GS-493

A cell-permeable, bioavailable, non-toxic p-nitro analog of PHPS1 (Cat. No. 540213) that exhibits enhanced potency and selectivity. Acts as a phosphotyrosine mimetic, substrate-competitive and reversible catalytic domain inhibitor of SHP2 (IC₅₀ = 0.071, 2.08 & 3.17 µM for SHP2, SHP1 & PTP1B, respectively). Dose-dependently reverts HGF-stimulatd epithelial-mesenchymal transition of HPAF II cells and blocks human lung adenocarcinoma LXFA 526L anchorage-independent growth. Shown to significantly retard LXFA 526L xenografted tumor growth in mice (46 mg/kg/day, i.p., q.d.).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Cell permeable: yes

Primary Target
SHP2

Reversible: yes

Target IC₅₀: 0.071, 2.08 & 3.17 &micro

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Grosskopf, S., et al. 2015. ChemMedChem.10, 815.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)