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
