mTOR

INK 128 is a TORC1/2 inhibitor, is also an orally bioavailable inhibitor of raptor-mTOR (TOR complex 1 or TORC1) and rictor-mTOR (TOR complex 2 or TORC2) with potential antineoplastic activity.

Torin1 is a potent inhibitor of mTOR with IC50 of 2-10 nM.

Torin 2 is a potent and selective mTOR inhibitor (IC50 = 2.1 nM). Displays 800-fold cellular selectivity for mTOR over PI3K (cellular EC50 values are 0.25 and 200 nM for mTOR and PI3K respectively).

PI-103 is a potent, cell-permeable, ATP-competitive inhibitor of phosphatidylinositol 3-kinase (PI3K) family members with selectivity toward DNA-PK, PI3K (p110α), and mTOR.

ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM.

WYE-354 is a potent cell-permeable inhibitor of mTOR (IC50 = 4.3 nM) which blocks signaling through both mTOR complex 1 (mTORC1) and mTORC2. It is a much weaker inhibitor of PI3K α (IC50 = 1026 nM) and other kinases.

GSK1059615 is a potent, reversible, ATP-competitive, thiazolidinedione inhibitor of PI3Kα (IC50 = 2 nM).

AZD8055 is a potent, selective, and orally bioavailable ATP-competitive mTOR kinase inhibitor with an IC50 of 0.8 nM.

GDC-0980 (RG7422) is a selective, potent, orally bioavailable inhibitor of Class I PI3 kinase and mTOR kinase (TORC1/2) with in vitro IC50 of 5, 27, 7 and 14 nM for p110 α, β, δ and γ isoforms, respectively.

BEZ235 (NVP-BEZ235) inhibits PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these enzymes.

PP242 is a potent and selective mTOR inhibitor in both mTORC1 and mTORC2.

Aloe emodin is a anthraquinone present in aloe latex, an exudate from the aloe plant. It has a strong stimulant-laxative action.

Everolimus (RAD-001) is the 40-O-(2-hydroxyethyl) derivative of sirolimus and works similarly to sirolimus as an mTOR inhibitor.

Rapamycin (Sirolimus) prevents activation of T cells and B-cells by inhibiting their response to interleukin-2 (IL-2).

AZD2014 is an orally bioavailable inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity. mTOR kinase inhibitor.

FK-506 is an immunosuppressive drug that is mainly used after allogeneic organ transplant to reduce the activity of the patient's immune system and so lower the risk of organ rejection. It reduces interleukin-2 (IL-2) production by T-cells.

PF-04691502 is a PI3K/mTOR kinase inhibitor, is also an agent targeting the phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) in the PI3K/mTOR signaling pathway.

Gedatolisib (PKI-587) is a highly potent PI3K/mTOR kinase inhibitor that inhibits PI3K-α,β,γ, δ isoforms and mTOR with IC50 of 0.4, 6.0, 5.4, 6.0 and 1.6 nM respectively.

Samotolisib (LY3023414) is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK, extracted from patent WO/2012097039A1, compound example 1, has an IC50 of 64.9 nM, 42.1 nM, 10.6 nM, 19.1 nM for Akt1(pT308), Akt1 (pS473), P70S6(pT389), S6RP(pS240/242).

Deforolimus (Ridaforolimus) is an investigational targeted and small-molecule inhibitor of the protein mTOR. Blocking mTOR creates a starvation-like effect in cancer cells by interfering with cell growth, division, metabolism, and angiogenesis.

KU-0063794 is a selective inhibitor of mammalian target of rapamycin (mTOR) (IC50 ~10 nM for mTORC1 and mTORC2 respectively).

Palomid 529 is a dual TORC1/2 inhibitor of the PI3K/Akt/mTOR pathway having broad activity in angiogenesis and cellular proliferation.

Desmethyl-VS-5584 is a demethyl analogue of VS-5584, which is a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer.

