PROTAC IDO1 Degrader-1 |
Katalog-Nr.GC62689 |
PROTAC IDO1 Degrader-1 ist der erste potente IDO1 (Indolamin 2,3-Dioxygenase 1) Degrader, der IDO1 in Cereblon E3 Ligase entfÜhrt, um IDO1 in UPS einzufÜhren und schließlich Ubiquitinierung und Abbau zu erreichen (DC50=2,84 μM).
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Cas No.: 2488851-89-2
Sample solution is provided at 25 µL, 10mM.
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].
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].
[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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