An inhibitor of the β-catenin-TCF4 protein-protein interaction
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LF3

Item No. 36164

Technical Information
Formal Name
N-[4-(aminosulfonyl)phenyl]-4-(3-phenyl-2-propen-1-yl)-1-piperazinecarbothioamide
CAS Number
664969-54-4
Molecular Formula
C20H24N4O2S2
Formula Weight
Purity
≥98%
A solid
λmax
256 nm
SMILES
O=S(N)(C1=CC=C(NC(N2CCN(CC2)CC=CC3=CC=CC=C3)=S)C=C1)=O
InChi Code
InChI=1S/C20H24N4O2S2/c21-28(25,26)19-10-8-18(9-11-19)22-20(27)24-15-13-23(14-16-24)12-4-7-17-5-2-1-3-6-17/h1-11H,12-16H2,(H,22,27)(H2,21,25,26)
InChi Key
ZUQIFHLBPBLRRM-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product 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 µM. 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 µM, 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

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zhao, L., Sun, L., Lu, Y., et alA small-molecule LF3 abrogates β-catenin/TCF4-mediated suppression of NaV 1.5 expression in HL-1 cardiomyocytes. J. Mol. Cell. Cardiol. 135, 90-96 (2019).

    2. Yu, Z., Jiang, X., Qin, L., et alA novel UBE2T inhibitor suppresses Wnt/β-catenin signaling hyperactivation and gastric cancer progression by blocking RACK1 ubiquitination. Oncogene 40(5), 1027-1042 (2021).

    3. Lei, Y., Yang, Q., Nie, Y., et alSmall-molecule inhibitor LF3 restrains the development of pulmonary hypertension through the Wnt/β-catenin pathway. Acta Biochim Biophys. Sin. (Shanghai) 53(10), (2021).