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

基本信息物理化学性质安全数据常见问题列表

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

GRI977143
GRI977143
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

物理化学性质

储存条件2-8°C

溶解度DMSO：可溶10mg/mL，澄清

形态粉末

颜色白色至浅棕色

安全数据

危险性符号(GHS)

GHS07,GHS09

警示词警告

危险性描述H302-H410

防范说明P264-P270-P273-P301+P312-P391-P501

危险品标志Xn,N

危险类别码22-43-50/53

安全说明36/37-60-61

危险品运输编号UN 3077 9 / PGIII

WGK Germany3

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.