PROTAC TBK1 degrader-2_product_DataBase

Bioactivity	PROTAC TBK1 degrader-2 is a Ligands for Target Protein for PROTAC. PROTAC TBK1 degrader-2 is a potent degrader based on the serine/threonine kinase TANK-binding kinase 1 (TBK1) (DC50=15 nM; Kd=4.6 nM) with a maximum efficiency of 96%. PROTAC TBK1 degrader-2 also targets to IkB kinase IKKε (IC50=8.7 nM), with low selectivity over TBK1 (IC50=1.3 nM)[1].
Target	IC50: 1.3 nM (TBK1), 8.7 nM (IKKε)
Invitro	PROTAC TBK1 degrader-2 (compound 3i) (100 nM) 介导的 TBK1 降解能够被 VHL 配体 2 (10 μM) 或蛋白酶体抑制剂 Carfilzomib (HY-10455) (100 nM) 抑制[1]。PROTAC TBK1 degrader-2 (0-3 μM) 在 TBK1 和 IKKε 间表现出较差的选择性 (IC50 分别为 1.3 nM 和 8.7 nM)，但当浓度超过对 TBK1 DC50 的 50 倍以上时，对 IKKε 水平没有影响[1]。PROTAC TBK1 degrader-2 (100 nM; 300 M; 72 h) 在 K-Ras 突变体与野生型细胞中不具有合成致命性[1]。 Cell Viability Assay[1] Cell Line:
Name	PROTAC TBK1 degrader-2
CAS	2052306-13-3
Formula	C53H74BrN9O9S
Molar Mass	1093.18
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Crew AP, et al. Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1. J Med Chem. 2018 Jan 25;61(2):583-598.

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