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Molibresib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Molibresib图片
CAS NO:1260907-17-2
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
I-BET 762
GSK 525762A
GSK525762
(4S)-6-(4-氯苯基)-N-乙基-8-甲氧基-1-甲基-4H-[1,2,4]三唑并[4,3-a][1,4]苯并二氮杂卓-4-乙酰胺
产品介绍
Molibresib 是一种 BET 溴结构域抑制剂,IC50为32.5在42.5 nM之间。

产品描述

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

体外活性

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.

体内活性

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)。

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 2 nM 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)

Cas No.

1260907-17-2

分子式

C22H22ClN5O2

分子量

423.9

别名

I-BET 762;GSK 525762A;GSK525762;(4S)-6-(4-氯苯基)-N-乙基-8-甲氧基-1-甲基-4H-[1,2,4]三唑并[4,3-a][1,4]苯并二氮杂卓-4-乙酰胺

储存和溶解度

DMSO:78 mg/mL (184 mM)
Ethanol:39 mg/mL (92 mM)
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years