mTOR inhibitor-8

• CAT Number: I045760
• CAS Number: 2489196-70-3
• Molecular Formula: C24H19ClN4OS
• Molecular Weight: 446.95
• Purity: ≥95%
• Synonyms: 2-[5-(4-chlorophenyl)-3-(4-methoxyphenyl)-3,4-dihydropyrazol-2-yl]-4-pyridin-4-yl-1,3-thiazole
• InChI: InChI=1S/C24H19ClN4OS/c1-30-20-8-4-18(5-9-20)23-14-21(16-2-6-19(25)7-3-16)28-29(23)24-27-22(15-31-24)17-10-12-26-13-11-17/h2-13,15,23H,14H2,1H3
• InChIKey: YYORGGAMBAZQIJ-UHFFFAOYSA-N
• SMILES: COC1=CC=C(C=C1)C2CC(=NN2C3=NC(=CS3)C4=CC=NC=C4)C5=CC=C(C=C5)Cl

mTOR inhibitor-8 is an mTOR inhibitor and autophagy inducer. mTOR inhibitor-8 inhibits the activity of mTOR via FKBP12 and induces autophagy of A549 human lung cancer cells[1].
mTOR inhibitor-8 (Compound 5e; 0.1-10 μM; 24 and 48 hours) suppresses the growth of A549 cells in a dose-dependent manner[1].
mTOR inhibitor-8 induces autophagy in an mTOR-dependent manner. mTOR inhibitor-8 (10 μM; 3-24 hours) induces autophagy in a time-dependent manner. The levels of LC3B-II are enhanced[1].
mTOR inhibitor-8 (10 μM; 3-24 hours) reduces the phosphorylation of RPS6KB1 (ribosomal protein S6 kinase) and EIF4EBP1 (eukaryotic translation initiation factor 4E-binding protein 1), two essential substrates of mTOR[1]
mTOR inhibitor-8 (25 and 50 μM; 6 days) effectively inhibits tumor growth in vivo without adverse effect on normal chick chorioallantoic membrane angiogenesis[1].

Reference

[1]. ZhaoMin Lin, et al. Discovery of new fluorescent thiazole-pyrazoline derivatives as autophagy inducers by inhibiting mTOR activity in A549 human lung cancer cells. Cell Death Dis. 2020 Jul 20;11(7):551.
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