PROTAC IRAK4 degrader-2

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PROTAC IRAK4 degrader-2 

PROTAC IRAK4 degrader-2 (Compound 9) 是一种 PROTAC IRAK4 降解剂，在外周血单个核细胞 (PBMC) 中，降解 IRAK4，DC50 为 151 nM。PROTAC IRAK4 Degrader-2 在 PBMC 细胞中诱导 IRAK4 蛋白水平降低，DC50 为 36 nM。PROTAC IRAK4 degrader-2 还抑制 PBMC 中多种细胞因子释放。

PROTAC IRAK4 degrader-2

PROTAC IRAK4 degrader-2 Chemical Structure

CAS No. : 2374122-27-5

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生物活性

PROTAC IRAK4 degrader-2 (Compound 9) is a PROTAC-based IRAK4 degrader that affords potent IRAK4 degradation with a DC50 in peripheral blood mononuclear cells (PBMCs) cells of 151 nM. PROTAC IRAK4 degrader-2 induce a reduction of IRAK4 protein levels with a DC50 of 36 nM in PBMC cells. PROTAC IRAK4 degrader-2 also leads to the inhibition of multiple cytokines in PBMCs[1].

体外研究
(In Vitro)

PROTAC IRAK4 degrader-2 (compound 9) (0.01~10 μM; 22 hours; PBMCs) mediated degradation is occurring in a proteasome dependent manner[1].
PROTAC IRAK4 degrader-2 (compound 9) (0.01~10 μM; 24 hours; PBMCs) induces a reduction of IRAK4 protein levels[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: PBMCs
Concentration: 0.01, 0.03, 0.1, 0.3, 1, 3 and 10 μM
Incubation Time: 22 and 24 hours
Result: Induced a reduction of IRAK4 protein levels with a DC50 value of 36 nM and IRAK4 PROTAC-mediated degradation was occurring in a proteasome dependent manner.

分子量

1086.28

Formula

C57H68FN11O8S
CAS 号

2374122-27-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Joao Nunes, et al. Targeting IRAK4 for Degradation with PROTACs. ACS Med Chem Lett. 2019 Jun 14;10(7):1081-1085.

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