PTP1B-IN-2

Product NamePTP1B-IN-2
CAS1919853-46-5
MFC34H36N2O9S2
MW680.79
EINECS
MOL File1919853-46-5.mol

Chemical Properties

Boiling point	813.4±75.0 °C(Predicted)
Density	1.350±0.06 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	DMF: 10 mg/ml; DMSO: 10 mg/ml; Ethanol: insol; PBS (pH 7.2): insol
form	A solid
pka	-3.81±0.50(Predicted)
color	White to off-white

Usage And Synthesis

Uses

PTP1B-IN-2 is a potent protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 50 nM.

Biological Activity

PTP1B-IN-2 (MDK3465, Ptp1B-In-2, Compound P6) is a potent and selective inhibitor of protein tyrosine phosphatase-1B (PTP1B) with IC50 of 50 nM. It enhances insulin-mediated phosphorylation of insulin receptor beta (IRβ) and insulin-stimulated glucose uptake.

in vitro

PTP1B-IN-2 displays more than 40-fold selectivity for PTP1B over SHP-2 and LAR and 15-fold higher selectivity for PTP1B over the highly homologous TCPTP.

target

Target	Value
PTP1B (Cell-free assay)	50 nM

References

[1] Liu P, et al. Discovery of novel, high potent, ABC type PTP1B inhibitors with TCPTP selectivity and cellular activity. Eur J Med Chem. 2016 Aug 8;118:27-33. DOI:10.1016/j.ejmech.2016.04.014