质量水平
检测方案
≥98% (HPLC)
形式
powder
颜色
white to beige
溶解性
DMSO: >15 mg/mL
储存温度
2-8°C
SMILES字符串
O=C1SN(C(=O)N1Cc2ccccc2)c3cccc4ccccc34
InChI
1S/C19H14N2O2S/c22-18-20(13-14-7-2-1-3-8-14)19(23)24-21(18)17-12-6-10-15-9-4-5-11-16(15)17/h1-12H,13H2
InChI key
PMJIHLSCWIDGMD-UHFFFAOYSA-N
基因信息
human ... GSK3B(2932)
应用
Tideglusib已被用于:
- 作为ADP-GloTM激酶测定中的参考化合物
- 作为GSK-3的变构抑制剂β 研究其对心肌重塑和血管生成的影响
- 作为分化剂(具体而言是糖原合酶激酶(GSK)-3β 抑制剂)将成纤维细胞转化为八聚物结合转录因子4(OCT4)+和血管内皮生长因子受体2(VEGFR-2/胎儿肝激酶1(FLK1)+细胞
生化/生理作用
Tideglusib,也称为 NP031112 或 NP-12,是一种强效非 ATP 竞争性糖原合成酶激酶-3 (GSK3) 抑制剂,GSK3 是研究干细胞研究和神经退行性疾病的重要激酶。目前正处于阿尔茨海默氏症和进行性核上性麻痹 (PSP)临床试验阶段研究。Tideglusib 可减少 tau 蛋白的磷酸化和淀粉样斑块的积聚,减少海马和内嗅皮层神经元的丢失并改善空间记忆缺陷。在多种动物模型中也显示出神经保护和抗炎活性。
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Combined Shape-Based Screening and Molecular Docking Approach
International Journal of Pharmaceutical Sciences and Drug Research, 9(3), 145-148 (2017)
The allosteric glycogen synthase kinase-3 inhibitor NP12 limits myocardial remodeling and promotes angiogenesis in an acute myocardial infarction model
The Journal of Biological Chemistry, 292(50), 20785-20798 (2017)
Chromatin-modifying agents convert fibroblasts to OCT4+ and VEGFR-2+ capillary tube-forming cells
Testing, 12(5), e0176496-e0176496 (2017)
Molecular cancer therapeutics, 18(6), 1081-1091 (2019-04-25)
Pioneering success of antibodies targeting immune checkpoints such as PD-1 and CTLA4 has opened novel avenues for cancer immunotherapy. Along with impressive clinical activity, severe immune-related adverse events (irAE) due to the breaking of immune self-tolerance are becoming increasingly evident
商品
Glycogen synthase kinase 3 (GSK-3) is a highly conserved family of serine/threonine kinases for over 100 proteins in many pathways. See a list of accepted GSK-3 modulators and related products.
肝醣合成酶激酶3 (GSK-3)是一种高度保守的丝氨酸/苏氨酸激酶家族,适于在多种途径中处理100多种蛋白质。查看允许的GSK-3调节剂和相关产品列表。
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