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PROTAC IDO1 Degrader-1

رقم الكتالوجGC62689

PROTAC IDO1 Degrader-1 هو أول جهاز تحطيم فعال لـ IDO1 (indoleamine 2،3-dioxygenase 1) الذي يخطف IDO1 إلى Cereblon E3 ligase لإدخال IDO1 في UPS وتحقيق الانتشار والتحلل في النهاية (DC50 = 2.84 ميكرومتر)

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PROTAC IDO1 Degrader-1 التركيب الكيميائي

Cas No.: 2488851-89-2

الحجم السعر المخزون الكميّة
5 mg
765٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents

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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