LYP-IN-3

Description

LYP-IN-3 is a selective, orally active and reversible lymphoid-tyrosine phosphatase LYP inhibitor IC50 = 2.55 ?M, Ki = 0.93 ?M . D34 exhibits high selectivity of PTP1B, PTPN12, PTPN5 and SSH2. LYP-IN-3 regulates the T-cell receptor TCR signaling by specifically inhibiting LYP. LYP-IN-3 does not significantly inhibit MC38 cell viability; its anti-tumor effect stems from immune regulation. LYP-IN-3 can significantly upregulate PD-L1 or PD-1 expression in different immune cells. LYP-IN-3 facilitates T-cell infiltration and enhances T-cell functions. LYP-IN-3 synergizes with PD-L1 blockade can significantly improve colorectal tumor regression. LYP-IN-3 can be used for the study of colorectal cancer.