Potent inhibitor of PTEN (phosphatase and tensin homolog) (IC50
= 35 nM). Displays selectivity for PTEN over cysteine-based phosphatases such as SopB, MTM, PTPβ
and SAC (IC50
values are 588 nM, 4.03, 57.5 and >10 μ
M respectively). Increases PIP2
levels; also increases Akt translocation in NIH/3T3 fibroblasts. Blocks the immunosuppressant activity of IDO-activated Tregs
. Promotes antitumor inflammatory response in combination with immunotherapy and enhances anticancer chemotherapy in tumor-bearing mice.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
A small-molecule inhibitor for phosphatase and tensin homologue deleted on chromosome 10 (PTEN).
Rosivatz et al.
ACS Chem.Biol., 2006;1:780
The PTEN pathway in Tregs is a critical driver of the suppressive tumor microenvironment.
Sharma et al.