325850-81-5
中文名称
GRI977143; GRI-977143
英文名称
2-[3-(1,3-Dioxo-1H,3H-benzo[de]isoquinolin-2-yl)-propylsulfanyl]-benzoic acid
CAS
325850-81-5
分子式
C22H17NO4S
分子量
391.44
MOL 文件
325850-81-5.mol
更新日期
2023/03/20 15:41:25
![325850-81-5 结构式](/CAS/GIF/325850-81-5.gif)
基本信息
中文别名
2-[3-(1,3-二氧代-1H,3H-苯并[DE]异喹啉-2-基)-丙基磺酰基]-苯甲酸 英文别名
GRI977143GRI977143
GRI-977143
2-[[3-(1,3-Dioxo-1H-benz[de]isoquinolin-2(3H)-yl)propyl]thio]-benzoic acid
2-((3-(1,3-Dioxo-(1H)benzo[de]isoquinolin-2(3H)-yl)propyl)thio)benzoic Acid
Benzoic acid, 2-[[3-(1,3-dioxo-1H-benz[de]isoquinolin-2(3H)-yl)propyl]thio]-
2-[3-(1,3-Dioxo-1H,3H-benzo[de]isoquinolin-2-yl)-propylsulfanyl]-benzoic acid
常见问题列表
生物活性
GRI977143 是特异性的 LPA2 受体的激动剂,其EC50 值为3.3 μM。靶点
LPA 2 Receptor 3.3 μM (EC 50 ) |
体外研究
GRI977143 (10 μM, 24-72 h) is effective in reducing activation of caspases 3, 7, 8, and 9 and inhibits poly(ADP-ribose)polymerase 1 cleavage and DNA fragmentation in different extrinsic and intrinsic models of apoptosis.
GRI977143 is an effective stimulator of extracellular signal-regulated kinase 1/2 activation and promotes the assembly of a macromolecular signaling complex consisting of LPA2, Na+-H+ exchange regulatory factor 2, and thyroid receptor interacting protein 6.
Cell Proliferation Assay
Cell Line: | Vector- and LPA2-transduced MEF cells (2 × 10 4 ) [1] . |
Concentration: | 10 μM. |
Incubation Time: | 24-72 h. |
Result: | Did not cause a significant increase in vector cell proliferation except at 72 h (p < 0.05). |
Apoptosis Analysis.
Cell Line: | Doxorubicin-induced apoptotic signaling in vector-transduced or LPA2-transduced MEF. |
Concentration: | 10 μM. |
Incubation Time: | 24 h. |
Result: |
Reduced caspase 3 and 7 activation on LPA2-transduced MEF cells by 51 ± 3% and was approximately as potent as 3 μM LPA or OTP.
Protected against doxorubicin-induced apoptosis by inhibiting caspase 3, 7, 8, and 9 and reducing DNA fragmentation. |