PP242, Free Base (Torkinib, CAS 1092351-67-1), >99%

LC Laboratories' Product Number P-6666 - PP242, Free Base (Torkinib, 1092351-67-1), >99% - for research use only. PP242 is an inhibitor at the kinase domain of the mammalian target of rapamycin (mTOR), which is a Ser/Thr kinase and a cell growth controller. NOTE: the term "torkinib" has been used to specify PP242 itself, but is also now in use to generically describe compounds that inhibit mTOR at the kinase domain. In the presence of 100 µM ATP, PP242 inhibits both mTORC1 and mTORC2, with IC50 values of 0.03 and 0.058 µM, respectively. PP242 inhibits mTORC1 more effectively than rapamycin. Unlike rapamycin, PP242 inhibits both mTORC1 and mTORC2. PP242 blocks the phosphorylation of Akt at S473 and prevents its activation. PP242 inhibits the proliferation of primary cells more efficiently than rapamycin. Unlike rapamycin, it also inhibits cap-dependent translation under conditions. Manual docking analyses demonstrated that PP242 was able to fit into the TOR model. PP242, but not rapamycin, induced death of mouse and human leukemia cells in vitro. In vivo, PP242 delayed leukemia onset and enhanced the effects of the front-line tyrosine kinase inhibitors more effectively than does rapamycin. However, PP242 had much weaker effects than rapamycin on the proliferation of normal lymphocytes. PP242 significantly augmented histone deacetylase inhibitor-induced apoptosis in hepatocellular carcinoma cells. PP242 inhibited growth and induced apoptosis of multiple myeloma (MM) cells more effectively than rapamycin. PP242 was an effective inhibitor of primary MM cells in vitro and growth of 8226 cells in mice. Combining bortezomib with PP242 resulted in synergistic anti-MM effects. PP242 inhibited basal serum- and glucocorticoid-inducible protein kinase 1 (SGK1) activity and prevented insulin- and dexamethasone-induced SGK1 activation, possibly by suppressing TORC1/2. It inhibited basal Na(+) absorption modestly and insulin/dexamethasone-induced Na(+) transport substantially.

• Supplier: LC Laboratories
• Product #: P-6666
• Sku #: P-6666_100mg