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mTOR

The mammalian target of rapamycin (mTOR), sometimes also referred to as the mechanistic target of rapamycin and FK506-binding protein 12-rapamycin-associated protein 1 (FRAP1), is a kinase that in humans is encoded by the MTOR gene. mTOR is a member of the phosphatidylinositol 3-kinase-related kinase family of protein kinases.mTOR links with other proteins and serves as a core component of two distinct protein complexes, mTOR complex 1 and mTOR complex 2, which regulate different cellular processes. In particular, as a core component of both complexes, mTOR functions as a serine/threonine protein kinase that regulates cell growth, cell proliferation, cell motility, cell survival, protein synthesis, autophagy, and transcription. As a core component of mTORC2, mTOR also functions as a tyrosine protein kinase that promotes the activation of insulin receptors and insulin-like growth factor 1 receptors. mTORC2 has also been implicated in the control and maintenance of the actin cytoskeleton.

Capivasertib
T19201143532-39-1
Capivasertib (AZD5363) is a broad-spectrum AKT inhibitor with inhibitory activity against Akt1, Akt2, and Akt3 (IC50=3 7 7 nM) with oral activity. Capivasertib has antitumor activity for the treatment of breast cancer.
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NV-5138
T122702095886-80-7In house
NV-5138 is a selective, orally active intracerebral mTORC1 agonist that binds to Sestrin2. It is a leucine analog. It can be used in biological studies of antidepressants.
  • $91
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hSMG-1 inhibitor 11j
T88841402452-15-6In house
hSMG-1 inhibitor 11j is a pyrimidine derivative. hSMG-1 inhibitor 11j is a potent and selective inhibitor of hSMG-1, IC50 = 0.11 nM. hSMG-1 inhibitor 11j exhibits >455-fold selectivity for hSMG-1 over mTOR (IC50=50 nM), PI3Kα γ (IC50=92 60 nM) and CDK1 CDK2 (IC50=32 7.1 μM). hSMG-1 inhibitor 11j can be used for the research of cancer.
  • $163 TargetMol
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Everolimus
T1784159351-69-6
Everolimus (SDZ-RAD) is a potent mTOR inhibitor that binds to FKBP-12. It is used alone or in combination with calcineurin inhibitors.
  • $37
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Tacrolimus
T2144104987-11-3
Tacrolimus (Fujimycin) can bind FKBP12 to form a high-affinity complex (Ki: 0.2 nM) which inhibits the activity of the calcium calmodulin-dependent protein phosphatase.
  • $38
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Polyphyllin I
T389550773-41-6
Polyphyllin D induces apoptosis via the mitochondrial apoptotic pathway as evidenced by decreased Bcl-2 expression levels, disruption of MMP and increased Bax, cytochrome C, and cleaved-caspase-3 levels. Polyphyllin D has an anti-angiogenic effect. Polyphyllin D has toxicity in human RBCs as well as its underlying mechanism for the hemolysis and eryptosis erythroptosis. Polyphyllin D has strong anticancer activity, can overcome drug resistance in R-HepG2 cells and elicit programmed cell death via mitochondrial dysfunction.
  • $52
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Torin 1
T60451222998-36-8
Torin 1 is an effective inhibitor of mTORC1/2 with (IC50: 2 nM/10 nM); has 1000-fold selectivity for mTOR than PI3K.
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Vincristine
T3S020957-22-7
Vincristine binds to tubulin and inhibits the formation of microtubules, thereby inhibiting mitosis of the cancer cell. Vincristine can be used as a microtubule-destabilizing agent for research on the treatment of hematologic cancers, such as leukemia and
  • $148
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Timosaponin AIII
T339541059-79-4
Timosaponin AIII (Timosaponin A3) induces autophagy in HeLa cells followed by apoptotic cell death (IC50: 10 μM). The Timosaponin AIII cellular response is mediated via inhibition of mTORC1 and induction of ER stress (IC50: 2.5 μM, BT474 cells; 6 μM, MDAMB231). The Timosaponin AIII pro-apoptotic response is selective for tumor cells over normal cells but autophagy is induced in both.
