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4μ8C (Synonyms: IRE1 Inhibitor III)
4μ8C (IRE1 Inhibitor III)是IRE1α的小分子抑制劑。
生物活性
4μ8C (IRE1 Inhibitor III) is a small-molecule inhibitor of IRE1α.
體外研究(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].
體內(nèi)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 EC50 of 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
性狀：Solid
Formula：C11H8O4
CAS 號(hào)：14003-96-4
運(yùn)輸條件：Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
| Powder | -20°C | 3 years |
|---|---|---|
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
溶解性數(shù)據(jù)
DMSO : ≥ 27 mg/mL (132.24 mM)
* "≥" means soluble, but saturation unknown.
| 濃度溶劑體積質(zhì)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 |
請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)月內(nèi)使用，-20°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。
以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用； 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶
參考文獻(xiàn)
[1]. Cross BC, et al. The molecular basis for selective inhibition of unconventional mRNA splicing by an IRE1-binding small molecule. Proc Natl Acad Sci U S A. 2012 Apr 10;109(15):E869-78. [Content Brief]
[2]. Zhang L, et al. IRE1 inhibition perturbs the unfolded protein response in a pancreatic β-cell line expressing mutant proinsulin, but does not sensitize the cells to apoptosis. BMC Cell Biol. 2014 Jul 10;15:29. [Content Brief]
[4]. Tufanli O, et al. Targeting IRE1 with small molecules counteracts progression of atherosclerosis. Proc Natl Acad Sci U S A. 2017 Feb 21;114(8):E1395-E1404. [Content Brief]
[5]. Nam ST, et al. Suppression of IgE-mediated mast cell activation and mouse anaphylaxis via inhibition of Sykactivation by 8-formyl-7-hydroxy-4-methylcoumarin, 4μ8C. Toxicol Appl Pharmacol. 2017 Oct 1;332:25-31. [Content Brief]
4μ8C (Synonyms: IRE1 Inhibitor III)
4μ8C (IRE1 Inhibitor III)是IRE1α的小分子抑制劑。
生物活性
4μ8C (IRE1 Inhibitor III) is a small-molecule inhibitor of IRE1α.
體外研究(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].
體內(nèi)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 EC50 of 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
性狀：Solid
Formula：C11H8O4
CAS 號(hào)：14003-96-4
運(yùn)輸條件：Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
| Powder | -20°C | 3 years |
|---|---|---|
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
溶解性數(shù)據(jù)
DMSO : ≥ 27 mg/mL (132.24 mM)
* "≥" means soluble, but saturation unknown.
| 濃度溶劑體積質(zhì)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 |
請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)月內(nèi)使用，-20°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。
以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用； 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶
參考文獻(xiàn)
[1]. Cross BC, et al. The molecular basis for selective inhibition of unconventional mRNA splicing by an IRE1-binding small molecule. Proc Natl Acad Sci U S A. 2012 Apr 10;109(15):E869-78. [Content Brief]
[2]. Zhang L, et al. IRE1 inhibition perturbs the unfolded protein response in a pancreatic β-cell line expressing mutant proinsulin, but does not sensitize the cells to apoptosis. BMC Cell Biol. 2014 Jul 10;15:29. [Content Brief]
[4]. Tufanli O, et al. Targeting IRE1 with small molecules counteracts progression of atherosclerosis. Proc Natl Acad Sci U S A. 2017 Feb 21;114(8):E1395-E1404. [Content Brief]
[5]. Nam ST, et al. Suppression of IgE-mediated mast cell activation and mouse anaphylaxis via inhibition of Sykactivation by 8-formyl-7-hydroxy-4-methylcoumarin, 4μ8C. Toxicol Appl Pharmacol. 2017 Oct 1;332:25-31. [Content Brief]
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