化合物 Molibresib|T1906|TargetMol

Molibresib
1260907-17-2

￥428 1mg 起订

￥617 2mg 起订

￥913 5mg 起订

上海更新日期：2024-09-23

TargetMol中国（陶术生物）

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产品详情:

中文名称：: 化合物 Molibresib

英文名称：: Molibresib

CAS号：: 1260907-17-2

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.08%

产品类别：: 抑制剂

货号：: T1906

Product Introduction

Bioactivity

Name	Molibresib
Description	Molibresib (GSK525762) is an inhibitor of BET proteins (IC50: about 35 nM).
Cell Research	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)
Kinase Assay	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).
In vitro	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.
In vivo	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）。
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	Ethanol : 39 mg/mL (92 mM) H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 60 mg/mL (141.54 mM)
Keywords	GSK525762A \| Inhibitor \| inhibit \| GSK-525762 \| I-BET-762 \| Epigenetic Reader Domain \| I-BET762 \| Molibresib \| GSK 525762
Inhibitors Related	Bisdemethoxycurcumin \| dBET6 \| 3-methyl-1,2,3,4-tetrahydroquinazolin-2-one \| CeMMEC1 \| (+)-JQ-1 \| Curcumin \| Naphthol AS-E \| J-147 \| ABBV-744 \| Piflufolastat \| Hexamethylene bisacetamide \| Anacardic Acid
Related Compound Libraries	Inhibitor Library \| Bioactive Compound Library \| Anti-Cancer Active Compound Library \| Bioactive Compounds Library Max \| Anti-Aging Compound Library \| Highly Selective Inhibitor Library \| Drug Repurposing Compound Library \| Anti-Cancer Clinical Compound Library \| Anti-Cancer Drug Library \| Reprogramming Compound Library

I-BET 762|||GSK525762|||GSK 525762A|||(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|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子