tc-ptp-in-1

TC-PTP-IN-1 (compound 8) is a potent inhibitor of TC-PTP, with an IC50 value of 9.2 nM and Ki values of 4.3 nM and 34 nM for TC-PTP and PTP1B, respectively. TC-PTP-IN-1 increases the expression of pSre416 protein. TC-PTP-IN-1 (compound 3) also acts as a TC-PTP ligand for TP1L.

PTP1B/TC-PTP IN-1 is a dual inhibitor of PTP1B and TC-PTP. It can be used as a target protein ligand for the synthesis of the PROTAC DU-14 (PTP1B/TC-PTP PROTAC).

PTP1B/AKR1B1-IN-1 is a dual inhibitor targeting protein tyrosine phosphatase 1B (PTP1B) and aldose reductase (AKR1B1), with IC50s of 0.06 μM for PTP1B and 4.3 μM for AKR1B1. It also inhibits T-cell protein tyrosine phosphatase (TC-PTP) with an IC50 of 9 μM. This compound acts as an insulin-mimetic in murine myoblasts, reduces AKR1B1-mediated sorbitol accumulation, and aids in managing blood glucose levels and inhibiting type 2 diabetes mellitus (T2DM) development [1].