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| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
TWS119, 糖原合酶激酶 3 beta 抑制剂
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
TWS119已被用作糖原合酶激酶3β（GSK-3β）GSK3β抑制剂
Information
TWS119 is aGSK-3βinhibitor withIC50of 30 nM in a cell-free assay; capable of inducing neuronal differentiation and may be useful to stem cell biology. GSK-3β inhibition triggersautophagy.
In vitro
Treatment of a monolayer of P19 cells with 1 μM TWS119 causes 30–40% cells to differentiate specifically into neuronal lineages based on countingof TuJ1 positive cells with correct neuronal morphology (up to 60% neuronal differentiation occurred through the standard EB formation protocol with concomitant TWS119 treatment). TWS119 tightly binds to GSK-3β (K D = 126 nM) which is quantified by surface plasmon resonance (SPR) and further demonstrates an IC50 of 30 nM. TWS119 is found to potently induces neuronal differentiation in both mouse embryonal carcinoma and ES cells. TWS119 treatment towards hepatic stellate cells (HSC) leads to reduced b-catenin phosphorylation, induces nuclear translocation of b-catenin, elevates glutamine synthetase production, impedes synthesis of smooth muscle actin and Wnt5a, but promotes the expression of glial fibrillary acidic protein, Wnt10b, and paired-like homeodomain transcription factor 2c. TWS119 triggers a rapid accumulation of β-catenin (mean 6.8 -fold increase by densitometry), augments nuclear protein interaction with oligonucleotide containing the DNA sequences to which Tcf and Lef bind and sharply up-regulates the expression of Tcf7, Lef1 and other Wnt target genes including Jun, Ezd7 (encoding Frizzled-7), Nlk (encoding Nemo-like kinase). TWS119 induces a dose-dependent decrease in T cell-specific killing and IFN-g release associated with the preservation of the ability to produce IL-2. A recent study indicates Wnt signaling is induced in polyclonally activated human T cells by treatment with TWS119. These T cells preserve a native CD45RA(+)CD62L(+) phenotype compared with control-activated T cells that progresses to a CD45RO(+)CD62L(-) effector phenotype and this occurs in a TWS119 dose-dependent manner. TWS119-induced Wnt signaling reduces T cell expansion as a result of a block in cell division, and impairs acquisition of T cell effector function as measured by degranulation and IFN-γ production in response to T cell activation. The block in T cell division may be attributed to reduced IL-2Rα expression in TWS119-treated T cells that lowers their capacity to use autocrine IL-2 for expansion.
In vivo
A cell population that expressed low levels of CD44 and high levels of CD62L on the cell surface when 30 mg/kg of TWS119 is administered.
Cell Data
cell lines：CLL cells
Concentrations：
Incubation Time：
Powder Purity:≥95%
规格
英文别名
3-(6-(3-aminophenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yloxy)phenol
规格或纯度
Moligand™, 10mM in DMSO
英文名称
TWS119
生化机理
TWS119 是一种 GSK-3β 抑制剂，在无细胞试验中的 IC50 为 30 nM；能够诱导神经元分化，可能对干细胞生物学有用。抑制 GSK-3β 可引发自噬。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
糖原合酶激酶 3 beta 抑制剂
名称和识别符
EC号
637-358-8
分子类型
小分子
Isomeric SMILES
C1=CC(=CC(=C1)N)C2=CC3=C(N2)N=CN=C3OC4=CC=CC(=C4)O
PubChem CID
分子量
318.33
技术文档
高级数据
关联靶点（人）
GSK3B
Tclin
糖原合酶激酶-3β(Glycogen synthase kinase-3 beta)
(1 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro Water: 45 mg/mL (197.13 mM); DMSO: Insoluble;
熔点
249 °C
安全和危险性（GHS）
象形图
信号词
Warning
危险声明
H319: 引起严重眼睛刺激
H302: 吞食有害
预防措施声明
P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。
P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。
P501: 将内容物/容器处理到。。。
P264: 处理后要彻底洗手。
P270: 使用本产品时，请勿进食、饮水或吸烟。
P330: 漱口
P264+P265: 处理后彻底洗手[和…]。不要触摸眼睛。
P301+P317: 如果被吞咽：请寻求医疗帮助。
P337+P317: 如果眼睛刺激持续：寻求医疗帮助。
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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