LF3
目录号 : GC32763An inhibitor of the β-catenin-TCF4 protein-protein interaction
Cas No.:664969-54-4
Sample solution is provided at 25 µL, 10mM.
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)
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. |
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 |
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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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 | 2.4006 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 |
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。
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