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Salidroside
T271710338-51-9
Salidroside is a bioactive phenolic glycoside compound isolated from Rhodiola rosea and is a prolyl endopeptidase inhibitor. Salidroside can alleviate cachexia symptoms in a tumor cachexia mouse model by activating mTOR signaling and protect dopaminergic neurons by enhancing PINK1 Parkin-mediated mitochondrial autophagy. Salidroside can also inhibit the growth of cancer cells by regulating the CDK4-cyclin D1 pathway to block the G1 phase and or regulating the Cdc2-cyclin B1 pathway to block the G2 phase.
  • $52
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JR-AB2-011
T117282411853-34-2
JR-AB2-011 is a selective mTORC2 inhibitor with an IC50 value of 0.36 μM. It inhibits mTORC2 activity by blocking Rictor-mTOR association (Ki: 0.19 μM) and exhibits cytotoxicity in glioblastoma [1].
  • $87
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PI3Kα/mTOR-IN-1
T125891013098-90-2In house
PI3Kα mTOR-IN-1 is a potent dual inhibitor of PI3Kα mTOR, with an IC50 of 7 nM for PI3Kα in a cell assay and Kis of 12.5 nM and 10.6 nM for mTOR and PI3Kα [in a cell-free assay], respectively.
  • $656
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GNE-477
T36921032754-81-6
GNE-477 is a potent and efficacious dual (PI3K mTOR) inhibitor.
  • $64
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Temsirolimus
T2145162635-04-3
Temsirolimus (CCI-779) is a specific mTOR inhibitor ( IC50: 1.76 μM), used in the treatment of advanced renal cell cancer.
  • $38
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MHY1485
T1908326914-06-1
MHY1485 is an mTOR activator that is cell-permeable. MHY1485 inhibits autophagosome and lysosome fusion, leading to accumulation of LC3II proteins and increased autophagosomes, thereby inhibiting cellular autophagy.
  • $43
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AZD-8055
T18591009298-09-2
AZD8055 is an ATP-competitive mTOR inhibitor (IC50: 0.8 nM in MDA-MB-468 cells). It is ~1,000-fold selective for mTOR over all PI3K isoforms.
  • $36
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Gedatolisib
T19701197160-78-3
Gedatolisib (PF-05212384) is a highly effective dual inhibitor targeting the PI3Kα/γ (IC50: 0.4/5.4 nM)and mTOR (IC50: 1.6 nM) in the PI3K/mTOR signaling pathway.
  • $45
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Dihydromyricetin
T299827200-12-0
Dihydromyricetin (Ampelopsin) is a natural antioxidant flavonoid from Ampelopsis grossedentata. Dihydromyricetin is a potent inhibitor of dihydropyrimidinase with an IC50 of 48 μM. Dihydromyricetin can activate autophagy by inhibiting mTOR signaling.
  • $39
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Jolkinolide B
T2S104037905-08-1
Jolkinolide B is a bioactive diterpene isolated from the roots of Euphorbia fischeriana Steud. Jolkinolide B induces apoptosis in cancer cells. Jolkinolide B can be used for studies on preventing and treating osteolysis.
  • $60
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Sapanisertib
T18381224844-38-5
Sapanisertib (INK 128) is an orally bioavailable inhibitor of raptor-mTOR (TOR complex 1 or TORC1) and rictor-mTOR (TOR complex 2 or TORC2) with potential antineoplastic activity.
  • $34
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MTI-31
T353431567915-38-1
MTI-31 (LXI-15029) is a potent, orally active, and highly selective inhibitor of mTORC1 and mTORC2, exhibiting a Kd of 0.20 nM for mTOR and >5,000-fold selectivity over PIK3CA, PIK3CB, and PIK3G in binding assays, with an IC50 of 39 nM for mTOR in a LANCE assay of mTOR substrate phosphorylation with 100 μM ATP [1].
  • $197
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mTOR inhibitor 13
T93101144075-44-4In house
mTOR inhibitor 13 is a selective mTOR inhibitor with IC50 of 0.29nM and 119nM for mTOR and PI3Kα, respectively.
  • $197
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Omipalisib
T18611086062-66-9
Omipalisib (GSK2126458) is a small-molecule pyridylsulfonamide inhibitor of phosphatidylinositol 3-kinase (PI3K) with potential antineoplastic activity.
  • $57
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Copanlisib dihydrochloride
T149981402152-13-9
Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is an ATP-competitive pan-class I PI3K inhibitor, with IC50 values of 0.5 nM for PI3Kα, 0.7 nM for PI3Kδ, 3.7 nM for PI3Kβ, and 6.4 nM for PI3Kγ. It exhibits superior antitumor activity and demonstrates more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR.
  • $47
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KU-0063794
T2475938440-64-3
KU-0063794 is a potent and highly specific dual inhibitor of mTORC1 and mTORC2.
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Torin 2
T61001223001-51-1
Torin 2(IC50=0.25 nM), a specific and effective mTOR inhibitor, is the 800-fold greater specific activity for mTOR than PI3K and improves pharmacokinetic properties. The EC50 of Torin 2 for ATM ATR DNA-PK inhibition is 28 nM 35 nM 118 nM, respectively.
  • $35
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3BDO
T14033890405-51-3
3BDO is an activator of mTOR. It can also inhibit autophagy..
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KU-55933
T2685587871-26-9
KU-55933 (ATM Kinase Inhibitor) is an ATM inhibitor (IC50=12.9 nM; Ki=2.2 nM) that is selective and ATP-competitive. KU-55933 induces apoptosis and has antitumor effects.
  • $43
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BGT226
T6072L915020-55-2In house
BGT226 (NVP-BGT226) is a novel dual PI3K mTOR inhibitor, targeting PI3K α, β, and γ with IC50 values of 4 nM, 63 nM, and 38 nM, respectively.
  • $48
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AZD 3147
T362001101810-02-9
AZD 3147 is an inhibitor of mTORC with IC50s of 40.7 and 5.75 nM for mTORC1 and mTORC2. AZD 3147 shows IC50s of 912, 5495, 9333, and 6310 nM for PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively.
  • $98
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Cbz-B3A
T148861884710-81-9In house
Cbz-B3A is a potent inhibitor of mTORC1 signalling, inhibits phosphorylation of eIF4E-binding protein 1 (4EBP1) and blocks translation by 68%.
  • $108 TargetMol
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Ridaforolimus
T6334572924-54-0
Ridaforolimus (AP23573) is a small molecule and non-prodrug analogue of the lipophilic macrolide antibiotic rapamycin with potential antitumor activity. Ridaforolimus binds to and inhibits the mammalian target of rapamycin (mTOR), which may result in cell cycle arrest and, consequently, the inhibition of tumor cell growth and proliferation. Upregulated in some tumors, mTOR is a serine/threonine kinase involved in regulating cellular proliferation, motility, and survival that is located downstream of the PI3K/Akt signaling pathway.
  • $51
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Dactolisib
T2235915019-65-7
Dactolisib (BEZ235) is an orally bioavailable inhibitor of PI3K and mTOR, with IC50 values of 4 nM for p110α, 5 nM for p110γ, 7 nM for p110δ, 75 nM for p110β, and 20.7 nM for mTOR.
  • $39
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PI-103
T6143371935-74-9
PI-103 is a potent, cell-permeable, ATP-competitive inhibitor of PI3K family members (IC50s: 2/3/3/15/30/23 nM for p110α/β/δ/γ, mTOR, and DNA-PK).
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Samotolisib
T68831386874-06-1
Samotolisib (LY3023414) is an oral ATP competitive inhibitor of the class I PI3K isoforms, DNA-PK, and mTOR. Samotolisib (LY3023414) has been used in trials studying the treatment of Neoplasm, Solid Tumor, COLON CANCER, BREAST CANCER, and Advanced Cancer, among others.
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MKC-1
T9831125313-92-0In house
MKC-1 (Ro-31-7453) is an orally bioavailable small-molecule bisindolylmaleimide cell cycle inhibitor with potential antineoplastic activity. MKC-1 and its metabolites inhibit tubulin polymerization, blocking mitotic spindle formation, which may result in apoptosis and tumor cell death.
