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LF3 Sale

目录号 : GC32763

An inhibitor of the β-catenin-TCF4 protein-protein interaction

LF3 Chemical Structure

Cas No.:664969-54-4

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥589.00
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5mg
¥536.00
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10mg
¥696.00
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25mg
¥1,562.00
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50mg
¥2,499.00
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100mg
¥4,641.00
现货

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Sample solution is provided at 25 µL, 10mM.

Description

LF3 is an inhibitor of the protein-protein interaction between β-catenin and T cell factor 4 (TCF4).1 It inhibits the β-catenin-TCF4 interaction in an immunoprecipitation assay and prevents β-catenin-induced inhibition of SCN5A promoter activity in HEK293 cells when used at a concentration of 10 ?M. LF3 increases levels of the voltage-gated sodium channel Nav1.5 in HL-1 cardiomyocytes. It is cytotoxic to GES-1, HGC-27, MKN45, and AGS gastric cancer cells (IC50s = 24.68, 18.2, 489, and 56.76 ?M, respectively).2 In vivo, LF3 (25 mg/kg) decreases pulmonary artery systolic pressure (PASP) and the right ventricular hypertrophy index (RVHI) in a rat model of total pneumonectomy-induced pulmonary hypertension.3

1.Zhao, L., Sun, L., Lu, Y., et al.A small-molecule LF3 abrogates β-catenin/TCF4-mediated suppression of NaV 1.5 expression in HL-1 cardiomyocytesJ. Mol. Cell. Cardiol.13590-96(2019) 2.Yu, Z., Jiang, X., Qin, L., et al.A novel UBE2T inhibitor suppresses Wnt/β-catenin signaling hyperactivation and gastric cancer progression by blocking RACK1 ubiquitinationOncogene40(5)1027-1042(2021) 3.Lei, Y., Yang, Q., Nie, Y., et al.Small-molecule inhibitor LF3 restrains the development of pulmonary hypertension through the Wnt/β-catenin pathwayActa Biochim Biophys. Sin. (Shanghai)53(10)(2021)

实验参考方法

Cell experiment:

LF3 is dissolved in DMSO to a concentration of 50 mM and diluted with culture medium. Two colon cancer cell lines (HCT116 and HT29) and a breast cancer cell line (MCF7) are treated with LF3 (0, 30, 60 μM) for 24 hours and labeled with BrdUrd for 4 to 5 hours to detect proliferating cells[1].

Animal experiment:

Mice: Unsorted GFPlow and GFPhigh SW480 cells are subcutaneously injected into the back skin of NOD/SCID mice. Tumor growth is monitored over a period of 45 days. For therapy, LF3 is administered i.v. at 50 mg/kg body weight for three rounds over 5 consecutive days, with 2-day breaks[1].

References:

[1]. Fang L, et al. A Small-Molecule Antagonist of the β-Catenin/TCF4 Interaction Blocks the Self-Renewal of Cancer Stem Cells and Suppresses Tumorigenesis. Cancer Res. 2016 Feb 15;76(4):891-901.

化学性质

Cas No. 664969-54-4 SDF
Canonical SMILES S=C(N1CCN(C/C=C/C2=CC=CC=C2)CC1)NC3=CC=C(S(=O)(N)=O)C=C3
分子式 C20H24N4O2S2 分子量 416.56
溶解度 DMSO : ≥ 32 mg/mL (76.82 mM) 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.4006 mL 12.0031 mL 24.0061 mL
5 mM 0.4801 mL 2.4006 mL 4.8012 mL
10 mM 0.2401 mL 1.2003 mL 2.4006 mL
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