GRI 977143

LPA2 receptor non-lipid agonist CAS# 325850-81-5

GRI 977143

Catalog No. BCC2401----Order now to get a substantial discount!

Product Name & Size Price Stock
GRI 977143: 5mg $115 In Stock
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Chemical structure

GRI 977143

3D structure

Chemical Properties of GRI 977143

Cas No. 325850-81-5 SDF Download SDF
PubChem ID 3114900 Appearance Powder
Formula C22H17NO4S M.Wt 391.44
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in DMSO
Chemical Name 2-[3-(1,3-dioxobenzo[de]isoquinolin-2-yl)propylsulfanyl]benzoic acid
SMILES C1=CC=C(C(=C1)C(=O)O)SCCCN2C(=O)C3=CC=CC4=C3C(=CC=C4)C2=O
Standard InChIKey GMVZUCHUOYUMLL-UHFFFAOYSA-N
Standard InChI InChI=1S/C22H17NO4S/c24-20-16-9-3-6-14-7-4-10-17(19(14)16)21(25)23(20)12-5-13-28-18-11-2-1-8-15(18)22(26)27/h1-4,6-11H,5,12-13H2,(H,26,27)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of GRI 977143

DescriptionSelective lysophosphatidic acid 2 (LPA2) receptor non-lipid agonist (EC50 = 3.3 μM). Does not activate other LPA GPCRs at concentrations up to 10 μM. Antiapoptotic; inhibits activation of caspases 3, 7, 8 and 9, Bax translocation and PARP-1 cleavage. Activates ERK1/2 survival pathway.

GRI 977143 Dilution Calculator

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GRI 977143 Molarity Calculator

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Preparing Stock Solutions of GRI 977143

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.5547 mL 12.7733 mL 25.5467 mL 51.0934 mL 63.8667 mL
5 mM 0.5109 mL 2.5547 mL 5.1093 mL 10.2187 mL 12.7733 mL
10 mM 0.2555 mL 1.2773 mL 2.5547 mL 5.1093 mL 6.3867 mL
50 mM 0.0511 mL 0.2555 mL 0.5109 mL 1.0219 mL 1.2773 mL
100 mM 0.0255 mL 0.1277 mL 0.2555 mL 0.5109 mL 0.6387 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on GRI 977143

Selective lysophosphatidic acid 2 (LPA2) receptor non-lipid agonist (EC50 = 3.3 μM). Does not activate other LPA GPCRs at concentrations up to 10 μM. Antiapoptotic; inhibits activation of caspases 3, 7, 8 and 9, Bax translocation and PARP-1 cleavage. Activates ERK1/2 survival pathway.

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References on GRI 977143

Arabidopsis GRI is involved in the regulation of cell death induced by extracellular ROS.[Pubmed:19279211]

Proc Natl Acad Sci U S A. 2009 Mar 31;106(13):5412-7.

Reactive oxygen species (ROS) have important functions in plant stress responses and development. In plants, ozone and pathogen infection induce an extracellular oxidative burst that is involved in the regulation of cell death. However, very little is known about how plants can perceive ROS and regulate the initiation and the containment of cell death. We have identified an Arabidopsis thaliana protein, GRIM REAPER (GRI), that is involved in the regulation of cell death induced by extracellular ROS. Plants with an insertion in GRI display an ozone-sensitive phenotype. GRI is an Arabidopsis ortholog of the tobacco flower-specific Stig1 gene. The GRI protein appears to be processed in leaves with a release of an N-terminal fragment of the protein. Infiltration of the N-terminal fragment of the GRI protein into leaves caused cell death in a superoxide- and salicylic acid-dependent manner. Analysis of the extracellular GRI protein yields information on how plants can initiate ROS-induced cell death during stress response and development.

Improvement of methyl orange dye biotreatment by a novel isolated strain, Aeromonas veronii GRI, by SPB1 biosurfactant addition.[Pubmed:26396008]

Environ Sci Pollut Res Int. 2016 Jan;23(2):1742-54.

