SN-011 是一种有效和选择性的STING抑制剂，抑制 STING 信号传导的IC50值为 76 nM。SN-011 与环状二核苷酸 (CDN) 竞争 STING 二聚体的结合口袋，从而阻断 CDN 结合和 STING 激活。SN-011 可用于 STING 驱动的自身免疫和炎症性疾病的研究。
| 生物活性 | SN-011 is a potent and selective mouse and humanSTINGinhibitor, with anIC50of 76 nM forSTINGsignaling. SN-011 competes with cyclic dinucleotide (CDN) for the binding pocket of theSTINGdimer, blocking CDN binding andSTINGactivation. SN-011 can be used for the research of STING-driven autoimmune and inflammatory disease[1]. |
| IC50& Target | IC50: 76 nM (STING signaling)[1] |
体外研究
(In Vitro) | SN-011 (1 μM; pretreated for 6 h) significantly suppresses the STING stimulator-induced expression of Ifnb, Cxcl10, and Il6 mRNA in mouse embryonic fibroblasts (MEFs)[1].
SN-011 (0.001-10 μM; pretreated for 6 h) inhibits 2′3′-cGAMP-induced Ifnb expression in MEFs, mouse bone marrow-derived macrophages (BMDMs) and human foreskin fibroblasts (HFFs) with IC50s of 127.5, 107.1, and 502.8 nM, respectively[1].
SN-011 (1 μM; pretreated for 3 h) inhibits 2′3′-cGAMP-induced STING oligomerization and phosphorylation in HFFs[1].
SN-011 (1 μM) suppresses HSV-1 infection (4 h), HT-DNA (1 h), or 2′3′-cGAMP stimulation (30 min) induced STING ER-to-Golgi translocation[1].
Western Blot Analysis[1] | Cell Line: | Human foreskin fibroblasts | | Concentration: | 1 μM | | Incubation Time: | Pretreated and then stimulated with 2′3′-cGAMP for 1 h | | Result: | Suppressed 2′3′-cGAMP-induced STING oligomerization and phosphorylation. |
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体内研究
(In Vivo) | SN-011 (5 mg/kg; i.p. 3 times weekly for a month) strongly inhibits hallmarks of inflammation and autoimmunity disease, and protectsTrex1–/–mice from death[1].
| Animal Model: | 4-wk-oldTrex1–/–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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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(216.22 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.1622 mL | 10.8110 mL | 21.6221 mL | | 5 mM | 0.4324 mL | 2.1622 mL | 4.3244 mL | | 10 mM | 0.2162 mL | 1.0811 mL | 2.1622 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (5.41 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.41 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (5.41 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.41 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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