mTOR Inhibitor

GNE-493 is a potent, selective, and orally available dual pan-PI3-kinase/mTOR inhibitor with IC₅₀s of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR.

PI3K/mTOR Inhibitor-2 is a potent dual pan-PI3K/mTOR inhibitor with IC₅₀s of 3.4/34/16/1 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ and 4.7 nM for mTOR. Antitumor activity.

PKI-179 is a potent and orally active dual PI3K/mTOR inhibitor, with IC₅₀s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 also exhibits activity over E545K and H1047R, with IC₅₀s of 14 nM and 11 nM, respectively. PKI-179 shows anti-tumor activity in vivo.

Ifupinostat (BEBT-908) is a blood-brain barrier-permeable PI3K/HDAC inhibitor. Ifupinostat exerts anticancer activity against hematologic malignancies, lung cancer, colon cancer, brain cancer and other cancers. Ifupinostat inhibits the PI3K/AKT/mTOR signaling pathway, suppresses c-Myc expression and induces ferroptosis. Ifupinostat can be used in tumor research.

L-Glutamine-1-¹³C is the ¹³C-labeled L-Glutamine (HY-N0390). L-Glutamine is an orally active nutritional agent and cellular metabolism regulator. L-Glutamine is taken up in a Na⁺-dependent manner and targets multiple key molecules including glutaminase, mTORC1, NF-κB, STAT-3 and HIF-1α. L-Glutamine enhances glutaminolytic catabolism, drives the conversion of glutamate to α-ketoglutarate, thereby regulating gene expression, integrating metabolic signals, mediating glutamine flux and maintaining redox homeostasis. L-Glutamine also promotes cell proliferation, osteogenic differentiation and fracture healing, exerts neuroprotective and cardioprotective effects, and inhibits osteoarthritis. L-Glutamine can be applied to research related to osteoporosis, osteoarthritis, ischemic stroke and acute cantharidin-induced cardiotoxicity.

Guaiazulene is a bicyclic sesquiterpene. Guaiazulene exhibits various biological activities such as anti-inflammatory, antioxidant, hepatoprotective, antibacterial, and anti-tumor properties. Guaiazulene is also commonly used as a colorant in cosmetics. Guaiazulene shows in vitro cytotoxicity to rat neuronal cells and N2a neuroblastoma cells at high concentrations.

Curzerenone is an orally active sesquiterpene compound and Antibacterial agent. Curzerenone can be isolated from Curcuma zedoaria and Curcuma aeruginosa plants. Curzerenone increases ROS levels, activates Apoptotic signaling pathways, and attenuates the PI3K/AKT/mTOR signaling pathway. Curzerenone exhibits anticancer activity against liver cancer and cervical cancer. Curzerenone has antioxidant effects. Curzerenone shows weak antibacterial activity against Escherichia coli. Curzerenone can be used in research related to hepatocellular carcinoma, cervical cancer, and Escherichia coli infection.

Dammarenediol II is a ginsenoside precursor. Dammarenediol II reduces the activity of O-GlcNAc transferase (OGT) and downregulates the global O-GlcNAcylation level. Dammarenediol II inhibits the phosphorylation of Akt, mTOR and GSK3β. Dammarenediol II inhibits human carboxylesterase activity, VEGF-induced ROS production, stress fiber formation and vascular endothelial cadherin disruption. Dammarenediol II promotes cell apoptosis (apoptosis), increases the levels of cleaved PARP1 and p53, and inhibits retinal microvascular leakage. Dammarenediol II can be used in studies related to liver cancer and diabetic retinopathy.

WAY-600 is a potent, ATP-competitive, and selective mTOR inhibitor with an IC₅₀ of 9 nM for recombinant mTOR enzyme. WAY-600 blocks mTOR complex 1/2 (mTORC1/2) assemble and activation.

HDACs/mTOR Inhibitor 1 is a dual HDACs and mTOR inhibitor, with IC₅₀s of 0.19 nM, 1.8 nM, 1.2 nM for HDAC1, HDAC6, mTOR, respectively. HDACs/mTOR Inhibitor 1 stimulates cell cycle arrest in G0/G1 phase and induces tumor cell apoptosis with low toxicity in vivo. HDACs/mTOR Inhibitor 1 can be used in the research of hematologic malignancies.

