| Identification | Back Directory | [Name]
[1]Benzothieno[2,3-b]pyridine-3-carboxamide, N-[4-(aminosulfonyl)phenyl]-1,2,5,6,7,8-hexahydro-4-hydroxy-2-oxo- | [CAS]
1359431-16-5 | [Synonyms]
M435-1279
[1]Benzothieno[2,3-b]pyridine-3-carboxamide, N-[4-(aminosulfonyl)phenyl]-1,2,5,6,7,8-hexahydro-4-hydroxy-2-oxo- | [Molecular Formula]
C18H17N3O5S2 | [MOL File]
1359431-16-5.mol | [Molecular Weight]
419.47 |
| Hazard Information | Back Directory | [Uses]
M435-1279 is a UBE2T inhibitor. M435-1279 inhibits the Wnt/β-catenin signaling pathway hyperactivation through blocking UBE2T-mediated degradation of RACK1[1]. | [Biological Activity]
M435-1279 is a UBE2T inhibitor. M435-1279 inhibits the Wnt/β-catenin signaling pathway hyperactivation through blocking UBE2T-mediated degradation of RACK1[1].
M435-1279 (0, 2, 4, 8, 16, 31 μM; 48 h) significantly inhibits the growth of HGC27, AGS, and MKN45 cells[1].M435-1279 (0, 4, 8, 12, 16, 20 μM) inhibits the cell viability with IC50s of 16.8, 11.88, 6.93, 7.76 μM of GES-1, HGC27, MKN45, AGS cells, respectively[1].M435-1279 (31 nM to 500 μM) binds to UBE2T with a KD value of 50.5 μM[1].M435-1279 (11.88 μM; 48 h) inhibits the ubiquitination of RACK1 and the hyperactivation of the Wnt/β-catenin pathway[1].
M435-1279 (5 mg/kg/day; intratumor injection for 18 days) slows the tumor growth[1].M435-1279 induces higher RACK1 proteins expression, and lower Ki-67 and β-catenin proteins expression in intratumor tumors[1]. | [in vivo]
M435-1279 (5?mg/kg/day; intratumor injection for 18 days) slows the tumor growth[1].
?
M435-1279 induces higher RACK1 proteins expression, and lower Ki-67 and β-catenin proteins expression in intratumor tumors[1]. | Animal Model: | BALB/C nude mice CDX model (MKN45 tumor size: 75–100?mm3)[1] | | Dosage: | 5?mg/kg/day | | Administration: | Intratumor injection for 18 days | | Result: | Slowed the tumor growth.
Induced higher RACK1 proteins expression, and lower Ki-67 and β-catenin proteins expression in intratumor tumors.
|
| [IC 50]
UBE2T | [storage]
Store at -20°C | [References]
[1]. Yu Z, et al. A novel UBE2T inhibitor suppresses Wnt/β-catenin signaling hyperactivation and gastric cancer progression by blocking RACK1 ubiquitination. Oncogene. 2021 Feb;40(5):1027-1042. doi: 10.1038/s41388-020-01572-w. Epub 2020 Dec 15. Erratum in: Oncogene. 2021 Apr;40(14):2622-2623. |
|
| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
|