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PROTAC IDO1 Degrader-1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PROTAC IDO1 Degrader-1图片
CAS NO:2488851-89-2
包装:5mg
市场价:7650元

PROTAC IDO1 Degrader-1 是第一个强效的 IDO1 (indoleamine 2,3-dioxygenase 1) 降解剂,它将IDO1劫持到crbne3连接酶上,最终实现泛素化和降解 (DC50=2.84 μM)。PROTAC-IDO1降解剂-1适度提高H-ER2-CAR-T细胞的杀伤活性。
Cas No.2488851-89-2
分子式C40H53BrFN9O13
分子量966.8
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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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