所有图片(1)
别名:
2-[(3,4-Dihydro-4-oxo-3,5-diphenylthieno[2,3-d]pyrimidin-2-yl)thio]-acetic acid hydrazide
经验公式（希尔记法）:
C20H16N4O2S2
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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, clear
储存温度
−20°C
InChI
1S/C20H16N4O2S2/c21-23-16(25)12-28-20-22-18-17(15(11-27-18)13-7-3-1-4-8-13)19(26)24(20)14-9-5-2-6-10-14/h1-11H,12,21H2,(H,23,25)
InChI key
WLBUICQBNZXIDJ-UHFFFAOYSA-N
生化/生理作用
LDN-27219 is a revesible inhibitor of transglutaminase 2 (TG2) that binds to the GTP binidng site of the enzyme and inhbits activity with and IC50 of 600 nM.
LDN-27219 is a thieno[2,3-d]pyrimidine-4-one-acylhydrazide derivative. Closed conformation of TG2 induced by LDN-27219 can be a potential therapeutic strategy for age-related vascular dysfunction and lowering blood pressure.
警示用语：
Warning
危险声明
危险分类
Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
靶器官
Respiratory system
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Nayeon Kim et al.
Organic & biomolecular chemistry, 12(27), 4932-4940 (2014-06-01)
In the process of optimization, we developed a novel core skeleton of thieno[3,4-b]pyrazine via GK-13. The derivatives synthesized were shown to inhibit TGase 2 activity in cancer cells. Some of the hit compounds such as the arylethynyl group-coupled thieno[3,4-b]pyrazine derivatives
Estéfano Pinilla et al.
Hypertension (Dallas, Tex. : 1979), 77(1), 216-227 (2020-12-01)
Transglutaminase 2 (TG2) is an enzyme which in the open conformation exerts transamidase activity, leading to protein cross-linking and fibrosis. In the closed conformation, TG2 participates in transmembrane signaling as a G protein. The unspecific transglutaminase inhibitor cystamine causes vasorelaxation
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