Salubrinal

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Chemical Structure| 405060-95-9 同义名 : -
CAS号 : 405060-95-9
货号 : A591957
分子式 : C21H17Cl3N4OS
纯度 : 99%+
分子量 : 479.81
MDL号 : MFCD00548612
存储条件：

Pure form Sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

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
生物活性
靶点

  • PERK
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].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 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
实验方案
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
参考文献

[1]Boyce M, Bryant KF, et al. A selective inhibitor of eIF2alpha dephosphorylation protects cells from ER stress. Science. 2005 Feb 11;307(5711):935-9.

[2]Hamamura K, Nishimura A, et al. Chondroprotective effects of Salubrinal in a mouse model of osteoarthritis. Bone Joint Res. 2015 May;4(5):84-92.

[3]Rani S, Sreenivasaiah PK, et al. Salubrinal Alleviates Pressure Overload-Induced Cardiac Hypertrophy by Inhibiting Endoplasmic Reticulum Stress Pathway. Mol Cells. 2017 Jan;40(1):66-72.

[4]Takigawa S, Frondorf B, et al. Salubrinal improves mechanical properties of the femur in osteogenesis imperfecta mice. J Pharmacol Sci. 2016 Oct;132(2):154-161.

[5]Hu Y, Lu X, et al. Salubrinal attenuated retinal neovascularization by inhibiting CHOP-HIF1α-VEGF pathways. Oncotarget. 2017 Aug 24;8(44):77219-77232.

[6]Tan HP, Guo Q, et al. Inhibition of endoplasmic reticulum stress alleviates secondary injury after traumatic brain injury. Neural Regen Res. 2018 May;13(5):827-836.

[7]Balakrishnan B, Siddiqi A, et al. Salubrinal enhances eIF2α phosphorylation and improves fertility in a mouse model of Classic Galactosemia. Biochim Biophys Acta Mol Basis Dis. 2019 Nov 1;1865(11):165516.

[8]Zhang P, Hamamura K, et al. Salubrinal promotes healing of surgical wounds in rat femurs. J Bone Miner Metab. 2012 Sep;30(5):568-79.