325850-81-5
中文名稱
GRI977143; GRI-977143
英文名稱
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 結(jié)構(gòu)式
基本信息
中文別名
2-[3-(1,3-二氧代-1H,3H-苯并[DE]異喹啉-2-基)-丙基磺?；鵠-苯甲酸 英文別名
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
安全數(shù)據(jù)
警示詞警告
危險性描述H302-H410
危險品標(biāo)志Xn,N
危險類別碼22-43-50/53
安全說明36/37-60-61
危險品運輸編號UN 3077 9 / PGIII
WGK Germany3
常見問題列表
生物活性
GRI977143 是特異性的 LPA2 受體的激動劑，其EC50 值為3.3 μM。靶點
|
LPA 2 Receptor 3.3 μM (EC 50 ) |
體外研究
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. |