mtor inhibitor-12

mTOR inhibitor-12 (Compound 11), a selective, brain-penetrant mTOR inhibitor, exhibits no genotoxicity risk and is utilized in research pertaining to central nervous system (CNS) diseases [1].

PI3K/mTOR Inhibitor-12, a potent and selective orally active inhibitor, exhibits IC50 values of 0.06 nM for PI3Kα and 3.12 nM for mTOR, indicating significant antitumor activity with reduced liver toxicity [1].

Everolimus (SDZ-RAD) is a potent mTOR inhibitor that binds to FKBP-12. It is used alone or in combination with calcineurin inhibitors.

BMX-IN-3 (B6a) is an irreversible and selective inhibitor of BMX with an IC50 value of 12 nM. It induces cell cycle arrest and apoptosis, triggers protective autophagy, and inhibits the BMX/AKT/mTOR pathway. BMX-IN-3 (B6a) is applicable for research in gastric cancer.

PI3K/mTOR-IN-18 (Compound 12) is a highly selective dual inhibitor of PI3K/mTOR. It exerts antitumor effects through competitive binding to PI3Kα (Ki=0.130 nM) and mTOR (Ki=0.111 nM). By blocking the PI3K/AKT/mTOR pathway, PI3K/mTOR-IN-18 inhibits tumor cell proliferation (IC50=144 nM) and holds potential for research in solid tumors such as breast cancer and non-small cell lung cancer.

CAII-IN-12 (compound 6c) is a potent and selective inhibitor of carbonic anhydrase (CA) II and VII, with inhibition constants hCA II Ki= 47.8 nM and hCA VII Ki= 3.6 nM, and exhibits antiepileptic activity. It is selective for hCA I with a Ki of 370 nM. In mouse models of epilepsy induced by Pentylenetetrazol and Pilocarpine, CAII-IN-12 demonstrates strong anticonvulsant effects. Additionally, it increases the expression of KCC2 in the hippocampus, maintains neuronal integrity, and reduces mTOR activity. CAII-IN-12 is applicable for epilepsy research.

PP-121 is a multi-targeted inhibitor of PDGFR (IC50: 2 nM), Hck (IC50: 8 nM), mTOR (IC50: 10 nM), VEGFR2(IC50: 12 nM), Src (IC50: 14 nM) and Abl (IC50: 18 nM) , also inhibits DNA-PK (IC50: 60 nM).

PI3K/mTOR Inhibitor-3 (compound 12) is an imidazoline compound with potent dual inhibition of PI3K and mTOR, exhibiting notable anti-cancer activity [1].

PI3K/mTOR Inhibitor-8 is a dual inhibitor of PI3K (PI3Kα IC50: 0.46 nM) and mTOR (mTOR IC50: 12 nM). PI3K/mTOR Inhibitor-8 blocks the cell cycle of HCT-116 cells in G1/S phase and induces apoptosis. apoptosis).

GNE-493 is potent, selective, and orally available PI3K and mTOR inhibitor with potential anticancer activity.IC50s of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR,respectively.