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

PROTAC IDO1 Degrader-1 

Cat. No.: HY-131911 Purity: 98.17%
Handling Instructions

PROTAC IDO1 Degrader-1 is the first potent IDO1 (indoleamine 2,3-dioxygenase 1) degrader that hijacks IDO1 to Cereblon 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

Size Price Stock Quantity
5 mg USD 850 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1250 In-stock
Estimated Time of Arrival: December 31
25 mg USD 2600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 4500 In-stock
Estimated Time of Arrival: December 31
100 mg USD 7200 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

PROTAC IDO1 Degrader-1 is the first potent IDO1 (indoleamine 2,3-dioxygenase 1) degrader that hijacks IDO1 to Cereblon 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.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (103.43 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0343 mL 5.1717 mL 10.3434 mL
5 mM 0.2069 mL 1.0343 mL 2.0687 mL
10 mM 0.1034 mL 0.5172 mL 1.0343 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 5 mg/mL (5.17 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 5 mg/mL (5.17 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
References
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Product Name:
PROTAC IDO1 Degrader-1
Cat. No.:
HY-131911
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