G150 是一种高选择性的 human cyclic GMP-AMP synthaseh-cGAS抑制剂IC50值为 10.2 nM。G150 可抑制 dsDNA 引发的干扰素表达,可用于炎症的研究。
生物活性 | G150 is a highly selectivehumancyclic GMP-AMP synthase(h-cGAS)inhibitor with anIC50of 10.2 nM. G150 represses dsDNA-triggered interferon expression, and G150 can be used for the research of inflammatory[1]. |
IC50& Target | IC50: 10.2 nM (h-cGAS)[1] |
体外研究 (In Vitro) | G150 (0.1-100 μM; 1 h) affects IFNB1 and CXCL10 expression in human THP1 cells and primary human macrophages[1].G150 (5-10 μM; 1 h) affects dsDNA sensing in THP1 cells and primary human macrophages[1].G150 (0.1-100 μM; 1 h) affects the NF-κB pathway activation in THP1-Dual cells[1].
RT-PCR[1] Cell Line: | Human THP1 cells and primary human macrophages | Concentration: | 0.1-100 μM | Incubation Time: | 1 hour | Result: | Dose-dependently inhibited IFNB1 and interferon-stimulated genes monitoring CXCL10 expression with IC50s of 1.96 and 7.57 μM respectively in human THP1 cells, and inhibited IFNB1 and CXCL10 expression with IC50s of 0.62 and 0.87 μM respectively in primary human macrophages. |
RT-PCR[1] Cell Line: | Human THP1 cells and primary human macrophages | Concentration: | 5 and 10 μM | Incubation Time: | 1 hour | Result: | Inhibited dsDNA sensing with a concentration of 10 μM in THP1 cells and with a concentration of 5 μM in primary human macrophages. |
RT-PCR[1] Cell Line: | THP1-Dual cells | Concentration: | 0.1-100 μM | Incubation Time: | 1 hour | Result: | Inhibited SEAP activity and luciferase activity with IC50s of 0.90 and 1.79 μM respectively in THP1-Dual cells. |
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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 : 125 mg/mL(319.49 mM;Need ultrasonic) 配制储备液 1 mM | 2.5559 mL | 12.7796 mL | 25.5591 mL | 5 mM | 0.5112 mL | 2.5559 mL | 5.1118 mL | 10 mM | 0.2556 mL | 1.2780 mL | 2.5559 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: ≥ 2.08 mg/mL (5.32 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.32 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 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% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (5.32 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.32 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (5.32 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.32 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 20.8 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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