iDeg-1
iDeg-1 is a potent IDO1 molecular glue degrader. iDeg-1 binds to apo-IDO1 and alters its C-terminal conformation, promoting CRL2-KLHDC3 E3 ligase-mediated ubiquitination and degradation of IDO1. iDeg-1 can be used in cancer-related research.
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- Formule: C30H40N2O4S
- Masse moléculaire:524.71
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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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Activité biologique
Description
IC50 & Target
[1]|
IDO1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BXPC-3 | IC50 |
1.1 μM
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Inhibition of kynurenine (Kyn) formation in IFN-γ-stimulated human BxPC3 cells incubated for 48 h, quantified using p-DMAB.
Inhibition of kynurenine (Kyn) formation in IFN-γ-stimulated human BxPC3 cells incubated for 48 h, quantified using p-DMAB.
|
41501556 |
| SK-OV-3 | IC50 |
1.6 μM
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Inhibition of kynurenine (Kyn) formation in IFN-γ-stimulated human SKOV-3 cells incubated for 48 h, quantified using p-DMAB.
Inhibition of kynurenine (Kyn) formation in IFN-γ-stimulated human SKOV-3 cells incubated for 48 h, quantified using p-DMAB.
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41501556 |
| HeLa | IC50 |
1.7 μM
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Inhibition of kynurenine (Kyn) formation in IFN-γ-stimulated human HeLa cells incubated for 48 h, quantified using p-DMAB.
Inhibition of kynurenine (Kyn) formation in IFN-γ-stimulated human HeLa cells incubated for 48 h, quantified using p-DMAB.
|
41501556 |
| HEK-293T | IC50 |
0.45 μM
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Inhibition of kynurenine (Kyn) formation in recombinant human IDO1 (rhIDO1)-electroporated human HEK293T cells.
Inhibition of kynurenine (Kyn) formation in recombinant human IDO1 (rhIDO1)-electroporated human HEK293T cells.
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41501556 |
| HEK-293T | IC50 |
0.42 μM
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Inhibition of kynurenine (Kyn) formation in transiently IDO1-expressing human HEK293T cells.
Inhibition of kynurenine (Kyn) formation in transiently IDO1-expressing human HEK293T cells.
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41501556 |
| BXPC-3 | IC50 |
0.83 μM
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Inhibition of kynurenine formation via indoleamine-2,3-dioxygenase 1 enzymatic activity in IFN-γ-stimulated BxPC3 cells incubated for 48 hrs by Kyn assay.
Inhibition of kynurenine formation via indoleamine-2,3-dioxygenase 1 enzymatic activity in IFN-γ-stimulated BxPC3 cells incubated for 48 hrs by Kyn assay.
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41501556 |
In Vitro
iDeg-1 (48 h) inhibits the production of kynurenine (Kyn) in BxPC3, SKOV-3, and HeLa cells stimulated with IFN-γ (HY-P7025), with IC50 values of 1.1 μM, 1.6 μM, and 1.7 μM, respectively[1].
iDeg-1 (0.03-50 μM; 6-24 h) reduces IDO1 protein levels and induces polyubiquitination of IDO1 in IFN-γ-stimulated BxPC3 cells in a dose-dependent manner[1].
iDeg-1 reduces IDO1 protein levels in a time-dependent manner and decreases Kyn production in a dose-dependent manner in HEK293T cells (electroporated with rhIDO1 or transfected with plasmids), with IC50 values of approximately 0.45 μM and 0.42 μM, respectively[1].
iDeg-1 (50 μM; 1 h) binds to and thermally stabilizes the IDO1 protein in SKOV-3 cells (ΔTm = 3.5 °C)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BxPC3
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Concentration:0.03 μM, 0.12 μM, 0.37 μM, 1.11 μM, 3.33 μM, 10 μM
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Incubation Time:24 h
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Result:Reduced endogenous IDO1 protein levels in a dose-dependent manner.
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Cell Line:BxPC3
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Concentration:50 μM
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Incubation Time:6 h
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Result:Markedly increased the polyubiquitination levels of IDO1.
Chemical Information
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Masse moléculaire 524.71
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Formule C30H40N2O4S
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SMILES
CC1=CC=C(C=C1)NC(OC[C@@]23[C@H](C[C@@H]4C[C@]2([H])CN(C3)S(C5=CC=C(C(C)(C)C)C=C5)(=O)=O)C4(C)C)=O
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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)
iDeg-1 Related Classifications
HY-177783 Related Classifications
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