Product Categories

mTOR Mammalian Target of Rapamycin

mTOR Inhibitors (28)

water-soluble

Cat.No. Product Name Information Product Citations Customer Reviews
S1039 Rapamycin (Sirolimus) Rapamycin (Sirolimus, AY-22989, WY-090217) is a specific mTOR inhibitor with IC50 of ~0.1 nM.
S1120 Everolimus (RAD001) Everolimus (RAD001) is an mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM.
S1555 AZD8055 AZD8055 is a novel ATP-competitive inhibitor of mTOR with IC50 of 0.8 nM.
S2811 INK 128 (MLN0128) INK 128 is a potent and selective mTOR inhibitor with IC50 of 1 nM.
S2218 PP242 PP242 is a selective mTOR inhibitor with IC50 of 8 nM.
S1009 BEZ235 (NVP-BEZ235) BEZ235 (NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor of p110α, p110γ, p110δ and p110β with IC50 of 4 nM, 5 nM, 7 nM and 75 nM, respectively, and also inhibits ATR with IC50 of 21 nM.
S1038 PI-103 PI-103 is a potent, ATP-competitive PI3K inhibitor of DNA-PK, p110α, mTORC1, PI3KC2β, p110δ, mTORC2, p110β, and p110γ with IC50 of 2 nM, 8 nM, 20 nM, 26 nM, 48 nM, 83 nM, 88 nM and 150 nM, respectively.
S2827 Torin 1 Torin1 is a potent inhibitor of mTOR with IC50 of 2-10 nM.
S1022 Deforolimus (Ridaforolimus) Deforolimus (Ridaforolimus, AP23573, MK-8669) is a selective mTOR inhibitor with IC50 of 0.2 nM.
S1044 Temsirolimus (Torisel) Temsirolimus (CCI-779, Torisel) is a specific mTOR inhibitor with IC50 of 1.76 μM.
Cat.No. Product Name Information Product Citations Customer Reviews
S1226 Ku-0063794 KU-0063794 is a potent and highly specific mTOR inhibitor for both mTORC1 and mTORC2 with IC50 ~10 nM.
S1523 XL765 (SAR245409) XL765 is a dual inhibitor of mTOR/PI3k for mTOR, p110α, p110β, p110γ and p110δ with IC50 of 157 nM, 39 nM, 113 nM, 9 nM and 43 nM, respectively.
S2658 GSK2126458 GSK2126458 is a highly selective and potent inhibitor of p110α, p110β, p110γ, p110δ, mTORC1 and mTORC2 with Ki of 0.019 nM, 0.13 nM, 0.024 nM, 0.06 nM, 0.18 nM and 0.3 nM, respectively.
S2624 OSI-027 OSI-027 is a selective and potent dual inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM, respectively.
S2743 PF-04691502 PF-04691502 is an ATP-competitive, selective inhibitor of PI3K(α/β/δ/γ)/mTOR with Ki of 1.8 nM/2.1 nM/1.6 nM/1.9 nM and 16 nM, also inhibits Akt phosphorylation on T308/S473 with IC50 of 7.5 nM/3.8 nM.
S2783 AZD2014 AZD2014 is a novel dual mTORC1 and mTORC2 inhibitor with potential antineoplastic activity.
S2628 PF-05212384 (PKI-587) PKI-587 is a highly potent dual inhibitor of PI3Kα, PI3Kγ and mTOR with IC50 of 0.4 nM, 5.4 nM and 1.6 nM, respectively.
S2696 GDC-0980 (RG7422) GDC-0980 (RG7422) is a potent, selective inhibitor of PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ with IC50 of 5 nM, 27 nM, 7 nM, and 14 nM, and also a mTOR inhibitor with Ki of 17 nM.
S1266 WYE-354 WYE-354 is a potent, specific and ATP-competitive inhibitor of mTOR with IC50 of 5 nM.
S1360 GSK1059615 GSK1059615 is a novel and dual inhibitor of PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR with IC50 of 0.4 nM, 0.6 nM, 2 nM, 5 nM and 12 nM, respectively.
Cat.No. Product Name Information Product Citations Customer Reviews
S2661 WYE-125132 WYE-125132 is a highly potent, ATP-competitive and specific mTOR inhibitor with IC50 of 0.19 nM.
S2668 WYE-687 WYE-687 is an ATP-competitive and selective inhibitor of mTOR with IC50 of 7 nM.
S2699 CH5132799 CH5132799 exhibits a strong inhibitory activity especially against PI3Kα with IC50 of 14 nM and also inhibits mTOR with IC50 of 1.6 µM.
S2817 Torin 2 Torin 2 is a highly potent and selective mTOR inhibitor with IC50 of 0.25 nM, and also exhibits potent cellular activity against ATM/ATR/DNA-PK with EC50 of 28 nM, 35 nM and 118 nM, respectively.
S2238 Palomid 529 Palomid 529 (P529) is a PI3K/Akt/mTOR inhibitor for VEGF-A and bFGF with IC50 of 10 nM and 30 nM, respectively.
S2622 PP-121 PP-121 is a multi-target inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, respectively, and also inhibits DNA-PK with IC50 of 60 nM.
S2749 NVP-BGT226 NVP-BGT226 is a novel dual PI3K/mTOR inhibitor with IC50 of 1 nM.
S2689 WAY-600 WAY-600 is a potent, ATP-competitive and selective inhibitor of mTOR with IC50 of 9 nM.
Page:
  • 1
  • 2
  • 3
All mTOR Inhibitors

