AT13148 is an oral-active and ATP-competitive, multi-AGC kinase inhibitor for Akt1/2/3, p70S6K, PKA, and ROCKI/II.

p70 S6K:8 nM, Akt1:38 nM, PKA:3 nM, Akt3:50 nM, RSK1:85 nM, Akt2:402 nM, SGK3:63 nM, ROCK1:6 nM, Chk2:860 nM, Aurora B:1840 nM, ROCK2:4 nM

In PTEN-deficient MES-SA cells, AT13148 was able to inhibit AKT and p70S6K signaling. In cancer cell lines with aberrant PI3K-AKT-mTOR or RAS-RAF pathways (GI50=1.5-3.8 μM), AT13148 was able to inhibit multiple AGC kinases, thereby suppressing cancer cell proliferation.

In PTEN-deficient MES-SA cells, AT13148 was able to inhibit AKT and p70S6K signaling. In cancer cell lines with aberrant PI3K-AKT-mTOR or RAS-RAF pathways (GI50=1.5-3.8 μM), AT13148 was able to inhibit multiple AGC kinases, thereby suppressing cancer cell proliferation.

In vitro kinase assays: AT13148 is assayed against 40 kinases and the percentage inhibition at 10 μM of AT13148 is determined. Individual IC50 values are measured for selected kinases using ATP concentrations equivalent to the Km for each enzyme.

Cytotoxicity is determined using a 72 h Alamar Blue assay or a 96 h SRB assay. (Only for Reference)