毛壳素 T6803

Product Introduction
Bioactivity


英文名: Chaetocin

描述: Chaetocin 特异性抑制组蛋白甲基转移酶(HMT) SU(VAR)3-9，IC50值为0.6 μM。它还可抑制硫氧还蛋白还原酶，IC50值为4 μM。

细胞实验: HeLa cells are transfected with 1 μg pcDNA or pcDNA-Trx. Twenty four h after transfection the cells are treated with either DMSO, 100 nM chaetocin or 100 nM doxorubicin for 24 h. The cells are then trypsinized and manually counted in trypan blue to exclude dead cells. For immunoblotting (24 h after transfections), cells are trypsinized, ished in cold PBS, and lysed in CelLytic lysis buffer containing protease inhibitors. Protein is analyzed by BCA assay and lysates are electrophoresed on 15% SDS-PAGE gels and transferred to nitrocellulose. Immunoblotting for thioredoxin and actin is then performed[2].

体外活性: In SL-2 Drosophila tissue culture cells, Chaetocin causes the inhibition of SU(VAR)3-9 and the number of H3 molecules dimethylated at Lys9, and also inhibits cell growth. [1] In HepG2, Hep3B, and Huh7 human hepatoma cells, Chaetocin inhibits HIF-1-Mediated hypoxic responses. [2] Chaetocin also potently inhibits proliferation and colony formation in a broad range of cancer cell lines with IC50 of 2-10 nM. [3]

体内活性: In Hepa 1c1c-7 tumor-bearing mice, Chaetocin (0.25 mg/kg, i.p.) inhibits tumor growth by deregulating HIF-1[alpha]-mediated angiogenesis. [2] In SKOV3 tumor-bearing nude mice, chaetocin treatment (0.25 mg/kg, i.p.) significantly delays the tumor growth with minimal evidence of toxicities. [3]

存储条件: store at low temperaturePowder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 7 mg/mL (10 mM)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)


关键字: Inhibitor | Histone Methyltransferase | Antibiotic | inhibit | Chaetocin | Bacterial

相关产品: WDR5-47 | MS023 | JIB-04 | Sinefungin | UNC3866 | EEDi-5285 | Metoprine | EZH2-IN-2 | UNC0224 | UNC6852

相关库: Epigenetics Compound Library | Natural Product Library for HTS | Microbial Natural Product Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途