5-羰基-8-羟基喹啉 T6545

Product Introduction
Bioactivity


英文名: IOX1

描述: IOX1是 2OG 氧合酶的一种广谱抑制剂，抑制 ALKBH5，包括 JmjC 去甲基酶。它抑制 KDM4C、KDM4E、KDM2A、KDM3A 和 KDM6B 的IC50值分别为 0.6、2.3、1.8、0.1 和 1.4 μM。

细胞实验: Antiproliferative activities of compounds are determined by the MTT assay. HeLa cells are seeded into 96-well plates and cultured at 37 °C for 24 h to achieve 70%. Subsequently, the medium is replaced with DMEM medium containing the tested compounds in different concentrations of 1-300 μM in 1% DMSO. Staurosporine in 0.03-10 μM final concentration is used as a control for cytotoxicity. After 24 h of treatment, the medium is replaced with CellTiter 96 Aqueous One Solution Reagent and incubated for 4 hours. CC50 values are calculated in Prism 6 software after normalisation against corresponding 1% DMSO treated cells and 1% DMSO in media (no cells) controls.(Only for Reference)

激酶实验: AlphaScreen Assay: All reagents are diluted in 50 mM HEPES, 0.1% BSA, pH 7.5 supplemented with 0.01% Tween20 and allowed to equilibrate to room temperature prior to addition to plates. Catalytic turnover assays are run in 10 μL volumes in lowvolume 384-well plates at RT. The reaction consisted of enzyme (5 nM), biotinylated substrate peptide (30 nM), Fe(II) (1 μM), ascorbate (100 μM), 2OG (10 μM) and run at RT. For PHD2, the reaction consisted of enzyme (5 nM), biotinylated substrate peptide (60 nM), Fe(II) (20 μM), ascorbate (200 μM), 2OG (2 μM) and run at RT. EDTA is used to quench the reaction (5 μL), AlphaScreen donor (Streptavidin-conjugated) and acceptor (Protein A-conjugated) beads preincubated with peptide product antibodies are added (5 μL). Plates are foil-sealed to protect from light, incubated at room temperature for 60 minutes and read on a PHERAstar FS plate reader using an AlphaScreen 680 excitation/570 emission filter set. The final bead concentration in 20 μL reaction is 20 μg/mL. IC50 values are calculated in Prism 6 after normalisation against corresponding DMSO controls.

体外活性: IOX1在体外对一系列2OG氧化酶（包括非JmjC 2OG氧化酶）表现出具有微摩尔范围的IC50值，是最有效的抑制剂。然而，在HeLa细胞中，其IC50为86uM，效能大约低百倍，这可能是由于其极性的C-5羧基团导致的低细胞渗透性。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (165.31 mM)


关键字: Inhibitor | inhibit | IOX-1 | Histone Demethylase | IOX 1 | IOX1

相关产品: KDM4D-IN-1 | LSD1-IN-6 | PFI-90 | JIB-04 | JQKD82 trihydrochloride | 3-pyridine toxoflavin | Iadademstat dihydrochloride | GSK 690 Hydrochloride | KDM5A-IN-1 | GSK2879552 2HCl (1401966-69-5(free base))

相关库: Anti-Aging Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Epigenetics Compound Library | Stem Cell Differentiation Compound Library | Methylation Compound Library | Histone Modification Compound Library | NO PAINS Compound Library | Chromatin Modification Compound Library | Bioactive Compound Library

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