IDO1-IN-34
IDO1-IN-34 is a selective IDO1 inhibitor with an IC50 of 0.093 μM. IDO1-IN-34 exhibits cytotoxicity against various cancer cell lines. IDO1-IN-34 inhibits the kynurenine (kynurenine) pathway and activates IL-2. IDO1-IN-34 induces cell apoptosis via the endogenous mitochondrial pathway, while increasing the levels of cytochrome c, caspase-3, caspase-9 and PARP-1. IDO1-IN-34 can be used for research on liver cancer, lung cancer, breast cancer, prostate cancer, colon cancer and leukemia.
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- Formule: C18H10BrF7N4O2
- Masse moléculaire:527.19
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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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IDO1 0.093 μM (IC50) |
IL-2 |
Caspase-9 |
Caspase-3 |
PARP-1 |
IDO1-IN-34 (Compound 3b) (0.1-100 μM; 48 h) exhibits selective cytotoxicity against a variety of cancer cell lines, with the highest potency against HepG2 cells (GI50 = 0.72 μM). It shows extremely low cytotoxicity against non-cancerous Vero cells, resulting in a selectivity index of 121.58 for HepG2 cells[1].
IDO1-IN-34 (0.03-0.3 μM; 24 h) dose-dependently reduces kynurenine production in IFN-γ-stimulated SK-OV-3 cells and reverses IDO1-mediated immunosuppression[1].
IDO1-IN-34 (0.03-0.3 μM; 2 days) restores T cell activation in a dose-dependent manner and increases IL-2 expression in an IDO1-inhibited SK-OV-3/Jurkat T cell co-culture system[1].
IDO1-IN-34 (0.36-0.72 μM; 24 h) induces apoptosis in HepG2 cells in a dose-dependent manner[1].
IDO1-IN-34 (0.36-0.72 μM; 48 h) dose-dependently activates the endogenous mitochondrial apoptotic pathway in HepG2 cells, as evidenced by increased levels of cleaved caspase-3, cleaved caspase-9, cleaved PARP-1, and cytochrome c, without activating cleaved caspase-8, a marker of the exogenous apoptotic pathway[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2, A549, MCF-7, PC-3, HT-29, K562, Vero
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Concentration:0.1-100 μM
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Incubation Time:48 h
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Result:Exhibited a GI50 of 0.72 μM against HepG2 liver cancer cells.
Exhibited a GI50 of 3.02 μM against A549 lung cancer cells.
Exhibited a GI50 of 4.55 μM against MCF-7 breast cancer cells.
Exhibited a GI50 of 3.28 μM against PC-3 prostate cancer cells.
Exhibited a GI50 of 6.04 μM against HT-29 colon cancer cells.
Exhibited a GI50 of 10.27 μM against K562 leukemia cells.
Exhibited a GI50 of 87.54 μM against non-cancerous Vero cells.
Yielded selectivity indices of 121.58 (HepG2), 28.98 (A549), 19.23 (MCF-7), 26.68 (PC-3), 14.49 (HT-29), and 8.52 (K562).
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Cell Line:SK-OV-3/Jurkat T-cell co-cultures
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Concentration:0.03, 0.1, 0.3 μM
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Incubation Time:2 days
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Result:Increased IL-2 levels to 416.59 pg/mL at 0.03 μM compared to 161.03 pg/mL in IFN-γ-only treated co-cultures.
Increased IL-2 levels to 648.84 pg/mL at 0.1 μM compared to 161.03 pg/mL in IFN-γ-only treated co-cultures.
Increased IL-2 levels to 865.67 pg/mL at 0.3 μM compared to 161.03 pg/mL in IFN-γ-only treated co-cultures.
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Cell Line:HepG2 liver cancer cells
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Concentration:0.36 μM, 0.72 μM
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Incubation Time:24 h
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Result:Increased total apoptosis (early + late) to 36.16% at 0.36 μM compared to 9.13% in control cells.
Increased total apoptosis (early + late) to 59.33% at 0.72 μM compared to 9.13% in control cells.
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Cell Line:HepG2 liver cancer cells
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Concentration:0.36 μM, 0.72 μM
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Incubation Time:48 h
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Result:Dose-dependently increased levels of cytochrome c, cleaved caspase-3, cleaved caspase-9, and cleaved PARP-1.
Dose-dependently reduced levels of total caspase-3, total caspase-9, and total PARP-1.
Did not increase cleaved caspase-8 levels at either concentration tested.
Chemical Information
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Masse moléculaire 527.19
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Formule C18H10BrF7N4O2
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SMILES
O=C(C1=NNN=C1C2=CC(C(F)(F)F)=CC(Br)=C2)NC3=CC=C(C(OCC(F)(F)F)=C3)F
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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)