SN-011

一种STING拮抗剂；与STING环状二核苷酸结合位点结合(Kd=4.03nM)并抑制MEF、BMDM和HFF中2'3'-cGAMP诱导的Ifnb表达(IC50s分别为127.5、107.1和502.8nM)；在过表达标记的野生型或SAVI连锁突变体STING和IRF3或TBK1的HEK293T细胞中，削弱IRF3或TBK1募集到STING信号体，并在1µM时抑制HSV-1诱导的STING从ER易位到高尔基体；在5mg/kg时，在Aicardi-Goutières综合征的Trex1-/-小鼠模型中增加存活率并降低IfnbmRNA水平。A STING antagonist; binds to the STING cyclic dinucleotide binding site (Kd = 4.03 nM) and inhibits 2'3'-cGAMP-induced Ifnb expression in MEFs, BMDMs, and HFFs (IC50s = 127.5, 107.1, and 502.8 nM, respectively); impairs recruitment of IRF3 or TBK1 to the STING signalosome in HEK293T cells overexpressing tagged wild-type or SAVI-linked mutant STING and IRF3 or TBK1, as well as inhibits HSV-1-induced translocation of STING from the ER to the Golgi at 1 µM; increases survival and reduces Ifnb mRNA levels in the Trex1-/- mouse model of Aicardi-Goutières syndrome at 5 mg/kg.分子式C25H19FN2O4S分子量462.5O=C(C1=CC=C(C2=CC=CC=C2)C=C1)NC3=CC=C(C(NS(=O)(C4=CC=C(C=C4)F)=O)=C3)O