ATP-competitive mTORC1/mTORC2 inhibitor (IC50
= 8 nM). Displays selectivity for mTOR over other PI 3K family kinases (IC50
values are 0.102, 0.408, 1.27, 1.96 and 2.2 μ
M for p110γ
, DNA-PK, p110δ
respectively) and 215 further kinases. Displays modest inhibition of PKCα
, JAK2, PKCβ
II and RET (IC50
values are 0.049, 0.110, 0.185, 0.198 and 0.224 μ
M respectively). Inhibits both S6K and 4EBP1 phosphorylation; activity causes a decrease in cap-dependent protein translation. Also triggers downregulation of cFLIPS
and augments TRAIL-induced apoptosis of cancer cells.
Soluble to 25 mM in DMSO
Store at +4°C
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.
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.
Apsel et al.
Effective and selective targeting of leukemia cells using a TORC1/2 kinase inhibitor.
Janes et al.
mTOR complex 2 is involved in regulation of Cbl-dependent c-FLIP regulation and sensitivity of TRAIL-induced apoptosis.
Zhao et al.
Cancer Res., 2013;73:1946
Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2.
Feldman et al.
PLoS Biol., 2009;7:371
The citations listed below are publications that use Tocris products. Selected citations for PP 242 include:
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