Mammalian target of Rapamycin (mTOR), also known as FKBP12-rapamycin-associated protein (FRAP), is a 280 kDa serine/threonine kinase [1-3]. mTOR kinase activity could be promoted by various extra- and intracellular stimulus like trophic factors, mitogens, hormones, amino acids and cellular stress [4-8]. In response to increased availability of stimuli, mTOR modulates numerous of important cellular processes, e.g. protein translation and autophagy, by phosphorylating its downstream molecules [9]. mTOR is the nuclear catalytic subunit of two complexes: mTORC1 and mTORC2 [1]. mTORC1 is comprised of mTOR, Raptor, mLST8, and PRAS40 (a mTOR inhibitor). This complex presented classic features of mTOR as a nutrient or energy sensor and protein synthesis conditioner [5, 10]. Low level of nutrient levels, growth factor and cellular stress inhibits the activity of mTORC1 [9, 10]. p70-S6 Kinase 1 (S6K1) and the eukaryotic initiation factor 4E (eIF4E) binding protein 1 (4E-BP1) are the best investigated targets of mTORC1 [5]. The activated mTORC1 showed a negative feedback inhibition on PI3K signaling [11]. mTORC1 could be specifically suppressed by rapamycin, as well as its allosteric ramifications. mTORC2 contains mTOR, Rictor, mLST8, and mSIN1 [12, 13]. Different from mTORC1, activated mTORC2 could induce the phosphorylation of Akt at serine 473  and serving as a positive feedback on PI3K signaling cascade [14]. Although mTORC2 was identified as a rapamycin-insensitive complex previously [14], an inhibition effect of rapamycin on free mTOR was observed in some cell lines [15]. Recent studies revealed that disordered activity of mTOR is related to some malignant and resistant cancer. The specific inhibitors, such as rapamycin and Temsirolimus(CCI-779), have been developed and trialed as novel anti-cancer agents [16, 17].

References

[1] Wullschleger, S., R. Loewith, and M.N. Hall, TOR signaling in growth and metabolism. Cell, 2006. 124(3): p. 471-84.
[2] Abraham, R.T. and J.J. Gibbons, The mammalian target of rapamycin signaling pathway: twists and turns in the road to cancer therapy. Clin Cancer Res, 2007. 13(11): p. 3109-14.
[3] Guertin, D.A. and D.M. Sabatini, Defining the role of mTOR in cancer. Cancer Cell, 2007. 12(1): p. 9-22.
[4] Avruch, J., et al., Recent advances in the regulation of the TOR pathway by insulin and nutrients. Curr Opin Clin Nutr Metab Care, 2005. 8(1): p. 67-72.
[5] Hay, N. and N. Sonenberg, Upstream and downstream of mTOR. Genes Dev, 2004. 18(16): p. 1926-45.
[6] Kimura, N., et al., A possible linkage between AMP-activated protein kinase (AMPK) and mammalian target of rapamycin (mTOR) signalling pathway. Genes Cells, 2003. 8(1): p. 65-79.
[7] O'Shea, C., et al., Adenoviral proteins mimic nutrient/growth signals to activate the mTOR pathway for viral replication. EMBO J, 2005. 24(6): p. 1211-21.
[8] Reiling, J.H. and D.M. Sabatini, Stress and mTORture signaling. Oncogene, 2006. 25(48): p. 6373-83.
[9] Fang, Y., et al., Phosphatidic acid-mediated mitogenic activation of mTOR signaling. Science, 2001. 294(5548): p. 1942-5.
[10] Kim, D.H., et al., mTOR interacts with raptor to form a nutrient-sensitive complex that signals to the cell growth machinery. Cell, 2002. 110(2): p. 163-75.
[11] Takano, A., et al., Mammalian target of rapamycin pathway regulates insulin signaling via subcellular redistribution of insulin receptor substrate 1 and integrates nutritional signals and metabolic signals of insulin. Mol Cell Biol, 2001. 21(15): p. 5050-62.
[12] Frias, M.A., et al., mSin1 is necessary for Akt/PKB phosphorylation, and its isoforms define three distinct mTORC2s. Curr Biol, 2006. 16(18): p. 1865-70.
[13] Sarbassov, D.D., et al., Rictor, a novel binding partner of mTOR, defines a rapamycin-insensitive and raptor-independent pathway that regulates the cytoskeleton. Curr Biol, 2004. 14(14): p. 1296-302.
[14] Sarbassov, D.D., et al., Phosphorylation and regulation of Akt/PKB by the rictor-mTOR complex. Science, 2005. 307(5712): p. 1098-101.
[15] Sarbassov, D.D., et al., Prolonged rapamycin treatment inhibits mTORC2 assembly and Akt/PKB. Mol Cell, 2006. 22(2): p. 159-68.
[16] Souza, E.C., A.C. Ferreira, and D.P. Carvalho, The mTOR protein as a target in thyroid cancer. Expert Opin Ther Targets, 2011. 15(9): p. 1099-112.
[17] Altman, J.K., A. Sassano, and L.C. Platanias, Targeting mTOR for the treatment of AML. New agents and new directions. Oncotarget, 2011. 2(6): p. 510-7.

Tags: mTOR inhibition | mTOR cancer | mTOR activation | mTOR target | mTOR tumor | mTOR phosphorylation | mTOR activity | mTOR inhibitor drugs | mTOR kinase assay | mTOR inhibitor cancer | mTOR inhibitor therapy | mTOR signaling pathway | mTOR inhibitor review