Salubrinal

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Salubrinal

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

405060-95-9

Salubrinal 是有效的选择性eIF2α去磷酸化抑制剂。Salubrinal 作为双特异性磷酸酶 2 (Dusp2) 抑制剂，抑制抗胶原蛋白抗体诱导的关节炎。Salubrinal 具有抗HSV-1病毒的活性，并抑制由HSV-1蛋白 ICP34.5 介导的eIF2α的去磷酸化。

生物活性

Salubrinal is a cell-permeable and selective inhibitor ofeIF2α dephosphorylation^[1]. Salubrinal acts as a dual-specificityphosphatase2 (Dusp2) inhibitor and suppresses inflammation in anti-collagen antibody-induced arthritis^[2]. Salubrinal has antiviral activity againstHSV-1and inhibits dephosphorylation ofeIF2αmediated by theHSV-1protein ICP34.5^[3].

IC₅₀& Target

HSV-1

Dusp2

体外研究
(In Vitro)

Salubrinal, a recently identified PP1 inhibitor capable to protect against endoplasmic reticulum (ER) stress in various model systems, strongly synergized with proteasome inhibitors to augment apoptotic death of different leukemic cell lines. Salubrinal preferentially seems to target the PP1/GADD34 complex, Salubrinal is of interest to examine whether the effect of Salubrinal could also be recapitulated by another inhibitor of this phosphatase. For this purpose cantharidin, wis selected, which is less toxic than okadaic acid, but which also blocks PP1 (IC₅₀=1.7 μM) activities^[1].

体内研究
(In Vivo)

Salubrinal is a synthetic chemical that inhibits de-phosphorylation of eukaryotic translation initiation factor 2 alpha (eIF2α). Salubrinal significantly suppresses inflammation of the paws of CAIA mice. For instance, the clinical scores are 1.94±1.7 (placebo) and 0.31±0.6 (Salubrinal) on day 6; and 4.63±3.4 (placebo) and 1.09±1.6 (Salubrinal) on day 12. Consistent with the clinical scores, the thickening of the paws is also reduced in the Salubrinal-treated group. Furthermore, Salubrinal reduces the histological scores from 1.47±1.10 (N=16; placebo) to 0.59±0.64 (N=16; Salubrinal) (p=0.01)^[2].

分子量

479.81

性状

Solid

Formula

C₂₁H₁₇Cl₃N₄OS

CAS 号

405060-95-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

In Vitro:

DMSO : 50 mg/mL(104.21 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	2.0842 mL	10.4208 mL	20.8416 mL
5 mM	0.4168 mL	2.0842 mL	4.1683 mL
10 mM	0.2084 mL	1.0421 mL	2.0842 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.
请依序添加每种溶剂： 45%PEG300 5%Tween-80 50% saline
Solubility: 10 mg/mL (20.84 mM); Suspended solution; Need ultrasonic

*以上所有助溶剂都可在本网站选购。