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Hederacolchiside A1
T2P2806106577-39-3
Hederacolchiside A1 (Raddeanoside R13) shows anti-leishmanial activity, it exhibits a strong antiproliferative activity on all stages of development of the parasite by altering membrane integrity and potential. Hederacolchiside A1 shows antiproliferation activities in three cancer cell lines with the IC50 value of 2.4 uM, it exhibits a preferential cytotoxicity on a pigmented melanoma cell line. It suppresses proliferation of tumor cells by inducing apoptosis through modulating PI3K Akt mTOR signaling pathway.
  • $40
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GNE-317
T68451394076-92-6
GNE-317, a PI3K mTOR inhibitor, can pass through the blood-brain barrier (BBB).
  • $33
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Vistusertib
T19611009298-59-2
Vistusertib (AZD2014) is an orally bioavailable inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity.
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DS-7423
T360831222104-37-1
DS-7423 is a dual PI3K and mTOR inhibitor, with IC50 values of 15.6 nM and 34.9 nM for PI3Kα and mTOR, respectively, and exhibits anti-tumor activity[1][2]. It increases TP53 expression, the level of p-TP53 on Ser-46, and induces apoptosis-related TP53 target genes (TP53AIP1 and PUMA) in OCCC cells[1]. DS-7423 also inhibits other isoforms of class I PI3K with IC50 values of 1,143 nM for PI3Kβ, 249 nM for PI3Kγ, and 262 nM for PI3Kδ[2]. [1]. Katsutoshi Oda, et al. Characterization of TP53 and PI3K signaling pathways as molecular targets in gynecologic malignancies. J Obstet Gynaecol Res. 2016 Jul;42(7):757-62. [2]. Tomoko Kashiyama, et al. Antitumor activity and induction of TP53-dependent apoptosis toward ovarian clear cell adenocarcinoma by the dual PI3K mTOR inhibitor DS-7423. PLoS One. 2014 Feb 4;9(2):e87220.
  • $129
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Rheb inhibitor NR1
T167412216763-38-9
Rheb inhibitor NR1 is a selective mTORC1 inhibitor that suppresses the phosphorylation of T389pS6K1 and enhances the phosphorylation of S473pAKT.
  • $84
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OSI-027
T6319936890-98-1
OSI-027 (ASP4786) is a selective and potent dual inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM, and more than 100-fold selectivity observed for mTOR than PI3Kα, PI3Kβ, PI3Kγ or DNA-PK. Phase 1.
  • $35
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GSK-25
T4488874119-56-9
GSK-25 maintains good selectivity against a panel of 31 kinases, as well as RSK1 and p70S6K (RSK1 IC50 of 398 nM, p70S6K IC50 of 1000nM), and a dramatically improved P450 profile (>2.2 uM at all isozymes tested).
  • $39
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PI3K/Akt/mTOR-IN-2
T605642757804-89-8In house
PI3K Akt mTOR-IN-2 is a potent PI3K AKT mTOR inhibitor with anticancer effects and selectivity for MDA-MB-231 cells (IC50 2.29 μM). It induces cell cycle arrest and apoptosis in cancer cells.
  • $33
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Palomid 529
T2706914913-88-5
Palomid 529 (SG 00529) has been used in trials studying the treatment of Age-Related Macular Degeneration.
  • $40
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GDC0084
T37051382979-44-3
GDC0084 (RG7666) is a PI3K inhibitor with potential antineoplastic activity. GDC0084 (RG7666) specifically inhibits PI3K in the PI3K AKT kinase (or protein kinase B) signaling pathway, thereby inhibiting the activation of the PI3K signaling pathway. This may result in the inhibition of both cell growth and survival in susceptible tumor cell populations.
  • $36
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D-α-Hydroxyglutaric acid disodium
T6820103404-90-6
D-α-Hydroxyglutaric acid disodium [Disodium (R)-2-Hydroxyglutarate] is a competitive inhibitor of α-ketoglutarate-dependent dioxygenases with a Ki of 0.628 mM.
  • $30
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Torkinib
T24141092351-67-1
Torkinib (PP 242) (PP 242) is a selective and ATP-competitive mTOR inhibitor (IC50: 8 nM). It also inhibits mTORC1 2 (IC50s: 30 58 nM).
  • $52
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