| Identification | Back Directory | [Name]
[1,1'-Biphenyl]-4-carboxamide, N-[3-[[(4-fluorophenyl)sulfonyl]amino]-4-hydroxyphenyl]- | [CAS]
2249435-90-1 | [Synonyms]
SN-011
GUN35901
STING INHIBITOR-2
N-(3-(4-Fluorophenylsulfonamido)-4-hydroxyphenyl)-[1,1'-biphenyl]-4-carboxamide
[1,1'-Biphenyl]-4-carboxamide, N-[3-[[(4-fluorophenyl)sulfonyl]amino]-4-hydroxyphenyl]- | [Molecular Formula]
C25H19FN2O4S | [MOL File]
2249435-90-1.mol | [Molecular Weight]
462.49 |
| Chemical Properties | Back Directory | [density ]
1.421±0.06 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
DMF: 5 mg/ml,DMSO: 25 mg/ml,Ethanol: 3 mg/ml,PBS (pH 7.2): insol | [form ]
A solid | [pka]
7.70±0.10(Predicted) | [color ]
Off-white to gray |
| Hazard Information | Back Directory | [Uses]
SN-011 is a potent and selective mouse and human STING inhibitor, with an IC50 of 76 nM for STING signaling. SN-011 competes with cyclic dinucleotide (CDN) for the binding pocket of the STING dimer, blocking CDN binding and STING activation. SN-011 can be used for the research of STING-driven autoimmune and inflammatory disease[1]. | [Biological Activity]
SN-011 is a stimulator of interferon genes (STING) antagonist.1 It binds to the STING cyclic dinucleotide binding site (Kd = 4.03 nM) and inhibits 2’3’-cGAMP-induced Ifnb expression in mouse embryonic fibroblasts (MEFs), mouse bone marrow-derived macrophages (BMDMs), and human foreskin fibroblasts (HFFs; IC50s = 127.5, 107.1, and 502.8 nM, respectively). SN-011 (1 μM) impairs recruitment of IFN regulatory factor 3 (IRF3) or TANK-binding kinase 1 (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 translocation of STING from the endoplasmic reticulum (ER) to the Golgi induced by herpes simplex virus 1 (HSV-1) in HFFs. In vivo, SN-011 (5 mg/kg) increases survival and reduces Ifnb mRNA levels in the Trex1-/- mouse model of Aicardi-Goutières syndrome, an autoimmune disorder characterized by constitutive activation of cGAS and IFN overproduction. | [in vivo]
SN-011 (5 mg/kg; i.p. 3 times weekly for a month) strongly inhibits hallmarks of inflammation and autoimmunity disease, and protects Trex1 / mice from death[1]. | Animal Model: | 4-wk-old Trex1?/? mice[1] | | Dosage: | 5 mg/kg | | Administration: | I.p. 3 times weekly for a month | | Result: | Improved survival of mice.
Reduced severe multiorgan inflammation.
Reduced serum antinuclear antibody.
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| [storage]
-20°C | [References]
1.Hong, Z., Mei, J., Li, C., et al.STING inhibitors target the cyclic dinucleotide binding pocketProc. Natl. Acad. Sci. USA.118(24)e2105465118(2021)
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