KU-0063794, Free Base **

产品名称：KU-0063794, Free Base
产品货号：LC  K-9090
产品规格：10 MG
Ku-0063794 inhibits both mTORC1 and mTORC2, with an IC50 value of approximately 10 nM.  But it does not inhibit the activity of 76 other protein kinases and seven lipid kinases at 1000-fold higher concentrations.  García-Martínez, J.M., et al.  "Ku-0063794 is a specific inhibitor of the mammalian target of rapamycin (mTOR)."  Biochem. J. 421:  29-42 (2009).
Mechanical stress is important in proliferation of venous smooth muscle cells (SMCs) in the neointima, which contributes to failure of vein grafts.  Mechanical cyclic stretch activates the transcription of SGK-1 (serum- and glucocorticoid-regulated kinase-1), and Ku-0063794 inhibited SGK-1 activation in response to stretch.  Cheng, J., et al.  "The mechanical stress-activated serum-, glucocorticoid-regulated kinase 1 contributes to neointima formation in vein grafts."  Circ. Res. 107:  1265-1274 (2010).
Ku-0063794 inhibited mTORC1 activity at 10 nM as tested by the dephosphorylation of S6 ribosomal protein and inhibited mTORC2 at 100 nM as tested by the dephosphorylation of Akt in human umbilical vein endothelial cells.  It also increased MAPK phosphorylation.  Dormond-Meuwly, A., et al.  "The inhibition of MAPK potentiates the anti-angiogenic efficacy of mTOR inhibitors."  Biochem. Biophys. Res. Commun. 407:  714-719 (2011).
Ku-0063794 inhibited growth of BCR-ABL+ Ph+ B precursor acute lymphoblastic leukemia cells with a GI50 of 36 nM but had little effect on B cell proliferation at 100 nM.  Janes, M.R. et al.  "Effective and selective targeting of leukemia cells using a TORC1/2 kinase inhibitor."  Nat. Med. 16:  205-213 (2010).
Ku-0063794 inhibited mTORC1 and mTORC2 in U87MG glioblastoma cells with IC50 values of 0.1 and 0.15 µM, respectively.  It also inhibited growth of T47D breast cancer cells with a GI50 of 0.35 µM.  Malagu, K., et al.  "The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase."  Bioorg. Med. Chem. Lett. 19:  5950-5953 (2009).
Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO.  Disposal:  A

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