Giripladib - CAS 865200-20-0
Catalog number: 865200-20-0
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
Giripladib is a Phospholipase A2 inhibitor. Treatment with Giripladib attenuated radiation induced increases of phospho-ERK and phospho-Akt in endothelial cells. Giripladib in combination with irradiation significantly reduced migration and proliferation in endothelial cells and induced cell death and attenuated invasion by tumor cells.
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4-[3-[5-Chloro-1-(diphenylmethyl)-2-[2-[[[[2-(trifluoromethyl)phenyl]methyl]sulfonyl]amino]ethyl]-1H-indol-3-yl]propyl]benzoic Acid; 4-(3-[5-Chloro-1-(diphenylmethyl)-2-[2-(((2-(trifluoromethyl)benzyl)sulfonyl)amino)ethyl]-1H-indole-3-yl]propyl)benzoic Acid; PLA 695
Soluble in DMSO
-20℃ Freezer
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Canonical SMILES:
Current Developer:
Originator Wyeth
1.Cytosolic phospholipaseA2 inhibition with PLA-695 radiosensitizes tumors in lung cancer animal models.
Thotala D1, Craft JM, Ferraro DJ, Kotipatruni RP, Bhave SR, Jaboin JJ, Hallahan DE. PLoS One. 2013 Jul 19;8(7):e69688. doi: 10.1371/journal.pone.0069688. Print 2013.
Lung cancer remains the leading cause of cancer deaths in the United States and the rest of the world. The advent of molecularly directed therapies holds promise for improvement in therapeutic efficacy. Cytosolic phospholipase A2 (cPLA2) is associated with tumor progression and radioresistance in mouse tumor models. Utilizing the cPLA2 specific inhibitor PLA-695, we determined if cPLA2 inhibition radiosensitizes non small cell lung cancer (NSCLC) cells and tumors. Treatment with PLA-695 attenuated radiation induced increases of phospho-ERK and phospho-Akt in endothelial cells. NSCLC cells (LLC and A549) co-cultured with endothelial cells (bEND3 and HUVEC) and pre-treated with PLA-695 showed radiosensitization. PLA-695 in combination with irradiation (IR) significantly reduced migration and proliferation in endothelial cells (HUVEC & bEND3) and induced cell death and attenuated invasion by tumor cells (LLC &A549). In a heterotopic tumor model, the combination of PLA-695 and radiation delayed growth in both LLC and A549 tumors.
2.Platelet Lipidomic Profiling: Novel Insight into Cytosolic Phospholipase A2α Activity and Its Role in Human Platelet Activation.
Duvernay MT1, Matafonov A2, Lindsley CW3, Hamm HE1. Biochemistry. 2015 Sep 15;54(36):5578-88. doi: 10.1021/acs.biochem.5b00549. Epub 2015 Sep 1.
With a newer, more selective and efficacious cytosolic phospholipase A2α (cPLA2α) inhibitor available, we revisited the role of cPLA2α activity in platelet activation and discovered that a component of platelet signaling, even larger than previously appreciated, relies on this enzyme. In a whole blood shear-based flow chamber assay, giripladib, a cPLA2α inhibitor, reduced platelet adhesion and accumulation on collagen. Moreover, giripladib differentially affected P-selectin expression and GPIIbIIIa activation depending on the agonist employed. While protease-activated receptor 1 (PAR1)-mediated platelet activation was unaffected by giripladib, the levels of PAR4- and GPVI-mediated platelet activation were significantly reduced. Meanwhile, the thromboxane A2 receptor antagonist SQ29548 had no effect on PAR-, GPVI-, or puriniergic receptor-mediated platelet activation, suggesting that another eicosanoid produced downstream of arachidonic acid liberation by cPLA2α was responsible for this large component of PAR4- and GPVI-mediated platelet activation.
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