Temsirolimus is a specific inhibitor of mTOR and interferes with the synthesis of proteins that regulate proliferation, growth, and survival of tumor cells.

XL765 is a PI3K/mTOR dual kinase inhibitor and it is more potent compared to an agent that inhibits either PI3K kinase or mTOR kinase alone.

GSK2126458 is a highly potent, orally bioavailable inhibitor of PI3Kα and mTOR with in vivo activity in both pharmacodynamic and tumor growth efficacy models.

WYE-125132 is an ATP-competitive and specific inhibitor of mTORC1 and mTORC2 (IC50 = 0.19 nM; >5,000-fold selective versus PI3Ks).

OSI-027 is a potent, selective and orally bioavailable mTOR kinase inhibitor that inhibits the kinase activity associated with both the TORC1 and TORC2 complexes of mTOR.

L-LEUCINE-13C6, also known as 13C6-D-Leucine or L-Leucine-1,2,3,4,5,5'-13C6, is a fully 13C labelled D-Leucine. L-Leucine is an essential branched-chain amino acid (BCAA), which activates the mTOR signaling pathway.

Veratramine is a selective inhibitor of the PI3K/Akt/mTOR signaling pathway and serves as a modulator of SIGMAR1. This compound facilitates autophagic apoptosis in tumor cells, effectively induces G0/G1 cell cycle arrest, and diminishes epithelial-mesenchymal transition (EMT) markers, thereby reducing tumor migration. Additionally, Veratramine exhibits neuroprotective effects by inhibiting SIGMAR1 interactions with NMDAR and the phosphorylation of NMDAR Ser896, resulting in reduced neurological damage in neuropathy models. Its diverse biological activities make it suitable for research on liver cancer, osteosarcoma, and diabetic peripheral neuropathy.

Methyl Eugenol is an anti-insect agent primarily effective against the oriental fruit fly (Bactrocera dorsalis). In addition to its insecticidal properties, Methyl Eugenol exhibits anti-cancer and anti-inflammatory activities, making it a versatile compound for biological research. It has been shown to induce autophagy in cells and can be utilized in studies related to intestinal ischemia/reperfusion injury.

RMC-4745 is a selective dual-site inhibitor of mTORC1 with a 35-fold higher affinity for mTORC1 compared to mTORC2. It effectively inhibits the proliferation of MCF-7 breast cancer cells and induces apoptosis by upregulating Caspase-3/7 activity. Notably, RMC-4745 does not lead to the upregulation of HER3 due to its selective inhibition of mTORC2. This compound is valuable for research focused on breast cancer and the mechanisms underlying mTOR signaling.

FD274 is a potent dual inhibitor of PI3K and mTOR, exhibiting IC50 values of 0.65 nM for PI3Kα, 1.57 nM for PI3Kβ, 0.65 nM for PI3Kγ, 0.42 nM for PI3Kδ, and 2.03 nM for mTOR. This compound demonstrates significant anti-proliferative effects on acute myeloid leukemia (AML) cell lines, specifically HL-60 and MOLM-16, inducing G1 phase cell cycle arrest and promoting apoptosis. In vivo studies reveal dose-dependent inhibition of tumor growth in HL-60 xenograft models, making FD274 a valuable tool for research into acute myeloid leukemia therapies.

PWT-33597 free base is a dual inhibitor targeting PI3Kα and mTOR, effectively disrupting downstream signaling pathways associated with cell growth and metabolism. This compound induces apoptosis in tumor cells and demonstrates significant inhibitory effects on tumor proliferation. PWT-33597 free base is applicable in research focused on various tumors, including renal cell carcinoma, making it a valuable tool for cancer studies.

HSP90/mTOR-IN-1 is a potent inhibitor targeting both Hsp90 and mTOR, exhibiting IC50 values of 69 nM and 29 nM, respectively. This compound effectively suppresses the proliferation of SW780 cells by over-activating the PI3K/AKT/mTOR signaling pathway. In addition to inducing apoptosis and autophagy through selective inhibition, HSP90/mTOR-IN-1 demonstrates significant in vivo anti-tumor activity. It serves as a valuable reagent for research applications focused on bladder cancer.

