[1]Benzothieno[2,3-b]pyridine-3-carboxamide, N-[4-(aminosulfonyl)phenyl]-1,2,5,6,7,8-hexahydro-4-hydroxy-2-oxo-
- Product 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 No.
- 1359431-16-5
- Chemical Name
- [1]Benzothieno[2,3-b]pyridine-3-carboxamide, N-[4-(aminosulfonyl)phenyl]-1,2,5,6,7,8-hexahydro-4-hydroxy-2-oxo-
- Synonyms
- M435-1279;M435-1279 ，S9965;M435 1279,M4351279;M435-1279, 10 mM in DMSO;4-Hydroxy-2-oxo-N-(4-sulfamoylphenyl)-1,2,5,6,7,8-hexahydrobenzo[4,5]thieno[2,3-b]pyridine-3-carboxamide;[1]Benzothieno[2,3-b]pyridine-3-carboxamide, N-[4-(aminosulfonyl)phenyl]-1,2,5,6,7,8-hexahydro-4-hydroxy-2-oxo-
- CBNumber
- CB09788558
- Molecular Formula
- C18H17N3O5S2
- Formula Weight
- 419.47
- MOL File
- 1359431-16-5.mol
[1]Benzothieno[2,3-b]pyridine-3-carboxamide, N-[4-(aminosulfonyl)phenyl]-1,2,5,6,7,8-hexahydro-4-hydroxy-2-oxo- Property
- Density
- 1.620±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- pka
- 4.50±1.00(Predicted)
- form
- Solid
- color
- White to off-white
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P501Dispose of contents/container to..…
[1]Benzothieno[2,3-b]pyridine-3-carboxamide, N-[4-(aminosulfonyl)phenyl]-1,2,5,6,7,8-hexahydro-4-hydroxy-2-oxo- Chemical Properties,Usage,Production
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 (5mg/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: 75–100mm3)[1] |
| Dosage: | 5mg/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
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.
[1]Benzothieno[2,3-b]pyridine-3-carboxamide, N-[4-(aminosulfonyl)phenyl]-1,2,5,6,7,8-hexahydro-4-hydroxy-2-oxo- Preparation Products And Raw materials
Raw materials
Preparation Products
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