Salubrinal是一种细胞渗透性和选择性的 eIF2α 去磷酸化抑制剂。它作为一种双特异性磷酸酶 2 (Dusp2) 抑制剂,抑制抗胶原抗体诱导的关节炎中的炎症,对 HSV-1 具有抗病毒活性,并抑制 HSV-1 蛋白 ICP34.5 介导的 eIF2α 去磷酸化。
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产品名称 | PERK ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
ISRIB |
++
PERK, IC50: 5 nM |
98% | |||||||||||||||||
GSK2656157 |
+++
PERK, IC50: 0.9 nM |
99%+ | |||||||||||||||||
GSK2606414 |
++++
EIF2AK3 (PERK), IC50: 0.4 nM |
99%+ | |||||||||||||||||
Salubrinal | ✔ | 99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | UPR (unfolded protein response), dysregulation of which has been implicated in many important pathologies, is an essential pathway to cope with ER stress. The PERK-eIF2α is one of the important parts of UPR. Salubrinal is a selective inhibitor of cellular complexes that can dephosphorylate eIF2α and dose-dependently induced phosphorylation of eIF2a in PC12 cells after 36 hours treatment at concentration ranging in 1-75μM. Treatment with Salubrinal at concentration ranging in 10-100μM can inhibit ER stress-mediated apoptosis induced by tunicamycin (750ng/ml) in a concentration-dependent manner with EC50 value of 15μM[1]. Daily administration of Salubrinal at dose of 1.5mg/kg on 3 days after induction of OA could significantly suppress OA-induced NFκB phosphorylation and MMP13 activity in vivo[2]. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
human 697 cell | Growth inhibition assay | Inhibition of human 697 cell growth in a cell viability assay, IC50=3.98788 μM | SANGER | ||
human 8-MG-BA cell | Growth inhibition assay | Inhibition of human 8-MG-BA cell growth in a cell viability assay, IC50=10.9999 μM | SANGER | ||
human A101D cell | Growth inhibition assay | Inhibition of human A101D cell growth in a cell viability assay, IC50=13.8207 μM | SANGER | ||
human A3-KAW cell | Growth inhibition assay | Inhibition of human A3-KAW cell growth in a cell viability assay, IC50=8.43289 μM | SANGER | ||
Dose | Mice: 0.5 mg/kg[3](s.c.), 2 mg/kg[4] (s.c.), 0.5 mg/kg[5] (i.p.), 1 mg/kg[6] (i.p.), 5 mg/kg[7] (p.o.) | ||||||||
Administration | s.c., i.p., p.o. | ||||||||
Pharmacokinetics |
|
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.08mL 0.42mL 0.21mL |
10.42mL 2.08mL 1.04mL |
20.84mL 4.17mL 2.08mL |
CAS号 | 405060-95-9 |
分子式 | C21H17Cl3N4OS |
分子量 | 479.81 |
别名 | |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry,Store in freezer, under -20°C |
溶解方案 |
DMSO: 50 mg/mL(104.21 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |