dsdna/cgas

RU.521 (RU3205217) 是选择性的环状 GMP-AMP 合成酶 (cGAS) 抑制剂，抑制 cGAS 介导的干扰素上调。它也抑制dsDNA 激活受体的活性，IC50为 700 nM。它可降低来自 Aicardi-Goutières 综合征小鼠模型的巨噬细胞中干扰素的组成型表达。

G150 是高选择性h-cGAS 抑制剂，IC50值为 10.2 nM，用于抑制 dsDNA 引发的干扰素表达。

PROTAC cGAS degrader-1 (Compound TH35) 是一种高效且选择性的 cGAS PROTAC 降解剂，在 THP-1 和 RAW 264.7 细胞中，其 DC50 分别为 0.9 μM 和 4.6 μM。它能够抑制 dsDNA 引发的 cGAS 信号激活，并表现出抗炎活性，适用于研究与 cGAS 相关的炎症性疾病。(Pink: cGAS inhibitor; Black: Linker; Blue: E3 ligase ligand)

Cyclic di-UMP is a pyrimidine-containing cyclic dinucleotide (CDN).1It is produced by bacterial cGAS DncV-like nucleotidyltransferases (CD-NTases), such as LpCdnE02 fromL. pneumophila, and binds to cGAS, in the apo or dsDNA-bound forms, with reduced affinity compared to 2'3'-cGAMP or 3'3'-cGAMP .1,2Cyclic di-UMP is intended for use as a negative control for cyclic di-GMP signaling. 1.Whiteley, A.T., Eaglesham, J.B., de Oliveira Mann, C.C., et al.Bacterial cGAS-like enzymes synthesize diverse nucleotide signalsNature564(7747)194-199(2019) 2.Hall, J., Ralph, E.C., Shanker, S., et al.The catalytic mechanism of cyclic GMP-AMP synthase (cGAS) and implications for innate immunity and inhibitionProtein Sci.26(12)2367-2380(2017)