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You are here:Home-Inhibitors & Agonists-PI3K/Akt/mTOR Pathway-mTOR

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mTOR (mammalian target of Rapamycin) is a protein that in humans is encoded by the mTOR gene. mTOR is a serine/threonine protein kinase that regulates cell growth, cell proliferation, cell motility, cell survival, protein synthesis, and transcription. mTOR belongs to the phosphatidylinositol 3-kinase-related kinase protein family. mTOR integrates the input from upstream pathways, including growth factors and amino acids. mTOR also senses cellular nutrient, oxygen, and energy levels. The mTOR pathway is dysregulated in human diseases, such as diabetes, obesity, depression, and certain cancers. Rapamycin inhibits mTOR by associating with its intracellular receptor FKBP12. The FKBP12-rapamycin complex binds directly to the FKBP12-Rapamycin Binding (FRB) domain of mTOR, inhibiting its activity.

Cat. No. Product Name CAS No. Information
H9364

NV-5138 hydrochloride

2639392-70-2

NV-5138 hydrochloride is a leucine analog, is the first selective and orally active brain mTORC1 activator, binding to Sestrin2. NV-5138 hydrochloride is used for antidepressant studies.

H9363

NV-5138

2095886-80-7

NV-5138 is a leucine analog, is the first selective and orally active brain mTORC1 activator, binding to Sestrin2. NV-5138 is used for antidepressant studies.

H9323

RMC-5552

2382768-62-7

RMC-5552 is a potent and selective inhibitor of mTORC1. RMC-5552 inhibits phosphorylation of mTORC1 pS6K and p4EBP1 with IC50s of 0.14 nM and 0.48 nM, respectively;RMC-5552 has anti-cancer activity.

H6987

Zotarolimus

221877-54-9

Zotarolimus (ABT-578, A 179578) is a semi-synthetic analogue of rapamycin, inhibits FKBP-12 binding with IC50 of 2.8 nM and shows less potent systemic immunosuppression than rapamycin; effectively inhibits both smooth muscle cell and endothelial cell proliferation, with IC50 values of 2.9 nM and 2.6 nM, respectively; exhibits high-affinity binding to the immunophilin FKBP12, inhibiting in vitro proliferation of both human and rat T cells; inhibits Con A-induced human T cells with IC50 of 7.0 nM; reduce early complications and improve late clinical outcomes in patients needing interventional cardiology.

H6986

WYE-354

1062169-56-5

WYE-354 is a potent, selective and ATP-competitive inhibitor of mTOR with IC50 of 5 nM (recombinant mTOR ), displays >100-fold selectivity over PI3K isofoms; acutely blocks substrate phosphorylation by mTORC1 and mTORC2 in vitro and in cells in response to growth factor, amino acids, and hyperactive PI3K/AKT, reduces AKT downstream function and inhibits proliferation of diverse cancer cell lines; inhibits mTORC1 and mTORC2 and displayed robust antitumor activity in PTEN-null tumors.

H6985

WYE-125132

1144068-46-1

A potent, specific, ATP-competitive and orally active mTOR inhibitor with IC50 of 0.19 nM; dispalys high selectivity (>5,000-fold) over PI3Ks, the PI3K-related kinases hSMG1 and ATR, and a panel of 230 protein kinases; inhibits mTORC1-dependent phosphorylation of S6K(T389) and mTORC2-dependent phosphorylation of AKT(S473), inhibits cancer cell proliferation, cell cycle progression, and induces apoptosis; shows potent single-agent antitumor activity against multiple cancer models.

H6984

Torin2

1223001-51-1

Torin2 is a potent, selective, orally available inhibitor of mTOR, inhibits mTORC1-dependent T389 phosphorylation on S6K with IC50 of 0.25 nM, exhibits 800-fold selectivity over PI3K, and >100-fold over 440 other protein kinases; also exhibits potent biochemical and cellular activity against PIKK family kinases including ATM (EC50=28 nM), ATR (EC50=35 nM), and DNA-PK (EC50=118 nM); inhibits mTOR kinase and mTORC1 signaling activities, results in a prolonged block in negative feedback and consequent T308 phosphorylation on Akt in treated cancer cells; demonstrates significant growth inhibition against KRAS-driven lung tumors combined with MEK inhibitor AZD6244, does not yield significant efficacy as a single agent; overcomes the resistance of ALK(F1174L)/MYCN tumors to crizotinib in vivo.

H6983

Torin1

1222998-36-8

Torin1 is a highly potent, selective inhibitor of mTORC1 and mTORC2 with IC50 of 2 and 10 nM in cell-free assays, exhibits 1,000-fold selectivity PI3K (EC50=1,800 nM); exhibits 100-fold binding selectivity relative to 450 other protein kinases; causes cell cycle arrest through a rapamycin-resistant mechanism that is also independent of mTORC2, disrupts mTORC1-dependent phenotypes more completely than rapamycin; prevents the anti-inflammatory potency of GC both in human monocytes and myeloid dendritic cells.

H6982

Temsirolimus

162635-04-3

A rapamycin ester and mTOR inhibitor with biochemical IC50 of 1.74 uM; reduces global protein synthesis and disassembly of polyribosomes, increases the phosphorylation of eEF2 and the translation initiation factor eIF2 alpha, inhibits mTOR signaling through an FKBP12-independent mechanism in cancer cells; reduces neoplasia and normalizes p70/S6 kinase activity in Pten+/- mice, with no effect on Akt.

H6981

Seco Rapamycin sodium salt

148554-65-8

Seco-rapamycin is the first in vivo open-ring metabolite of rapamycin that does not affect mTOR.

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