mIDH1-IN-2
mIDH1-IN-2 is a brain-penetrant isocitrate dehydrogenase 1 (IDH1) inhibitor. mIDH1-IN-2 shows subnanomolar potency against IDH1 R132H and R132C (IC50 = 80.0 and 58.0 nM) and minimal activity against wt-IDH1/2. mIDH1-IN-2 also inhibits PDK1 (IC50 = 0.61 μM) and reduces PDH phosphorylation dose-dependently. mIDH1-IN-2 can inhibit cells proliferation, induces S phase arrest and promotes apoptosis. mIDH1-IN-2 can be used for the research of cancer, such as glioma.
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- Formule: C18H15Br2NO4S
- Masse moléculaire:501.19
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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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Chemical Information
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Help & FAQs
Activité biologique
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R132H IDH1 80 nM (IC50) |
R132C IDH1 58 nM (IC50) |
mIDH1-IN-2 (Compound 27j) inhibits HT1080 and U87-MG cells proliferation all profile with EC50 values of 121.1 nM and 69.0 nM, respectively[1].
mIDH1-IN-2 (1-5 μM, 24-48 h) induces S phase arrest and apoptosis in U87-MG IDH1 R132H cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U87-MG IDH1 R132H cells
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Concentration:1, 2 and 5 μM
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Incubation Time:24 and 48 h
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Result:Increased the proportion of apoptotic cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Masse moléculaire 501.19
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Formule C18H15Br2NO4S
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SMILES
O=C(C1=CC=C(SC2=CC=CC(OC3CCC3)=C2)C([N+]([O-])=O)=C1)C(Br)Br
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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)
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