化合物I-BET151 T2120

Product Introduction
Bioactivity


英文名: I-BET151

描述: I-BET151 (GSK1210151A) 是 BRD2/3/4 的特异性 BET 抑制剂，IC50值分别为0.5、0.25、0.79 μM。

细胞实验: Cells are exposed to various concentrations of I-BET151 for 24 or 72 hours in 384-well or 96-well plates. For cell growth inhibition assays, plates are added with CellTiter-Glo reagent using a volume equivalent to the cell culture volume in the wells, shaken for approximately 2 minutes and chemiluminescent signal is read on the Analyst GT or EnVision Plate Reader. For cell proliferation assays, CellTiter-Aqueous One is added to each well and plates are incubated for 4 hours at 37 °C. Absorbance is read at 490 nm on a SpectraMax Gemini reader (Only for Reference)

激酶实验: Fluorescence anisotropy (FP) ligand displacement assay: All components are dissolved in buffer of composition 50 mM HEPES pH 7.4, 150 mM NaCl and 0.5 mM CHAPS with final concentrations of BRD 2/3/4 75 nM, fluorescent ligand 5 nM. 10 μL of this reaction mixture is added using a micro multidrop to wells containing 100 nL of various concentrations of I-BET151 or DMSO vehicle (1% final) in Greiner 384 well Black low volume microtitre plate and equilibrated in the dark for 60 minutes at room temperature. Fluorescence anisotropy is read in Envision (lex = 485 nm, lEM = 530 nm; Dichroic = 505 nM).

体外活性: I-BET151（30 mg/kg/day）处理小鼠,可使鼠类MLL-AF9和人类MLL-AF4白血病肿瘤生长受到明显抑制,显著增加寿命.

体内活性: 作用于HL60核提取物时, I-BET151（0.5或5 μM）抑制BETs(BRD2/3/4/9)而非23种其他溴区蛋白结合到乙酰化的组蛋白肽。I-BET151对含不同 MLL融合的细胞系均有较强抑制效果,如MV4;11, RS4;11, MOLM13和NOMO1细胞（IC50：15-192 nM）。I-BET151对多种不同蛋白类型均有较好的选择性抑制作用,如COX-2,P450,Aurora B,GSK3β,PI3K-γ,GPCR,离子通道及转运体。与I-BET762 (GSK525762A)类似,I-BET151 对BRD2/3/4具有的结合亲和力较高（Kd：0.02-0.1 μM）,作用于人类外周血单核细胞和全血及大鼠WB时,对脂多糖刺激的IL-6细胞因子产生有显著抑制作用（IC50：0.16/1.26/1.26 μM）。

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

溶解度: DMSO : 50 mg/mL (120.35 mM)


关键字: I-BET-151 | I BET151 | inhibit | bromodomain | BET | Epigenetic Reader Domain | BRD2 | Inhibitor | BRD4 | I-BET 151 | BRD3 | I-BET151 | IBET151

相关产品: Menin-MLL inhibitor MI-2 | PROTAC BRD4 Degrader-21 | Menin-MLL inhibitor 29 | BRD4 Inhibitor-27 | BAY-299 | DC-BPi-11 hydrochloride | A-366 | CBP/p300-IN-2 | MZP-55 | 653-47 hydrochloride

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