mTORC1-IN-3
mTORC1-IN-3 is a potent and selective mTORC1 inhibitor with an IC50 of 26.38 μM . mTORC1-IN-3 selectively inhibits the phosphorylation of mTORC1 substrates and does not without affect the phosphorylation of mTORC2 substrate. mTORC1-IN-3 can reduce cellular lipid accumulation and induce autophagy. mTORC1-IN-3 can be used for the researches of cancer, immunology, metabolic and neurological disease, such as diabetes and Alzheimer’s disease.
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- Formule: C41H43F4N11O9
- Masse moléculaire:909.84
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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mTORC1 26.38 μM (IC50) |
mTORC1-IN-3 (Compound TCG3) (10 μM, 2 h) selectively inhibits the phosphorylation of mTORC1 substrates p-p70S6K (Thr389), p-S6 (Ser235/236) and p-4E-BP1 (Thr37/46) in HepG2 cells and mouse primary hepatocytes, without affecting the phosphorylation of mTORC2 substrate p-Akt (Ser473)[1].
mTORC1-IN-3 (10 μM, 24 h) inhibits AMPK-mediated phosphorylation of ULK1 (Ser757) to reduce ULK1 activation and induces the early stage of autophagy in HepG2 cells[1].
mTORC1-IN-3 (10 μM, 24 h) reduces fatty acid-induced lipid droplet accumulation in HepG2 cells[1].
mTORC1-IN-3 (1-30 μM, 24 h) shows low cytotoxicity in HepG2 cells[1].
mTORC1-IN-3 (10 μM, 24 h) continuously inhibits mTORC1 substrate phosphorylation in HEK293T, JURKAT, and 786-O cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 cells and mouse primary hepatocytes
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Concentration:10 μM
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Incubation Time:2 h
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Result:Reduced the levels of p-p70S6K (Thr389), p-S6 (Ser235/236) and p-4E-BP1 (Thr37/46).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice (male, 6-8 weeks)[1]
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Dosage:15 mg/kg
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Administration:Intraperitoneally injection, 30 mins before insulin injection
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Result:Reversed insulin-mediated hypoglycemiaand increased plasma glucose levels.
Inhibited insulin-induced phosphorylation of mTORC1 substrates p-S6 (Ser235/236) and p-4E-BP1 (Thr37/46) in liver.
Showed a 40% reduction in p-S6 positive area.
Showed no abnormalities or hepatocyte damage in liver.
Chemical Information
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Masse moléculaire 909.84
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Formule C41H43F4N11O9
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SMILES
CC1(O[C@@H]2[C@H]([C@H](O[C@@H]2O1)CN3C=C(N=N3)COCC4=C(C5=CC(C6=CN=C(N=C6)N)=CC=C5N=C4)NC7=CC=C(C(C(F)(F)F)=C7)F)OCO[C@H]8[C@H](O[C@H]9[C@@H]8OC(C)(O9)C)CN=[N+]=[N-])C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
mTORC1-IN-3 Related Classifications
HY-178192 Related Classifications
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