell Formation and Apoptosis Progression Through the Modulation of Membrane Lipid Rafts. Arch Med Res. 2026 Feb;57(2):103300.
[4] Kim SJ, Kang HG, Kim K, et al. Crosstalk between WNT and STAT3 is mediated by galectin-3 in tumor progression. Gastric Cancer. 2021 Sep;24(5):1050-1062.
[5] Lee JJ, Hsu YC, Li YS, et al. Galectin-3 Inhibitors Suppress Anoikis Resistance and Invasive Capacity in Thyroid Cancer Cells. Int J Endocrinol. 2021 May 7;2021:5583491.
[6] Wang Q, Wu Y, Jiang G, et al. Galectin-3 induces pathogenic immunosuppressive macrophages through interaction with TREM2 in lung cancer. J Exp Clin Cancer Res. 2024 Aug 13;43(1):224.
[7] Kim KS, Lee C, Kim HS, et al. TIM-3 on myeloid cells promotes pulmonary inflammation through increased production of galectin-3. Commun Biol. 2024 Sep 5;7(1):1090.
[8] MacKinnon AC, Humphries DC, Herman K, et al. Effect of GB1107, a novel galectin-3 inhibitor on pro-fibrotic signalling in the liver. Eur J Pharmacol. 2024 Dec 15;985:177077.
| Cell experiment [1]: | |
Cell lines | FTC-133 and 8505C cells (human thyroid cancer cell lines) |
Preparation Method | Cells were maintained in complete medium. For the anoikis assay, cells in medium containing GB1107 (10μM and 100μM) or vehicle (DMSO) were transferred to poly-HEMA-coated plates to create an anchorage-independent condition. |
Reaction Conditions | 10μM and 100μM; 24 hours |
Applications | GB1107 did not influence cell viability or clonogenicity. However, GB1107 significantly inhibited cell coherence and counteracted anoikis resistance. GB1107 also decreased the migratory and invasive abilities of thyroid cancer cells in a dose-dependent manner. These effects were associated with the attenuation of AKT phosphorylation and decreased expression of β-catenin and MMP2. |
| Animal experiment [2]: | |
Animal models | C57BL/6J mice |
Preparation Method | Liver fibrosis was induced by intraperitoneal (i.p.) injection of carbon tetrachloride (CCl₄, 25% in olive oil, 1μL/g) twice weekly for 8 weeks. GB1107 (10mg/kg) or vehicle was administered during the last 4 weeks of the CCl₄ treatment period. |
Dosage form | 10mg/kg/day; oral gavage; 4 weeks. |
Applications | Neoandrographolide pretreatment significantly improved heart systolic function, reduced myocardial infarct size, attenuated inflammatory cell infiltration, and decreased cardiomyocyte apoptosis in mice with MI/R. These cardioprotective effects were associated with the inhibition of the NF-κB signaling pathway and modulation of the Bax/Bcl-2 apoptotic pathway. |
References: | |
| Cas No. | 1978336-61-6 | SDF | |
| Canonical SMILES | O[C@H]([C@@H](N1N=NC(C2=CC(F)=C(F)C(F)=C2)=C1)[C@H]([C@@H](CO)O3)O)[C@H]3SC4=CC=C(Cl)C(Cl)=C4 | ||
| Formula | C₂₀H₁₆Cl₂F₃N₃O₄S | M.Wt | 522.32 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C,protect from light |
| 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 | 1.9145 mL | 9.5727 mL | 19.1454 mL |
| 5 mM | 382.9 μL | 1.9145 mL | 3.8291 mL |
| 10 mM | 191.5 μL | 957.3 μL | 1.9145 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 37 reference(s) in Google Scholar.)