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PROTAC IDO1 Degrader-1

Catalog No. T37329   CAS 2488851-89-2
Synonyms: PROTAC IDO1 Degrader-1

PROTAC IDO1 Degrader-1, a pioneering compound, efficiently targets indoleamine 2,3-dioxygenase 1 (IDO1) for ubiquitination and degradation by recruiting IDO1 to the CRBN E3 ligase, thereby facilitating its entry into the ubiquitin-proteasome system (UPS) with a DC50 of 2.84 μM. This compound also moderately enhances the tumor-killing efficacy of HER2 CAR-T cells[1].

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PROTAC IDO1 Degrader-1 Chemical Structure
PROTAC IDO1 Degrader-1, CAS 2488851-89-2
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Biological Description
Chemical Properties
Storage & Solubility Information
Description PROTAC IDO1 Degrader-1, a pioneering compound, efficiently targets indoleamine 2,3-dioxygenase 1 (IDO1) for ubiquitination and degradation by recruiting IDO1 to the CRBN E3 ligase, thereby facilitating its entry into the ubiquitin-proteasome system (UPS) with a DC50 of 2.84 μM. This compound also moderately enhances the tumor-killing efficacy of HER2 CAR-T cells[1].
Targets&IC50 IDO1:1.07 μM (IC50), IDO1:2.84 μM (DC50)
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].
Synonyms PROTAC IDO1 Degrader-1
Molecular Weight 966.816
Formula C40H53BrFN9O13
CAS No. 2488851-89-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Hu M, et al. Discovery of the first potent proteolysis targeting chimera (PROTAC) degrader of indoleamine 2,3-dioxygenase 1. Acta Pharm Sin B. 2020;10(10):1943-1953.

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Keywords

PROTAC IDO1 Degrader-1 2488851-89-2 PROTAC IDO1 Degrader 1 PROTAC IDO-1 Degrader-1 PROTAC IDO1 Degrader1 inhibitor inhibit

 

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