PWT-33597 is a potent dual inhibitor of PI3Kα and mTOR, effectively disrupting downstream signaling pathways associated with cell growth and survival. This reagent induces apoptosis in tumor cells and demonstrates significant anti-tumor activity. PWT-33597 is a valuable tool for research into various malignancies, including renal cell carcinoma, providing insights into tumor biology and therapeutic strategies.

MT-44 is a potent and selective inhibitor of the mechanistic target of rapamycin (mTOR), exhibiting an IC50 of 49.4 nM. It effectively inhibits cancer cell proliferation, migration, and invasion, while inducing apoptosis and increasing reactive oxygen species (ROS) production. MT-44 also causes G2/M phase cell cycle arrest and activates the cGAS/STING signaling pathway. This compound is valuable for cancer research, particularly in the study of triple-negative breast cancer.

Lipoteichoic acid is an orally active compound with anti-inflammatory and antitumor properties. It is a key immune molecule found in Gram-positive bacteria that activates the complement system by upregulating C3 and inhibiting CD55. Lipoteichoic acid modulates macrophage autophagy via the PI3K/Akt/mTOR pathway, induces lung injury in mouse models, and inhibits melanin production.

PI3K/Akt/mTOR-IN-2 is an inhibitor of the PI3K/AKT/mTOR signaling pathway with demonstrated anticancer activity. It selectively inhibits the proliferation of MDA-MB-231 cells with an IC50 of 2.29 μM and induces cell cycle arrest and apoptosis, making it a promising candidate for cancer research.

AT-533 is a potent inhibitor of heat shock protein 90 (Hsp90) and herpes simplex virus (HSV), exhibiting strong antitumor and antiviral activities. It suppresses tumor growth and angiogenesis by disrupting the HIF-1α/VEGF/VEGFR-2 signaling axis, a critical pathway in tumor vascularization and progression. Additionally, AT-533 inhibits key downstream signaling cascades, including Akt/mTOR/p70S6K, ERK1/2, and FAK pathways. In endothelial cells, specifically human umbilical vein endothelial cells (HUVECs), AT-533 effectively inhibits tube formation, cell migration, and invasion, highlighting its anti-angiogenic properties. These combined effects position AT-533 as a promising candidate for cancer therapy and angiogenesis-related disease research.

AR420626 is a selective agonist of free fatty acid receptor 3 (FFAR3, also known as GPR41), with an IC₅₀ of 117 nM. It demonstrates anti-inflammatory, antitumor, and antidiabetic activities. AR420626 improves neurogenic diarrhea by modulating neural pathways mediated by nicotinic acetylcholine receptors (nAChRs). In cancer models, it suppresses the growth of HepG2 xenografts and inhibits hepatoma cell proliferation through apoptosis induction. Additionally, AR420626 mitigates allergic asthma and eczema and enhances glucose uptake by activating FFAR3-mediated Ca²⁺ signaling, offering potential therapeutic benefits in metabolic disorders such as diabetes.

Ovalitenone is a flavonoid compound known to inhibit the mTOR signaling pathway. This compound demonstrates significant anti-cancer activity, as it effectively reduces anchorage-independent growth and suppresses the migration and invasion of cancer cells without inducing cytotoxicity in lung cancer cell lines H460 and A549. Ovalitenone modulates epithelial-mesenchymal transition (EMT) by decreasing N-cadherin, snail, and slug levels while promoting E-cadherin expression. Additionally, it inhibits signaling pathways associated with focal adhesion kinase (FAK), ATP-dependent tyrosine kinase (AKT), and cell division cycle 42 (Cdc42), making it a valuable reagent for cancer research applications.

