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PTP1B-IN-4

Names

[ CAS No. ]:
765317-72-4

[ Name ]:
PTP1B-IN-4

[Synonym ]:
3-(3,5-Dibromo-4-hydroxybenzoyl)-2-ethyl-N-[4-(1,3-thiazol-2-ylsulfamoyl)phenyl]-1-benzofuran-6-sulfonamide
1t4j
6-Benzofuransulfonamide, 3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethyl-N-[4-[(2-thiazolylamino)sulfonyl]phenyl]-
PTP1B Inhibitor
FRJ

Biological Activity

[Description]:

PTP1B-IN-4 is a non-competitive allosteric inhibitor of the protein tyrosine phosphatase PTP1B, with an IC50 of 8 μM. PTP1B-IN-4 is potentail for the research of obesity and diabetes[1][2].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphatase
Research Areas >> Metabolic Disease

[Target]

IC50: 8 μM (PTP1B)[1]


[In Vitro]

PTP1B-IN-4 (250 µM; 1 hour) stimulates insulin receptor (IR) phosphorylation in CHO cells overexpressing human IR[1]. PTP1B-IN-4 also induces phosphorylation of IRS-1 and Akt, proteins downstream of the insulin receptor[1]. Western Blot Analysis[1] Cell Line: CHO cells Concentration: 250 µM Incubation Time: 1 hour Result: Stimulated insulin receptor phosphorylation.

[References]

[1]. Wiesmann, C., et al. Allosteric inhibition of protein tyrosine phosphatase 1B. Nature Structural & Molecular Biology, 2004. 11(8), 730–737.

[2]. Jin, T., et al. Selective binding modes and allosteric inhibitory effects of lupane triterpenes on protein tyrosine phosphatase 1B. Scientific Reports, 2016. 6(1).

Chemical & Physical Properties

[ Density]:
1.8±0.1 g/cm3

[ Boiling Point ]:
855.0±75.0 °C at 760 mmHg

[ Molecular Formula ]:
C26H19Br2N3O7S3

[ Molecular Weight ]:
741.448

[ Flash Point ]:
470.9±37.1 °C

[ Exact Mass ]:
738.875183

[ PSA ]:
200.67000

[ LogP ]:
6.80

[ Vapour Pressure ]:
0.0±3.3 mmHg at 25°C

[ Index of Refraction ]:
1.727

Related Compounds