|1-(4-乙基苯基)-3-(1H-吲哚-3-基)脲|CsnPharm

CAS No.: 941987-60-6

H-151 Catalog No. CSN23676

1-(4-Ethylphenyl)-3-(1H-indol-3-yl)urea, also known as H-151, is a irreversible inhibitor of STING that can inhibit the type I interferon (IFN) response and reduce the phosphorylation of TBK1 and palmitoylation of human STING in vitro.

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技术信息

生物活性

描述H-151 is a potent and selective STING antagonist. It dose-dependently abrogated IFNβ luciferase reporter at concentration ranging in 0.02-2μM in HEK293T cells. It reduced TBK1 phosphorylation (0.5μM, for 2h) in THP-1 cells and suppression of hsSTING palmitoylation (1μM, for 3h) without affecting respective controls. Pre-treatment of H-151 markedly reduced systemic cytokine responses in CMA (STING agonist)-treated mice^[2].
作用机制H-151 can bind covalently with Cys91 of hsSTING.^[2]
参考文献

[1] Haag SM, Gulen MF, et al. Targeting STING with covalent small-molecule inhibitors. Nature. 2018 Jul;559(7713):269-273.
[2] Haag SM, Gulen MF, Reymond L, Gibelin A, Abrami L, Decout A, Heymann M, van der Goot FG, Turcatti G, Behrendt R, Ablasser A. Targeting STING with covalent small-molecule inhibitors. Nature. 2018 Jul;559(7713):269-273. doi: 10.1038/s41586-018-0287-8. Epub 2018 Jul 4. PMID: 29973723.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.5799 mL
- 17.8996 mL
- 35.7991 mL
- 5 mM
- 0.7160 mL
- 3.5799 mL
- 7.1598 mL
- 10 mM
- 0.3580 mL
- 1.7900 mL
- 3.5799 mL

技术信息

CAS号

941987-60-6

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H17N3O

运输

蓝冰

分子量

279.34

别名

溶解度

DMSO	230.0 mg/mL (823.4 mM)
Water	insoluble

动物实验配方

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H-151 Catalog No. CSN23676

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