H-151

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Chemical Structure| 941987-60-6 同义名 : -
CAS号 : 941987-60-6
货号 : A923731
分子式 : C17H17N3O
纯度 : 99%+
分子量 : 279.34
MDL号 : MFCD08026581
存储条件：

Pure form Sealed in dry,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(375.89 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
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]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.58mL

0.72mL

0.36mL

17.90mL

3.58mL

1.79mL

35.80mL

7.16mL

3.58mL
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.