首页Chromatin/EpigeneticEpigenetic Reader DomainMolibresib
Molibresib
编号 T1906     别名: I-BET 762, GSK 525762A, GSK525762
CAS 1260907-17-2     分子式 C22H22ClN5O2     分子量 423.90
靶点: BET proteins;
GSK 525762A (I-BET 762) is an inhibitor of BET proteins (IC50: about 35 nM).
纯度:98.82%
规格 库存 单价 数量
2 mg 上海现货 679.00
5 mg 上海现货 1012.00
10 mg 上海现货 1829.00
50 mg 上海现货 7196.00
1 mL * 10 mM (in DMSO) 上海现货 1012.00
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生物活性

产品描述

GSK 525762A (I-BET 762) is an inhibitor of BET proteins (IC50: about 35 nM).

靶点活性

BET proteins,35nM

体外活性

在分化的第2天,I-BET-762处理可改变CD4+T细胞的细胞因子产生,使一些抗炎基因产物的表达上调,并使一些促炎细胞因子的表达下调。I-BET-762抑制溴区和额外的末端结构域的蛋白和BRD2/3/4结合到BET的串联溴区(Kd:50.5-61.3 nM), 在FRET分析中,置换BET串联溴区一种四乙酰化的H4肽(IC50:32.5-42.5 nM)。

体内活性

连续两天每日注射两次I-BET-762,可使小鼠免于脓毒症造成的死亡。I-BET-762可防止细菌诱导的脓毒病和脂多糖诱导的内毒素休克。脂多糖注射后1.5 h,I-BET-762可治愈小鼠。在实验性自身免疫性脑脊髓炎小鼠模型中,I-BET-762早期处理可抑制Th1分化的2D2 T细胞诱发神经性炎症的能力。

激酶实验

Fluorescence resonance energy transfer (FRET) titrations: Fluorescence resonance energy transfer (FRET) titrations. I-BET is titrated against BRD2 (200 nM), BRD3 (100 nM) and BRD4 (50 nM) in 50 mM HEPES pH7.5, 50 mM NaCl, 0.5 mM CHAPS in the presence of tetra-acetylated Histone H4 peptide (200 nM). After equilibrating for 1 hour, the bromodomain protein : peptide interaction is detected using FRET following the addition of 2nM Europium cryptate labelled streptavidin and 10 nM XL-665-labelled anti-6His antibody in assay buffer containing 0.05% (v/v) BSA and 400 mM KF. Plates are read using an Envision Plate reader (excitation 320 nm, emission 615 nm and 665 nm).

细胞实验

CD4+ T cells are isolated from lymph nodes and spleens of 10- to 12-wk old mice and activated with plate bound anti-CD3 and anti-CD28 antibodies in the presence of indicated cytokines. I-BET-762 compounds is included during the 60–72 h of initial activation. Over the course of 5 d of T-cell culture and expansion, the compounds is diluted 12-fold relative to the starting concentrations.(Only for Reference)

细胞系: CD4+ T cells

动物实验

动物模型:Mouse

化学信息

分子量

423.90

分子式

C22H22ClN5O2

CAS

1260907-17-2

溶解度

DMSO: 78 mg/mL (184 mM)

Ethanol: 39 mg/mL (92 mM)

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

store at -80°C

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 2.359 ml 11.795 ml 23.59 ml
5 mM 0.472 ml 2.359 ml 4.718 ml
10 mM 0.236 ml 1.18 ml 2.359 ml
50 mM 0.047 ml 0.236 ml 0.472 ml
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