PP242, Free Base **

产品名称：PP242, Free Base
产品货号：LC  P-6666
产品规格：100 MG
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.
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.  Feldman, M.E., et al.  "Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2."  PLoS Biol. 7:  371-383 (2009).
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.  Janes, M.R., et al.  "Effective and selective targeting of leukemia cells using a TORC1/2 kinase inhibitor."  Nat. Med. 16:  205-213 (2010).
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.  Mansley, M.K. and Wilson, S.M.  "Dysregulation of epithelial Na+ absorption induced by inhibition of the kinases TORC1 and TORC2."  Br. J. Pharmacol. 161:  1778-1792 (2010).
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.  Hoang, B., et al.  "Targeting TORC2 in multiple myeloma with a new mTOR kinase inhibitor."  Blood 116:  4560-4568 (2010).
PP242 significantly augmented histone deacetylase inhibitor-induced apoptosis in hepatocellular carcinoma cells.  Shao, H., et al.  "Dual targeting of mTORC1/C2 complexes enhances histone deacetylase inhibitor-mediated anti-tumor efficacy in primary HCC cancer in vitro and in vivo."  J. Hepatol.  Aug 8 (2011) [Epub ahead of print].
Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO.  Disposal:  A

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