IOX1 - Histone Demethylase 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEIOX1Cat. No.: HY-12304CAS No.: 5852-78-8分式: CHNO分量: 189.17作靶點(diǎn): Histone Demethylase作通路: Epigenetics儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 13.33 mg/mL (70.47 mM; Need ultrasonic and

2、warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 5.2863 mL 26.4313 mL 52.8625 mL5 mM 1.0573 mL 5.2863 mL 10.5725 mL10 mM 0.5286 mL 2.6431 mL 5.2863 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，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(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，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，

3、適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (13.22 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (13.22 mM); Clear solutionBIOLOGICAL ACTIVITY1/3 Master of Small Molecules 您邊的抑制劑師www.MedChem

4、E物活性 IOX1，20G 氧合酶 (2OG oxygenases) 的有效譜抑制劑，包括 JmjC 去甲基酶。IOX1 抑制KDM4C，KDM4E，KDM2A，KDM3A 和 KDM6B 的 IC50 值分別為 0.6 M，2.3 M，1.8 M，0.1 M 和1.4 M。體外研究 IOX1 (0-200 M; 2 hours) inhibits the proliferation and migration of vascular smooth muscle cells (VSMCs)stimulated with angiotensin II (Ang II) in a concentr

5、ation-dependent manner 2.IOX1 (200 M; 24 hours)blocks the cell cycle progression of angiotensin II (Ang II)-VSMCs by increasing the percentage of cells in theG0/G1 phase 2.IOX1 (50-200 M; 2 hours) attenuates cyclin D1 and upregulates p21 mRNA levels in aconcentration-dependent 2.IOX1 (50-200 M; 2 ho

6、urs) mediates cyclin D1 and p21 expression by regainingH3K9me3 2.Cell Proliferation Assay 2Cell Line: Vascular smooth muscle cells (VSMCs)Concentration: 50 M, 100 M, 200 MIncubation Time: Pretreated 2 hoursResult: Exhibited a decrease in proliferation and migration.Cell Cycle Analysis 2Cell Line: Va

7、scular smooth muscle cells (VSMCs)Concentration: 200 MIncubation Time: 24 hoursResult: Slowed down the progression of the cell cycle from the G0/G1 to the S phase.RT-PCR 2Cell Line: Vascular smooth muscle cells (VSMCs)Concentration: 50 M, 100 M, 200 MIncubation Time: 2 hoursResult: Decreased cyclin

8、D1 mRNA expression and increased p21 mRNA expression.RT-PCR 2Cell Line: Vascular smooth muscle cells (VSMCs)Concentration: 50 M, 100 M, 200 MIncubation Time: 2 hoursResult: Enhanced the total protein levels of H3K9me3.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE戶(hù)使本產(chǎn)品發(fā)表的科研獻(xiàn) Patent. US20180263995

9、A1.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Schiller R, et al. A cell-permeable ester derivative of the JmjC histone demethylase inhibitor IOX1. ChemMedChem. 2014 Mar;9(3):566-71.2. Hu Q, et al. IOX1, a JMJD2A inhibitor, suppresses the proliferation and migration of vascular smooth muscle cells induced byangiotensin II by regulating the expression of cell cycle-related proteins. Int J Mol Med. 2016 Jan;37(1):189-96.McePdfHeightCaution: Product has not been fully validated f