TP1L

TP1L is a potent and selective T-cell protein tyrosine phosphatase (TC-PTP) PROTAC degrader, with a DC50 value of 35.8 nM. TP1L elevates the phosphorylation level of TC-PTP substrates including pSTAT1 and pJAK1. TP1L selectively enhances IFN-γ signaling and increases MHC-I expression. TP1L activates TCR signaling through increases phosphorylation of LCK. TP1L enhances CAR-T cell mediated tumor killing efficacy through activation of the CAR-T cells. TP1L can be used for the study of cancer. (Pink: TC-PTP ligand: , Blue: E3 ligase CRBN Ligand (HY-A0003), Black: Linker: (HY-140002) ).

C64H81F2N8O14P

1255.34

FC(C1=CC=C(C[C@H](NC([C@@H](NC(CO[C@@H]2[C@@H](C(C)C)CC[C@H](C)C2)=O)CC3=CC=CC=C3)=O)C(N[C@@H](CCCCNC(C4=CC=C(CC)C=C4)=O)C(NCCOCCC(NC5=CC=CC6=C5CN(C(CC7)C(NC7=O)=O)C6=O)=O)=O)=O)C=C1)(P(O)(O)=O)F

IFNAR; JAK; MHC; Phosphatase; PROTACs

10 mM in DMSO

Room temperature