GRI977143; GRI-977143

生物活性靶点体外研究 GRI977143; GRI-977143 试剂级价格

CAS号:325850-81-5
英文名:2-[3-(1,3-Dioxo-1H,3H-benzo[de]isoquinolin-2-yl)-propylsulfanyl]-benzoic acid
中文名:GRI977143; GRI-977143
CBNumber:CB42652142
分子式:C22H17NO4S
分子量:391.44
MOL File:325850-81-5.mol

GRI977143; GRI-977143化学性质

储存条件 :2-8°C
溶解度 :DMSO: soluble10mg/mL, clear
形态 :powder
颜色 :white to light brown

安全信息

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 Germany :3

GRI977143; GRI-977143性质、用途与生产工艺

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.