Sal003

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Chemical Structure| 1164470-53-4 同义名 : -
CAS号 : 1164470-53-4
货号 : A690119
分子式 : C18H15Cl4N3OS
纯度 : 99%+
分子量 : 463.21
MDL号 : MFCD00361095
存储条件：

Pure form Keep in dark place, sealed in dry, 2-8°C

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

DMSO: 105 mg/mL(226.68 mM)，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
描述 Sal003 is a salubrinal derivate which can inhibit eIF2α dephosphorylation[5]. The level of phosphoserine 51-eIF2α was increased in HT1080 cells treated with 75μM Sal003 for 8h and in NIH 3T3 cells treated with 75μM Sal003 for 4h[6]. Sal003 at 10μM sharply increased eIF2α phosphorylation in MEFs. Increase of eIF2α phosphorylation by Sal003 led to impairment of synaptic plasticity and memory[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.16mL

0.43mL

0.22mL

10.79mL

2.16mL

1.08mL

21.59mL

4.32mL

2.16mL
参考文献

[1]Robert F, Kapp LD, et al. Initiation of protein synthesis by hepatitis C virus is refractory to reduced eIF2.GTP.Met-tRNA(i)(Met) ternary complex availability. Mol Biol Cell. 2006 Nov;17(11):4632-44. Epub 2006 Aug 23.

[2]Baltzis D, Pluquet O, et al. The eIF2alpha kinases PERK and PKR activate glycogen synthase kinase 3 to promote the proteasomal degradation of p53. J Biol Chem. 2007 Oct 26;282(43):31675-87. Epub 2007 Sep 4.

[3]Costa-Mattioli M, Gobert D, et al. eIF2alpha phosphorylation bidirectionally regulates the switch from short- to long-term synaptic plasticity and memory. Cell. 2007 Apr 6;129(1):195-206.

[4]Darini C, Ghaddar N, et al. An integrated stress response via PKR suppresses HER2+ cancers and improves trastuzumab therapy. Nat Commun. 2019 May 13;10(1):2139.

[5]Robert F, Kapp LD, Khan SN, Acker MG, Kolitz S, Kazemi S, Kaufman RJ, Merrick WC, Koromilas AE, Lorsch JR, Pelletier J. Initiation of protein synthesis by hepatitis C virus is refractory to reduced eIF2.GTP.Met-tRNA(i)(Met) ternary complex availability. Mol Biol Cell. 2006 Nov;17(11):4632-44. doi: 10.1091/mbc.e06-06-0478. Epub 2006 Aug 23. PMID: 16928960; PMCID: PMC1635388.

[6]Baltzis D, Pluquet O, Papadakis AI, Kazemi S, Qu LK, Koromilas AE. The eIF2alpha kinases PERK and PKR activate glycogen synthase kinase 3 to promote the proteasomal degradation of p53. J Biol Chem. 2007 Oct 26;282(43):31675-87. doi: 10.1074/jbc.M704491200. Epub 2007 Sep 4. PMID: 17785458.

[7]Costa-Mattioli M, Gobert D, Stern E, Gamache K, Colina R, Cuello C, Sossin W, Kaufman R, Pelletier J, Rosenblum K, Krnjević K, Lacaille JC, Nader K, Sonenberg N. eIF2alpha phosphorylation bidirectionally regulates the switch from short- to long-term synaptic plasticity and memory. Cell. 2007 Apr 6;129(1):195-206. doi: 10.1016/j.cell.2007.01.050. PMID: 17418795; PMCID: PMC4149214.