Molibresib (I-BET-762)

For research use only. Not for use in humans.

目录号:S7189 别名: GSK525762, GSK525762A

Molibresib (I-BET-762) Chemical Structure

CAS No. 1260907-17-2

Molibresib (I-BET-762, GSK525762, GSK525762A) 是一种BET蛋白抑制剂,无细胞试验中IC50约为35 nM,抑制巨噬细胞产生促炎性蛋白质,并抑制急性炎症,对其他溴区结合域包含的蛋白具有高度选择性。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 2923.83 现货
RMB 1859.99 现货
RMB 3838.64 现货
RMB 9582.91 现货
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客户使用Selleck生产的Molibresib (I-BET-762)发表文献21篇:

产品安全说明书

Epigenetic Reader Domain抑制剂选择性比较

生物活性

产品描述 Molibresib (I-BET-762, GSK525762, GSK525762A) 是一种BET蛋白抑制剂,无细胞试验中IC50约为35 nM,抑制巨噬细胞产生促炎性蛋白质,并抑制急性炎症,对其他溴区结合域包含的蛋白具有高度选择性。
靶点
BET proteins [1]
(Cell-free assay)
35 nM
体外研究

I-BET-762抑制BET(溴区和额外的末端结构域) 蛋白, BRD2, BRD3 和 BRD4, 结合到BET的串联溴区,Kd为50.5-61.3 nM, 在FRET分析中,置换BET串联溴区的一种四乙酰化的H4肽,IC50为32.5-42.5 nM。I-BET-762占据BET蛋白的乙酰基-赖氨酸结合口袋,并抑制BET蛋白结合到乙酰化的组蛋白,从而破坏了炎性基因表达必不可少的染色质复合物的形成。[1]分化过程中的第2天使用I-BET-762处理,改变CD4+T细胞的细胞因子产生,上调一些抗炎基因产物的表达,并下调一些促炎细胞因子的表达。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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TY82 MVLGeY5kfGmxbjDhd5NigQ>? MojZNE4zKHSxIEGgeW0> NF;JVpAzPCCqcoO= NFSyfZhKdmirYnn0bY9vKG:oIFLSSFQhcW5iaIXtZY4hXFl6MjDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4h[y2PeXOgcXJPSSCneIDy[ZN{cW:wIHH0JFAvOiC2bzCxJJVOKGGodHXyJFI1KGi{czDifUBTXC2SQ2KgZY5idHm|aYO= NGjNdFg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUWyOVQ{PSd-Mkm1NlU1OzV:L3G+
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TY82 or NCI-H1299 MkXoSpVv[3Srb36gZZN{[Xl? M1nPUFAvOiC2bzCxJJVO MYiyOEBpenN? NWPI[GhIUW6qaXLpeIlwdiCxZjDCVmQ1KGmwIHj1cYFvKFS\OEKgc5IhVkOLLVixNlk6KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDQSE1NOSCvUl7BJIV5eHKnc4Ppc44h[XRiMD6yJJRwKDFidV2gZYZ1\XJiMkSgbJJ{KGK7IGLUMXBEWiCjbnHsfZNqew>? M4HvN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUK1OFM2Lz5{OUWyOVQ{PTxxYU6=
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22Rv1 MknKRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NIHJOFc6PiCqcoO= NFO1VpFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIEKyVpYyKGOnbHzzJIFnfGW{IEm2JIhzeyCkeTDD[YxtNVSrdHXyJIdtdyC{ZXHn[Y51KGKjc3XkJIx2dWmwZYPj[Y5k\SCjc4PhfS=> MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTV2MUO3NUc,Ojl3NEGzO|E9N2F-
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LNCAP MlHORY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M2S1XGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTF7DRXAh[2WubIOsJGlEPTBiPTCwMlM2PjVizszNMi=> MnGwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl5NUi1NVgoRjJ7N{W4OVE5RC:jPh?=
MV411 NFzmPYZEgXSxdH;4bYNqfHliYYPzZZk> M4XzNlczKGi{cx?= MYPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNWlQyOSClZXzsd{Bi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyMWdtdyCjc4PhfUwhUUN3MDC9JFAvQCEQvF2u M1XQSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMk[4O|AzLz5|MEK2PFcxOjxxYU6=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Growth inhibition assay
Cell viability ; 

PubMed: 26840085     


A., B. and C. Dose response curves of MPNST-derived cell lines treated with three bromodomain inhibitors: JQ1, OTX015 and I-BET-762.

26840085
体内研究 I-BET-762保护防止脂多糖诱导的内毒素休克和细菌诱导的脓毒病。LPS注射后1.5小时,单剂量I-BET处理,可治愈小鼠。I-BET每日两次注射,持续2天,保护小鼠免于脓毒症引起的死亡。[1]早期I-BET-762处理实验性自身免疫性脑脊髓炎(EAE)小鼠模型,抑制Th1分化的2D2 T细胞诱发神经性炎症的能力。[2]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
- 合并

荧光共振能量转移(FRET)滴定:

在有四乙酰化的组蛋白H4肽(200 nM)存在时,在50 mM HEPES pH7.5, 50 mM NaCl, 0.5 mM CHAPS中进行对BRD2 (200 nM), BRD3 (100 nM) 和 BRD4 (50 nM)的I-BET滴定。平衡1小时后,在含0.05% (v/v) BSA 和 400 mM KF的实验缓冲液中加入2nM 铕穴状化合物标记的链霉亲和素和10 nM XL-665标记的anti-6His 抗体,使用FRET检测溴区蛋白:肽相互作用。使用Envision酶标仪(激发菠菜320 nm,发射波长615 nm和665 nm)对实验板进行读数。
细胞实验:[2]
- 合并
  • Cell lines: CD4+ T 细胞
  • Concentrations: ~500 nM
  • Incubation Time: 60-72 小时
  • Method: 从10到12周的小鼠淋巴结和脾中分离CD4+ T细胞,在指定细胞因子存在时,使用与板结合的anti-CD3和anti-CD28抗体活化。在最初激活的60-72小时,包含I-BET-762化合物。在T细胞培养和扩张的5天过程中,化合物稀释到初始浓度的12倍。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: 小鼠
  • Dosages: 30 mg/kg
  • Administration: 静脉注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 84 mg/mL (198.15 mM)
Ethanol 42 mg/mL warmed (99.07 mM)
Water Insoluble

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 423.9
化学式

C22H22ClN5O2

CAS号 1260907-17-2
储存条件 粉状
溶于溶剂
别名 GSK525762, GSK525762A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03266159 Withdrawn Drug: GSK525762 Besylate tablets|Drug: Trametinib tablets Solid Tumours GlaxoSmithKline November 27 2017 Phase 2
NCT02964507 Active not recruiting Drug: GSK525762|Drug: Placebo|Drug: Fulvestrant Neoplasms GlaxoSmithKline February 2 2017 Phase 1
NCT01943851 Completed Drug: GSK525762 Neoplasms GlaxoSmithKline May 14 2014 Phase 2
NCT01587703 Completed Drug: GSK525762 Carcinoma Midline GlaxoSmithKline March 28 2012 Phase 1

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

Epigenetic Reader Domain Signaling Pathway Map

Epigenetic Reader Domain Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID