1. PROTAC
    Metabolic Enzyme/Protease
  2. PROTAC
    Indoleamine 2,3-Dioxygenase (IDO)
  3. PROTAC IDO1 Degrader-1

PROTAC IDO1 Degrader-1 

Cat. No.: HY-131911
Handling Instructions

PROTAC IDO1 Degrader-1 is the first potent IDO1 (indoleamine 2,3-dioxygenase 1) degrader that hijacks IDO1 to CRBN E3 ligase to introduce IDO1 into UPS and eventually achieve ubiquitination and degradation (DC50=2.84 μM). PROTAC IDO1 Degrader-1 moderately improves the tumor-killing activity of H ER2 CAR-T cells.

For research use only. We do not sell to patients.

PROTAC IDO1 Degrader-1 Chemical Structure

PROTAC IDO1 Degrader-1 Chemical Structure

CAS No. : 2488851-89-2

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Description

PROTAC IDO1 Degrader-1 is the first potent IDO1 (indoleamine 2,3-dioxygenase 1) degrader that hijacks IDO1 to CRBN E3 ligase to introduce IDO1 into UPS and eventually achieve ubiquitination and degradation (DC50=2.84 μM). PROTAC IDO1 Degrader-1 moderately improves the tumor-killing activity of H ER2 CAR-T cells[1].

IC50 & Target[1]

IDO1

2.84 μM (DC50)

IDO1

1.07 μM (IC50)

In Vitro

PROTAC IDO1 Degrader-1 (compound 2c) (10 μM; 24 hours) notably decreases IDO1 level induced by IFN-γ[1].
PROTAC IDO1 Degrader-1 and IFN-γ (5 ng/mL) are incubated with HeLa cells for 24 h, and a significant dose-dependent degradation is observed. PROTAC IDO1 Degrader-1 combined with chimeric antigen receptor-modified T (CAR-T) cells can improve the tumor-killing activity of HER-2 CAR-T cells[1].
PROTAC IDO1 Degrader-1 induces significant and persistent degradation of IDO1 with maximum degradation (dmax) of 93% in HeLa cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: HeLa cells
Concentration: 10 μM
Incubation Time: 24 hours
Result: Notably decreased IDO1 level induced by IFN-γ (5 ng/mL).
Molecular Weight

966.80

Formula

C₄₀H₅₃BrFN₉O₁₃

CAS No.
SMILES

O=C1C2=C(NCCOCCOCCOCCOCCOCCOCCOCCNCCNC3=NON=C3/C(NC4=CC(Br)=C(C=C4)F)=N/O)C=CC=C2C(N1C5C(NC(CC5)=O)=O)=O

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

PROTAC IDO1 Degrader-1PROTACIndoleamine 2,3-Dioxygenase (IDO)Proteolysis-targeting chimeraInhibitorinhibitorinhibit

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PROTAC IDO1 Degrader-1
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