PHPS1 sodium salt (CAS 314291-83-3 (free acid))
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PHPS1 sodium salt is a phenylhydrazonopyrazolone sulfonate, which is cell-permeable and inhibits the phosphatase and cellular activities of Shp2. The inhibition of Shp2 effects cellular events such as hepatocyte growth factor/scatter factor (HGF/SF)-induced epithelial cell scattering, branching morphogenesis, and downstream signaling such as paxillin dephosphorylation. Studies have revealed that PHPS1 sodium salt interacts with the active site of Shp2 via forming a seven hydrogen bond lattice between the sulfonate moiety and the PTP signature loop of the enzyme. PHPS1 is a compound that can enter cells and mimic phosphotyrosine. Its main effect is the inhibition of the Src homology region 2 domain-containing phosphatase (SHP)-2, with an IC50 value of 2.1 µM and a Ki value of 0.73 µM. It specifically targets SHP-2, although at higher concentrations, it can also inhibit ECPTP, PTP1B, SHP-1, and mycobacterium MptpA, with IC50 values of 5.4, 19, 30, and 39 µM, respectively.
PHPS1 sodium salt (CAS 314291-83-3 (free acid)) References
- Specific inhibitors of the protein tyrosine phosphatase Shp2 identified by high-throughput docking. | Hellmuth, K., et al. 2008. Proc Natl Acad Sci U S A. 105: 7275-80. PMID: 18480264
- Inducible SHP-2 activation confers resistance to imatinib in drug-tolerant chronic myeloid leukemia cells. | Li, X., et al. 2018. Toxicol Appl Pharmacol. 360: 249-256. PMID: 30290167
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
PHPS1 sodium salt, 5 mg | sc-253272 | 5 mg | $209.00 |