Биологическая активность
E722-2648 (Compound C-1) is a novel specific and competitive малая молекула β-catenin/BCL9 interaction ингибитор 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 клетка 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 клетка lines.E722-2648 (Compound C-1) disrupted cholesterol homeostasis via increased cholesterol esterification and липид droplet accumulation.E722-2648 (Compound C-1) demonstrated antitumorigenic activity in CRC клетка lines and xenograft mouse models.
Оригинал на английском
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.
Химические свойства
- CAS №
- 931963-55-2
- Брутто-формула
- C₂₁H₃₀N₂Os₂
- Мол. масса
- 390.61 г/моль
- SMILES
- S1C2C=C(C(NCCCN3CCCC(C)C3)=O)SCC=2C2=C1CCCC2
- Синонимы
- N-[3-(3-methylpiperidin-1-yl)propyl]-6,7,8,9-tetrahydro-1H-thiopyrano[4,3-b][1]benzothiole-3-carboxamide; N-(3-(3-Methylpiperidin-1-yl)propyl)-6,7,8,9-tetrahydro-1H-benzo[4,5]thieno[3,2-c]thiopyran-3-carboxamide; GLXC-25824; AKOS001924701; CCG-169651 и ещё 6
3D-структура молекулы
Вращайте мышью · Колесо — масштаб
Хранение и физические свойства
- Условия хранения
- 2 года -20°C порошок, 2 недели 4°C в ДМСО, 6 мес. -80°C в ДМСО Publication: 1. Helen Tanton, et al. Sci Adv. 2022 Apr 29;8(17):eabm3108.
Безопасность и документация
Только для научно-исследовательского применения. Не предназначено для использования у пациентов или в качестве лекарственного средства.