WYE-354 is an ATP-competitive mTOR inhibitor with an IC₅₀ of 5 nM. WYE-354 also inhibits PI3Kα and PI3Kγ with IC₅₀s of 1.89 μM and 7.37 μM, respectively. WYE-354 inhibits both mTORC1 and mTORC2. WYE-354 induces autophagy activation in vitro.

mTOR inhibitor-1 (Compound C-4) is an ATP-Competitive mTOR inhibitor which can suppress cells proliferation and inducing autophagy.

Simufilam hydrochloride (PTI-125 hydrochloride) is an orally active FLNA modulator. Simufilam hydrochloride restores NMDAR signaling and Arc expression. Simufilam hydrochloride inhibits overactive mTOR signaling by restoring the normal conformation of FLNA, improves insulin sensitivity, reduces Aβ₄₂-induced neuroinflammation and tau protein hyperphosphorylation. Simufilam hydrochloride can be used for research of Alzheimer's disease.

HZX-02-059 is an allosteric inhibitor of PIKFYVE, and a methuosis inducer. HZX-02-059 disrupts the PIKfyve/TFEB axis, suppresses tubulin polymerization, reduces phosphorylated mTOR levels, downregulates p53, PI3K/AKT, c-Myc, and NF-κB pathways. HZX-02-059 induces G₂/M cell cycle arrest, apoptosis, and inhibits cancer cell proliferation. HZX-02-059 can be used for the research of lymphoma, double-hit lymphoma, and B-cell acute lymphoblastic leukemia.

PQR626, a rapamycin derivative, is a potent, selective, orally active, and brain-penetrant mTOR inhibitor, with an IC₅₀ and K_i of 5 nM and 3.6 nM, respectively. PQR626 can be can be used for the research of neurological disorders.

GDC-0349 is a potent and selective ATP-competitive mTOR inhibitor with a K_i of 3.8 nM. GDC-0349 inhibits of both mTORC1 and mTORC2 complexes.

Rotundic acid is an orally effective triterpenoid with a K_d value of 51.3 µM for PTP1B. Rotundic acid downregulates the AKT/mTOR pro-survival pathway and modulates the MAPK pathway. Rotundic acid induces cell cycle S-phase arrest, DNA damage and apoptosis; it inhibits migration, invasion, angiogenesis and proliferation of cancer cells. Rotundic acid improves leptin sensitivity, regulates gut microbiota and reduces cellular senescence. Rotundic acid can be used in research related to hepatocellular carcinoma, obesity, aging, acute lung injury and type 2 diabetes.

MTI-31 (LXI-15029) is a potent, orally active and highly selective inhibitor of mTORC1 and mTORC2. MTI-31 is selective for mTOR (K_d: 0.20 nM) versus PIK3CA, PIK3CB and PIK3G with >5,000 fold selectivity in mTOR binding assays. MTI-31 shows an IC₅₀ of 39 nM for mTOR in LANCE assay of mTOR substrate phosphorylation with 100 μM ATP. MTI-31 can be used for the research of breast cancer.

Tegafur-gimeracil-oteracil potassium (S-1; TS-1) is an orally active anticancer agent composed of Tegafur (HY-17400), Gimeracil (HY-17469), and Oteracil potassium (HY-17511). Tegafur-gimeracil-oteracil potassium inhibits the proliferation, migration and invasion of endometrial cancer cells and induces apoptosis by blocking the PI3K/AKT/mTOR signaling pathway. Tegafur-gimeracil-oteracil potassium can be used in research related to endometrial cancer and gastric cancer with peritoneal metastasis.

Arnicolide D is a sesquiterpene lactone that can be isolated from Centipeda minima. Arnicolide D is cytotoxic to tumor cells and can induce cell cycle arrest, apoptosis, and oncosis in tumor cells. Arnicolide D has anti-tumor activity.