(2'Z,3'E)-6-溴靛玉红-3'-肟, 细胞周期蛋白依赖性激酶 1 抑制剂;细胞周期蛋白依赖性激酶 5 抑制剂;糖原合酶激酶 3 alpha 抑制剂;糖原合酶激酶 3 beta 抑制剂

JAK3 选择性抑制剂
有货

库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
B407765-1ml
1ml 现货 Stock Image
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Compound libraries (12332)

基本描述

英文别名 GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime, 6-Bromoindirubin-3'-oxime, MLS 2052 | 2H-Indol-2-one, 6-bromo-3-[(3E)-1,3-dihydro-3-(hydroxyimino)-2H-indol-2-ylidene]-1,3-dihydro-, (3Z)-
规格或纯度 Moligand™, 10mM in DMSO
英文名称 BIO
生化机理 BIO(GSK-3 抑制剂 IX,6-溴靛玉红-3-肟,6-Bromoindirubin-3\'-oxime,MLS 2052)是一种 GSK-3 特异性抑制剂,在无细胞试验中对 GSK-3α/β 的 IC50 为 5 nM,对 CDK5 的选择性大于 16 倍,也是一种泛 JAK 抑制剂,对 Tyk2 的 IC50 为 30 nM。BIO 可诱导人类黑色素瘤细胞凋亡。
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 抑制剂
作用机制 细胞周期蛋白依赖性激酶 1 抑制剂;细胞周期蛋白依赖性激酶 5 抑制剂;糖原合酶激酶 3 alpha 抑制剂;糖原合酶激酶 3 beta 抑制剂
产品介绍

BIO

Information

BIO (GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime, 6-Bromoindirubin-3'-oxime, MLS 2052) is a specific inhibitor ofGSK-3withIC50of 5 nM for GSK-3α/β in a cell-free assay, shows >16-fold selectivity over CDK5, also a pan-JAKinhibitor with IC50 of 30 nM forT
In vitro

BIO (6-bromoindirubin-3\'-oxime) is a specific inhibitor of glycogen synthase kinase-3 (GSK-3), with IC50 of 5 nM for GSK-3α/β, shows >16-fold selectivity over CDK5. BIO interacts within the ATP binding pocket of these kinases, reduces β-catenin phosphorylation on a GSK-3-specific site in cellular models, closely mimicks Wnt signaling in Xenopus embryos. In human and mouse embryonic stem cells, BIO maintains the undifferentiated phenotype and sustains expression of the pluripotent state-specific transcription factors Oct-3/4, Rex-1 and Nanog. BIO-mediated Wnt activation is functionally reversible, as withdrawal of the compound leads to normal multidifferentiation programs in both human and mouse embryonic stem cells. BIO promotes proliferation in mammalian cardiomyocytes. 6BIO is also a pan-JAK inhibitor, with IC50 values of 0.03, 1.5, 8.0, 0.5 μM for TYK2, JAK1, JAK2 and JAK3. BIO selectively inhibits phosphorylation of STAT3 and induces apoptosis of human melanoma cells.

In vivo

BIO suppresses melanoma tumor growth in a mouse xenograft model.
Cell Data

cell lines:

Concentrations:~10 μM

Incubation Time:12 or 24 h

Powder Purity:≥99%

产品属性

IC50 JAK3, IC50: 0.5 μM

关联靶点(人)

CDK1 Tchem 细胞周期蛋白依赖性激酶 1(Cyclin-dependent kinase 1) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
CDK5 Tchem 细胞周期蛋白依赖性类激酶 5(Cyclin-dependent-like kinase 5) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
GSK3B Tclin 糖原合酶激酶-3β(Glycogen synthase kinase-3 beta) (0 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
GSK3A Tclin 糖原合酶激酶-3α(Glycogen synthase kinase-3 alpha) (0 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

Canonical SMILES O\N=C/1\C(NC2=CC=CC=C12)=C3\C(=O)NC4=C3C=CC(=C4)Br
分子量 356.17

化学和物理性质

溶解性 Solubility (25°C) In vitro DMSO: 44 mg/mL (197.98 mM);    

安全和危险性(GHS)

技术规格说明书

Concentration 9-11(mmol/L)
Proton NMR spectrum Conforms to Structure

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

溶液计算器

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