Salubrinal

製品コードS2923 バッチS292301

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₁H₁₇Cl₃N₄OS

分子量

479.81

CAS No.

405060-95-9

Solubility (25°C)*

体外

DMSO

96 mg/mL (200.07 mM)

Ethanol

2 mg/mL (4.16 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Salubrinal is a selective inhibitor of eIF2α dephosphorylation and inhibits ER stress-mediated apoptosis with EC50 of ~15 μM in a cell-free assay.
in vitro	Salubrinal is a selective inhibitor of cellular complexes that dephosphorylate eukaryotic translation initiation factor 2 subunit α (eIF2α). This compound inhibited ER stress-mediated apoptosis induced by the protein glycosylation inhibitor tunicamycin (Tm) in a dose-dependent manner, with a median effective concentration (EC50) ∼ 15 μM. It also suppressed Tm-induced DNA fragmentation the processing of caspase-7, a caspase activated by ER stress. However, this chemical is not a general apoptosis inhibitor. It induced rapid and robust eIF2α phosphorylation and its downstream effects in PC12 cells, including down-regulation of cyclin D1 and up-regulation of GADD34 and CHOP, two proteins whose expression is induced by eIF2α phosphorylation. This inhibitor inhibits eIF2α dephosphorylation by inhibiting the PP1/GADD34 complex. It inhibits HSV replication with IC50 of ~ 3μM by inhibiting eIF2α dephosphorylation. ^[1] This compound increased non-rapid eye movement (NREM) sleep. ^[2]
in vivo	Salubrinal inhibits HSV replication in a mouse cornea infection model. Compared to vehicle control, topical treatment with this compound significantly reduced the viral titer recovered from eye swabs of infected animals. ^[1] I.C.V. administration of this chemical significantly modified the homeostatic sleep response. ^[3]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	PC12
	濃度	0-100 μM
	反応時間	48 hours
	実験の流れ	PC12 cells are plated in 384-well plates at 5000 cells per well in 40μL phenol red-free medium containing 3μg/ml Tm to induce ER stress. 100 nL of the DiverSet E (5 mg/ml in DMSO) or National Cancer Institute’s (NCI) Structural Diversity set and Open Collections (10 mM in DMSO) (NCI) are added to the wells by robotic pin transfer. After 48 hours, cell viability is assessed using a luminescence-based ATP assay. DMSO- and zVAD.fmk-treated wells on each plate served as negative and positive controls for rescue from ER stress-induced ATP loss, respectively.
動物実験	動物モデル	Eight-week-old male CD-1 outbred mice
	投薬量	75μM
	投与方法	On cornea

参考

https://pubmed.ncbi.nlm.nih.gov/15705855/
http://www.ncbi.nlm.nih.gov/pubmed?term=18971348
http://www.ncbi.nlm.nih.gov/pubmed?term=22387272

カスタマーフィードバック

: , , J Am Soc Nephrol, 2015, 26(8):1839-54.

: Data from [Data independently produced by , , Oncogenesis, 2017, 6(5):e341]

: Data from [Data independently produced by , , Neurotox Res, 2017, 31(2):204-217]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Suppressing protein damage response to overcome multidrug resistance in cancer therapy [ Cell Discov, 2025, 11(1):80]	PubMed: 41027888
The integrated stress response fine-tunes stem cell fate decisions upon serine deprivation and tissue injury [ Cell Metab, 2025, 37(8):1715-1731.e11]	PubMed: 40513561
The integrated stress response drives MET oncogene overexpression in cancers [ EMBO J, 2025, 44(4):1107-1130]	PubMed: 39774381
Repressing cytokine storm-like response in macrophages by targeting the eIF2α-integrated stress response pathway [ Int Immunopharmacol, 2025, 147:113965]	PubMed: 39752757
CB-5083 and luteolin synergistically induce the apoptosis of bladder cancer cells via multiple mechanisms [ Toxicol Appl Pharmacol, 2025, 499:117333]	PubMed: 40194745
Palmitate induces integrated stress response and lipoapoptosis in trophoblasts [ Cell Death Dis, 2024, 15(1):31]	PubMed: 38212315
GDF15 ameliorates sepsis-induced lung injury via AMPK-mediated inhibition of glycolysis in alveolar macrophage [ Respir Res, 2024, 25(1):201]	PubMed: 38725041
Multiplex single-cell chemical genomics reveals the kinase dependence of the response to targeted therapy [ Cell Genom, 2024, 4(2):100487]	PubMed: 38278156
Neurotransmitter release progressively desynchronizes in induced human neurons during synapse maturation and aging [ Cell Rep, 2023, 42(2):112042]	PubMed: 36701235
Lovastatin Treatment Inducing Apoptosis in Human Pancreatic Cancer Cells by Inhibiting Cholesterol Rafts in Plasma Membrane and Mitochondria [ Int J Mol Sci, 2023, 24(23)16814]	PubMed: 38069135

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。