SP600125 是一种口服有效的,可逆的,ATP竞争性的JNK抑制剂,抑制JNK1,JNK2和JNK3的IC50分别为 40,40,90 nM。SP600125 是一种有效的铁死亡 (ferroptosis) 抑制剂。SP600125 抑制自噬 (autophagy),诱导凋亡 (apoptosis)。
生物活性 | SP600125 is an orally active, reversible, and ATP-competitiveJNKinhibitor withIC50s of 40, 40 and 90 nM forJNK1,JNK2andJNK3, respectively. SP600125 is a potentferroptosisinhibitor. SP600125 inhibitsautophagyand activatesapoptosis[1][2][3]. |
IC50& Target[1] | JNK1 40 nM (IC50) | JNK2 40 nM (IC50) | JNK3 90 nM (IC50) | Autophagy |
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体外研究 (In Vitro) | SP600125 is an ATP-competitive inhibitor of JNK2 with a Kivalue of 0.19±0.06 μM. SP600125 inhibits the phosphorylation of c-Jun with IC50 of 5 μM to 10 μM in Jurkat T cells. In CD4+cells, such as Th0 cells isolated from either human cord or peripheral blood, SP600125 blocks cell activation and differentiation and inhibits the expression of inflammatory genes COX-2, IL-2, IL-10, IFN-γ, and TNF-α, with IC50of 5 μM to 12 μM[1]. In a mouse beta cells MIN6, SP600125 (20 μM) induces the phosphorylation of p38 MAPK and its downstream CREB-dependent promoter activation[2]. In HCT116 cells, SP600125 (20 μM) blocks the G2 phase to mitosis transition and induces endoreplication. This ability of SP600125 is independent of JNK inhibition, but due to its inhibition of CDK1-cyclin B activation upstream of Aurora A and Polo-like kinase 1[3].
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体内研究 (In Vivo) | Administration of SP600125 at 15 or 30 mg/kg i.v. significantly inhibits TNF-α serum levels, whereas oral administration dose-dependently blocks TNF-α expression with significant inhibition observed at 30 mg/kgper os[1]. SP600125 attenuates LPS-induced ALI in rats in vivo. The expression levels of TNF-α and IL-6 in the BALF in rats in the SP600125 group are significantly decreased[4].
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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 : 12.5 mg/mL(56.76 mM;Need ultrasonic) 配制储备液 1 mM | 4.5407 mL | 22.7035 mL | 45.4071 mL | 5 mM | 0.9081 mL | 4.5407 mL | 9.0814 mL | 10 mM | 0.4541 mL | 2.2704 mL | 4.5407 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: 1%CMC-Na/saline water Solubility: 3.33 mg/mL (15.12 mM); Suspended solution; Need ultrasonic 2. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: 2.08 mg/mL (9.44 mM); Suspended solution; Need ultrasonic
此方案可获得 2.08 mg/mL (9.44 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。 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。 3. 请依序添加每种溶剂: corn oil Solubility: 1 mg/mL (4.54 mM); Suspended solution; Need ultrasonic and warming and heat to 80℃ *以上所有助溶剂都可在本网站选购。
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