化合物SP2509 T2304

Product Introduction
Bioactivity


英文名: SP2509

描述: SP2509 是一种选择性 LSD1拮抗剂，IC50值为 13 nM。

细胞实验: Cultured AML cells are treated with SP2509 and/or PS for 96?h. At the end of treatment, cells are washed free of the drugs and 500 cells per condition are plated in methylcellulose and incubated at 37?°C. Colony formation is measured 7–10 days after plating.(Only for Reference)

激酶实验: SP2509 activity assays: Test compounds are diluted to 20 × the desired test concentration in 100% DMSO and 2.5?μL of the diluted drug sampleis added to a black 384-well plate. The LSD1 enzyme stock is diluted 17-fold with assay buffer and 40?μL of the diluted LSD1 enzyme is added to the appropriate wells. Substrate, consisting of horseradish peroxidase, dimethyl K4 peptide corresponding to the first 21 amino acids of the N-terminal tail of histone H3, and 10-acetyl-3,7-dihydroxyphenoxazine is then added to wells. Resorufin is analyzed on an Envision plate reader with an excitation wavelength of 530?nm and an emission wavelength of 595?nm. The activity of SP2509 on the other oxidases is determined by using commercially available kits. The glucose oxidase activity (which also noncovalently binds FAD in an elongate conformation), is determined using the glucose oxidase kit. The MAO assays are performed using the MAO-glo kit with MAO-A and MAO-B.

体外活性: 在负荷OCI-AML3异种移植物的小鼠中,SP2509（25 mg/kg i.p. ）,能够抑制肿瘤生长,延迟动物的存活.

体内活性: 在OCI-AML3中,SP250能够抑制集落形成,诱导细胞凋亡。在AML细胞中,SP2509能够抑制LSD1与CoREST作用,增加启动子特异性H3K4Me3,同时诱导p53,p21和C/EBPα。在原代AML细胞中,SP2509诱导细胞的增殖。

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

溶解度: DMSO : 36 mg/mL (82.2 mM)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)


关键字: HCI 2509 | Apoptosis | SP 2509 | Histone Demethylase | SP2509 | SP-2509 | inhibit | Inhibitor | HCI2509

相关产品: Alpha-Hederin | Indibulin | GW 5074 | Benzyl isothiocyanate | PARP-2-IN-3 | Hydroxy-PP-Me | (Rac)-Antineoplaston A10 | Fangchinoline | LY2409881 trihydrochloride | Sacubitril/Valsartan

相关库: Anti-Aging Compound Library | Inhibitor Library | Epigenetics Compound Library | Highly Selective Inhibitor Library | Apoptosis Compound Library | Methylation Compound Library | Stem Cell Differentiation Compound Library | Histone Modification Compound Library | Bioactive Compound Library | Chromatin Modification Compound Library

化合物SP2509 T2304信息由TargetMol中国为您提供，如您想了解更多关于化合物SP2509 T2304报价、型号、参数等信息，欢迎来电或留言咨询。

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