GB1107是一种半乳糖凝集素-3（Gal-3；Kd=37nM）抑制剂。
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.
GB1107是一种半乳糖凝集素-3（Gal-3；Kd=37nM）抑制剂[1-2]。GB1107具有抗病毒和抑制癌症的作用，可用于肺癌、胃癌、肝癌等多种肿瘤以及COVID-19和椎间盘退变的相关研究[3-4]。
在体外，GB1107（10–100μM）处理甲状腺癌细胞FTC-133和8505C 24小时。GB1107通过减弱AKT磷酸化及下调β-catenin、MMP2的表达，显著抑制细胞粘附性并诱导失巢凋亡，同时以剂量依赖的方式降低细胞的迁移和侵袭能力[5]。GB1107（5μM）预处理野生型小鼠骨髓来源巨噬细胞（WT BMDMs）24小时，随后以LLC肿瘤细胞条件培养基（LLC CM）刺激。GB1107可增强巨噬细胞对肿瘤细胞的吞噬作用，并抑制巨噬细胞向免疫抑制性的M2样表型极化[6]。
在体内，GB1107（5mg/kg）每两天一次腹腔注射，用于处理从7周龄开始直至10周龄的髓系细胞特异性TIM-3敲入小鼠（FSF-TIM3/LysM-Cre+/-）。GB1107显著减轻了肺部炎症，下调了肺部促炎细胞因子IL-1β和TNF-α的转录水平[7]。GB1107（10mg/kg）每日一次口服给药，用于处理在CCl4诱导肝纤维化C57BL/6J小模型4周。GB1107显著减轻了肝脏纤维化，表现为天狼星红染色面积减少，并降低了血浆ALT、AST等肝损伤标志物[8]。
| 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 | ||
| 分子式 | C₂₀H₁₆Cl₂F₃N₃O₄S | 分子量 | 522.32 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C,protect from light |
| 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。 |
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| 制备储备液 | |||
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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 |
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