4μ8C

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4μ8C

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:

14003-96-4

IRE1 Inhibitor III

4μ8C (IRE1 Inhibitor III)是IRE1α的小分子抑制剂。

生物活性

4μ8C (IRE1 Inhibitor III) is a small-molecule inhibitor ofIRE1α.

体外研究
(In Vitro)

When applies to the media of ER stressed cultured cells, 4μ8C (IRE1 Inhibitor III) inhibits Xbp1 splicing in a concentration-dependent manner. 4μ8C dissociates slowly from IRE1, but ishout of inhibitor leads to rapid recovery of Xbp1 splicing in cells^[1].The IRE1 endoribonuclease inhibitor 4μ8c prevents the splicing of the XBP1 mRNA in response to ER stress caused by mutant proinsulin production^[2]. The inositol-requiring enzyme 1α (IRE1α) is a serine-threonine kinase that plays crucial roles in activating the unfolded protein response. 4μ8C treatment dramatically inhibits IL-4 production by CD4⁺T cells under Th0 conditions because both the IL-4 levels in the culture supernatant and the percentage of IL-4 positive cells are reduced by 4μ8C treatment. In addition, both IL-5 and IL-13 production are significantly reduced upon treatment with 4μ8C^[3].

体内研究
(In Vivo)

4μ8c (IRE1 Inhibitor III) (i.p. injection; 10 mg/kg/day for 4 more weeks) leads to a significant reduction (45.2%) in atherosclerotic lesion area in en face aorta preparations. 4μ8c can effectively mitigate plaque development in mice^[4].
4μ8C (orally; 10, 50, or 100 mg/kg) suppresses passive cutaneous anaphylaxis (PCA) in mice (ED50 = 25.1 mg/kg)^[5].
4μ8C reverses the ER stress-dependent loss of several known RIDD targets, with an EC₅₀of approximately 4 μM, approximating that of inhibition of XBP1 target gene activation^[1].

Animal Model:	ApoE^-/-mice^[4]
Dosage:	10 mg/kg
Administration:	I.p. injection; daily; for 4 more weeks
Result:	Led to a significant reduction (45.2%) in atherosclerotic lesion area in en face aorta preparations.

分子量

204.18

性状

Solid

Formula

C₁₁H₈O₄

CAS 号

14003-96-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 27 mg/mL(132.24 mM)

*"≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	4.8976 mL	24.4882 mL	48.9764 mL
5 mM	0.9795 mL	4.8976 mL	9.7953 mL
10 mM	0.4898 mL	2.4488 mL	4.8976 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。-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： 10% DMSO 40%PEG300 5%Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (10.19 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (10.19 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在本网站选购。