E722-2648 (Compound C-1) is a novel specific and competitive small molecule β-catenin/BCL9 interaction inhibitor with ITC KD of 1.05 uM and IC50 of 9 uM, blocks oncogenic Wnt signaling and disrupts cholesterol homeostasis in colorectal cancer.E722-2648 (Compound C-1) inhibited β-catenin/BCL9 complexes at concentrations as low as 1 uM in BCL9-dependent CRC cell lines, Colo320 and HCT116.E722-2648 (Compound C-1) inhibited the expression of bona fide downstream Wnt/β-catenin target genes, AXIN2 and CD44, in the β-catenin/BCL9-dependent CRC cell lines.E722-2648 (Compound C-1) disrupted cholesterol homeostasis via increased cholesterol esterification and lipid droplet accumulation.E722-2648 (Compound C-1) demonstrated antitumorigenic activity in CRC cell lines and xenograft mouse models.
Cat.No
DC70375
Name
E722-2648
Chemical Properties
CAS
931963-55-2
Formula
C21H30N2OS2
MW
390.604
Storage
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
References
1. Helen Tanton, et al. Sci Adv. 2022 Apr 29;8(17):eabm3108.
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