An LPA2 receptor agonist (EC50 = 3.3 μM in LPA2-transfected RH7777 cells); selective for LPA2

GRI-977143 – 10 mg

Brand:
Cayman
CAS:
325850-81-5
Storage:
-20
UN-No:
Non-Hazardous - /

GRI-977143 is an agonist of G protein-coupled lysophosphatidic acid receptor 2 (LPA2) with an EC50 value of 3.3 μM in LPA2-transfected RH7777 cells.{40202} It is selective for LPA2, having no activity at LPA1, LPA3, LPA4, and LPA5 at concentrations up to 10 μM. GRI-977143 increases growth and reduces caspase-3 and -7 activation in LPA2-transduced MEF fibroblasts. It increases MM1 rat hepatoma cell invasion and inhibits apoptosis of IEC-6 cells induced by TNF-α, doxorubicin (Item No. 15007), or serum withdrawal. GRI-977143 also rescues apoptotic cells from γ-irradiation-induced injury in vitro and in vivo.{40203}  

 

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Description

An LPA2 receptor agonist (EC50 = 3.3 μM in LPA2-transfected RH7777 cells); selective for LPA2, having no activity at LPA1, LPA3, LPA4, and LPA5 at concentrations up to 10 μM; increases growth and reduces caspase-3 and -7 activation in LPA2-transduced MEF fibroblasts; increases MM1 rat hepatoma cell invasion and inhibits apoptosis of IEC-6 cells induced by TNF-α, doxorubicin, or serum withdrawal; rescues apoptotic cells from γ-irradiation-induced injury in vitro and in vivo

Formal name: 2-[[3-(1,3-dioxo-1H-benz[de]isoquinolin-2(3H)-yl)propyl]thio]-benzoic acid

Synonyms: 

Molecular weight: 391.4

CAS: 325850-81-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Migration & Metastasis

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