PI3K/Akt/mTOR-IN-3 is a potent inhibitor targeting the PI3K/AKT/mTOR signaling pathway. It demonstrates significant biological activity, exhibiting IC50 values of 0.77 μM, 1.23 μM, and 4.57 μM in MCF-7, HeLa, and HepG2 cells, respectively. Additionally, this compound effectively inhibits the migration of MCF-7 and HeLa cells at a concentration of 4 μM, while also inducing apoptosis and causing cell cycle arrest in the S phase. This makes PI3K/Akt/mTOR-IN-3 a valuable tool for research in cancer biology and therapeutic development.

Anticancer agent 235 is a modulator of the PI3K/AKT/mTOR signaling pathway. It promotes reactive oxygen species (ROS) generation and decreases mitochondrial membrane potential, leading to reduced proliferation of cancer cell lines including HCT116, Caco-2, AGS, and SMMC-772 with IC50 values ranging from 0.35 to 26.9 μM. Furthermore, Anticancer agent 235 effectively induces G2/M cell cycle arrest and apoptosis in HCT116 cells, making it a valuable tool for cancer research applications.

Royleanone, a diterpenoid isolated from plants, inhibits the proliferation of cancer cells by inducing cell cycle arrest and mitochondria-mediated apoptosis, also inhibits cell migration potential, inhibits mTOR/PI3/AKT signaling pathway in LNCaP prostate cancer cells.

Calebin A is a potent inhibitor of the PI3K/Akt/mTOR pathway, as well as MAPK and NF-κB signaling pathways. It exhibits significant anti-tumor activity through epigenetic regulation and can suppress apoptosis while inhibiting autophagy. Additionally, Calebin A modulates adipogenesis, enhances thermogenic processes, and supports gut microbiota. This compound is suitable for research in various domains, including osteoarthritis, Alzheimer's disease, type 2 diabetes, malignant peripheral nerve sheath tumors, and colorectal cancer.

22-(4′-py)-JA is a semisynthetic derivative of junamycin A, primarily targeting the AKT/mTOR/p70S6K signaling pathway. This compound exhibits significant antimetastatic activity by inhibiting tumor cell invasion and tube formation in human umbilical vein endothelial cells (HUVEC). Furthermore, 22-(4′-py)-JA downregulates key factors including metalloproteinases (MMP-2 and MMP-9), hypoxia-inducible factor 1α (HIF-1α), and vascular endothelial growth factor (VEGF). Its potent anticancer properties make it a valuable tool for research, particularly in non-small cell lung cancer (NSCLC) studies.

DHW-221 is a potent dual inhibitor of PI3K and mTOR, demonstrating low nanomolar potency across all four Class I PI3K isoforms (PI3Kα, IC50 = 0.50 nM; PI3Kβ, IC50 = 1.9 nM; PI3Kγ, IC50 = 1.8 nM; PI3Kδ, IC50 = 0.74 nM) and mTOR (IC50 = 3.9 nM). This compound exhibits significant antitumor activity by disrupting the PI3K/Akt/mTOR signaling pathway, promoting mitochondrial apoptosis and paraptosis via endoplasmic reticulum stress and MAPK signaling, while also hindering cell cycle progression, migration, invasion, and angiogenesis. DHW-221 serves as a valuable tool in research related to non-small cell lung cancer (NSCLC), colon cancer, and breast cancer.

IBL-302 is an orally available dual inhibitor targeting PIM and the PI3K/AKT/mTOR pathways. It exhibits significant antitumor activity against breast cancer and neuroblastoma, showing in vivo efficacy in nude mouse xenograft models by overcoming trastuzumab resistance. Additionally, IBL-302 enhances the cytotoxic effects of commonly used chemotherapeutic agents, including cisplatin, doxorubicin, and etoposide, making it a valuable compound for cancer research applications.

MKC-1 is an orally active and potent inhibitor targeting the Akt/mTOR signaling pathway. This compound exhibits broad antitumor activity by arresting cellular mitosis and inducing apoptosis. MKC-1 interacts with various cellular proteins, including tubulin and members of the importin β family, making it valuable for research in cancer cell cycle regulation and therapeutic mechanisms.