[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

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[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

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Hazard and Precautionary Statements (GHS)

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[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 (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

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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[1]Benzothieno[2,3-b]pyridine-3-carboxamide, N-[4-(aminosulfonyl)phenyl]-1,2,5,6,7,8-hexahydro-4-hydroxy-2-oxo- Suppliers

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1359431-16-5, [1]Benzothieno[2,3-b]pyridine-3-carboxamide, N-[4-(aminosulfonyl)phenyl]-1,2,5,6,7,8-hexahydro-4-hydroxy-2-oxo-Related Search:

[1]Benzothieno[2,3-b]pyridine-3-carboxamide, N-[4-(aminosulfonyl)phenyl]-1,2,5,6,7,8-hexahydro-4-hydroxy-2-oxo-

M435-1279

M435 1279,M4351279

4-Hydroxy-2-oxo-N-(4-sulfamoylphenyl)-1,2,5,6,7,8-hexahydrobenzo[4,5]thieno[2,3-b]pyridine-3-carboxamide

M435-1279, 10 mM in DMSO

M435-1279 ，S9965

1359431-16-5