Salubrinal

製品コードS2923 バッチS292304

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	3 mg/mL (6.25 mM)
		Water	Insoluble
* <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). Salubrinal 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. Salubrinal also suppressed Tm-induced DNA fragmentation the processing of caspase-7, a caspase activated by ER stress. However, Salubrinal is not a general apoptosis inhibitor. Salubrinal 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. Salubrinal inhibits eIF2α dephosphorylation by inhibiting the PP1/GADD34 complex. Salubrinal inhibits HSV replication with IC50 of ~ 3μM by inhibiting eIF2α dephosphorylation. ^[1] Salubrinal 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 Salubrinal treatment significantly reduced the viral titer recovered from eye swabs of infected animals. ^[1] I.C.V. administration of Salubrinal 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-freemedium containing 3μg/ml Tm to induce ER stress. 100 nL of the DiverSet E (5 mg/mlin 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

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：

Palmitate induces integrated stress response and lipoapoptosis in trophoblasts [ Cell Death Dis, 2024, 15(1):31]	PubMed: 38212315
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
Nuclear fragile X mental retardation-interacting protein 1-mediated ribophagy protects T lymphocytes against apoptosis in sepsis [ Burns Trauma, 2023, 11:tkac055]	PubMed: 36873287
Hesperadin suppresses pancreatic cancer through ATF4/GADD45A axis at nanomolar concentrations [ Oncogene, 2022, 10.1038/s41388-022-02328-4]	PubMed: 35551503
PARP1 Might Substitute HSF1 to Reactivate Latent HIV-1 by Binding to Heat Shock Element [ Cells, 2022, 11(15)2331]	PubMed: 35954175
Neurodegeneration Risk Factor, EIF2AK3 (PERK), Influences Tau Protein Aggregation [ J Biol Chem, 2022, S0021-9258(22)01264-9]	PubMed: 36563857
Pazopanib restricts small cell lung cancer proliferation via reactive oxygen species-mediated endoplasmic reticulum stress [ Thorac Cancer, 2022, 13(17):2421-2428]	PubMed: 35866204
mTORC1 couples cyst(e)ine availability with GPX4 protein synthesis and ferroptosis regulation [ Nat Commun, 2021, 12(1):1589]	PubMed: 33707434
Sestrin2 protects dendrite cells against ferroptosis induced by sepsis [ Cell Death Dis, 2021, 12(9):834]	PubMed: 34482365

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。

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