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  2. PROTACs IKK
  3. PROTAC TBK1 degrader-2

PROTAC TBK1 degrader-2 

目录号: HY-112557 纯度: 98.20%
COA 产品使用指南

PROTAC TBK1 degrader-2 是 PROTAC 靶蛋白配体,是一种强效的基于丝氨酸/苏氨酸激酶 TANK 结合激酶-1 (TBK1) 的降解剂 (DC50=15 nM; Kd=4.6 nM)。PROTAC TBK1 degrader-2 降解 TBK1 的最大效率达到 96%。PROTAC TBK1 degrader-2 也靶向 IkB 激酶 IKKε (IC50=8.7 nM),对 TBK1 (IC50=1.3 nM) 的选择性低。

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PROTAC TBK1 degrader-2 Chemical Structure

PROTAC TBK1 degrader-2 Chemical Structure

CAS No. : 2052306-13-3

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

IC50 & Target

IC50: 1.3 nM (TBK1), 8.7 nM (IKKε)[1]

体外研究
(In Vitro)

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 TBK1IKKε 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]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: K-Ras mutant cell lines (H23, A549, and H1792) and K-Rras wild type cell lines (H2110 and HCC827)
Concentration: 100 nM, 300 nM
Incubation Time: 72 hours
Result: Lacked synthetically lethality in K-Ras mutant versus wild type cells.
分子量

1093.18

Formula

C53H74BrN9O9S

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料
参考文献

PROTAC TBK1 degrader-2 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
PROTAC TBK1 degrader-2
目录号:
HY-112557
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