SU3327 是一种有效的,选择性的且具有底物竞争性的JNK抑制剂,IC50为 0.7 μM。SU3327 还以IC50值为 239 nM 抑制JNK和 JIP 之间的蛋白相互作用。SU3327 对 p38α 和 Akt 激酶的活性较低。
生物活性 | SU3327 is a potent, selective and substrate-competitiveJNKinhibitor with anIC50of 0.7 μM. SU3327 also inhibits protein-protein interactions betweenJNKandJNKInteracting Protein (JIP) with anIC50of 239 nM. SU3327 shows less active againstp38αandAktkinase[1][2]. |
IC50& Target | IC50: 0.7 μM (JNK); 239 nM (JNK-JIP interactions)[1] |
体外研究 (In Vitro) | SU3327 (compound 9) is able to inhibit TNF-α stimulated phosphorylation of c-Jun in HeLa cells (EC50= 6.23 μM)[1]. SU3327 (25 nM) pretreatment of human-derived cerebral microvascular endothelial cells (hCMEC/D3) effectively reduces LPS-induced polymorphonuclear leukocytes (PMN) rolling/adhesion to hCMEC/D3, prevents activation of AP-1, and significantly reduces expression of VCAM-1[3].
|
体内研究 (In Vivo) | SU3327 (Compound 9; 25 mg/kg; intraperitoneal injection; male BKS.Cg-+Leprdb/+Leprdb/OlaHsd db/db mice) treatment possesses the ability to restore insulin sensitivity in mice models of diabetes[1]. SU3327 (Compound 9) has favorable microsomal and plasma stability (T1/2= 27 min)[1].
Animal Model: | Male BKS.Cg-+Leprdb/+Leprdb/OlaHsd db/db mice (11-week-old ) injected with insulin[1] | Dosage: | 25 mg/kg | Administration: | Intraperitoneal injection | Result: | Resulted in a statistically significant reduction in blood glucose levels. |
|
分子量 | |
性状 | |
Formula | |
CAS 号 | |
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 |
|
溶解性数据 | In Vitro: DMSO : 62.5 mg/mL(239.19 mM;Need ultrasonic) 配制储备液 1 mM | 3.8270 mL | 19.1351 mL | 38.2702 mL | 5 mM | 0.7654 mL | 3.8270 mL | 7.6540 mL | 10 mM | 0.3827 mL | 1.9135 mL | 3.8270 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 (7.96 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (7.96 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 (7.96 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (7.96 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。 *以上所有助溶剂都可在本网站选购。
|