PHPS1

PHPS1 (Phenylhydrazonopyrazolone sulfonate 1) is a cell-permeable, potent, and selective small molecule inhibitor of the non-receptor protein tyrosine phosphatase SHP2 (PTPN11). It functions by binding to the catalytic domain of SHP2, effectively blocking its phosphatase activity and disrupting downstream signaling pathways, most notably the Ras/MAPK/ERK axis. In preclinical research for Acute Myeloid Leukemia (AML), PHPS1 is used to investigate the Siglec6/SHP2/Src/ERK/IL-3 signaling axis. By inhibiting SHP2, PHPS1 reduces the phosphorylation of downstream targets like ERK1/2 and decreases the expression of proteins involved in cell proliferation (e.g., Cyclin D1, Ki-67) and invasion (e.g., MMP2, MMP9). It is frequently utilized as a pharmacological tool to validate the role of SHP2 in tumor progression and to explore the efficacy of targeting this pathway in combination with other therapies like CAR-T cells.

Other names

Phenylhydrazonopyrazolone sulfonate 1