Aeromonas veronii GRI (KF964486), isolated from acclimated textile effluent after selective enrichment on azo dye, was assessed for methyl orange biodegradation potency. Results suggested the potential of this bacterium for use in effective treatment of azo-dye-contaminated wastewaters under static conditions at neutral and alkaline pH value, characteristic of typical textile effluents. The strain could tolerate higher doses of dyes as it was able to decolorize up to 1000 mg/l. When used as microbial surfactant to enhance methyl orange biodecolorization, Bacillus subtilis SPB1-derived lipopeptide accelerated the decolorization rate and maximized slightly the decolorization efficiency at an optimal concentration of about 0.025%. In order to enhance the process efficiency, a Taguchi design was conducted. Phytotoxicity bioassay using sesame and radish seeds were carried out to assess the biotreatment effectiveness. The bacterium was able to effectively decolorize the azo dye when inoculated with an initial optical density of about 0.5 with 0.25% sucrose, 0.125% yeast extract, 0.01% SPB1 biosurfactant, and when conducting an agitation phase of about 24 h after static incubation. Germination potency showed an increase toward the nonoptimized conditions indicating an improvement of the biotreatment. When comparing with synthetic surfactants, a drastic decrease and an inhibition of orange methyl decolorization were observed in the presence of CTAB and SDS. The nonionic surfactant Tween 80 had a positive effect on methyl orange biodecolorization. Also, studies ensured that methyl orange removal by this strain could be due to endocellular enzymatic activities. To conclude, the addition of SPB1 bioemulsifier reduced energy costs by reducing effective decolorization period, biosurfactant stimulated bacterial decolorization method may provide highly efficient, inexpensive, and time-saving procedure in treatment of textile effluents.

Mitigation of radiation injury by selective stimulation of the LPA(2) receptor.[Pubmed:23127512]

Biochim Biophys Acta. 2013 Jan;1831(1):117-25.

Due to its antiapoptotic action, derivatives of the lipid mediator lysophosphatidic acid (LPA) provide potential therapeutic utility in diseases associated with programmed cell death. Apoptosis is one of the major pathophysiological processes elicited by radiation injury to the organism. Consequently, therapeutic explorations applying compounds that mimic the antiapoptotic action of LPA have begun. Here we present a brief account of our decade-long drug discovery effort aimed at developing LPA mimics with a special focus on specific agonists of the LPA(2) receptor subtype, which was found to be highly effective in protecting cells from apoptosis. We describe new evidence that 2-((3-(1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl)propyl)thio)benzoic acid (GRI977143), a prototypic nonlipid agonist specific to the LPA(2) receptor subtype, rescues apoptotically condemned cells in vitro and in vivo from injury caused by high-dose gamma-irradiation. GRI977143 shows the features of a radiomitigator because it is effective in rescuing the lives of mice from deadly levels of radiation when administered 24h after radiation exposure. Our findings suggest that by specifically activating LPA(2) receptors GRI977143 activates the ERK1/2 prosurvival pathway, effectively reduces Bax translocation to the mitochondrion, attenuates the activation of initiator and effector caspases, reduces DNA fragmentation, and inhibits PARP-1 cleavage associated with gamma-irradiation-induced apoptosis. GRI977143 also inhibits bystander apoptosis elicited by soluble proapoptotic mediators produced by irradiated cells. Thus, GRI977143 can serve as a prototype scaffold for lead optimization paving the way to more potent analogs amenable for therapeutic exploration. This article is part of a Special Issue entitled Advances in Lysophospholipid Research.

Virtual screening for LPA2-specific agonists identifies a nonlipid compound with antiapoptotic actions.[Pubmed:22968304]

Mol Pharmacol. 2012 Dec;82(6):1162-73.

Lysophosphatidic acid (LPA) is a highly potent endogenous lipid mediator that protects and rescues cells from programmed cell death. Earlier work identified the LPA(2) G protein-coupled receptor subtype as an important molecular target of LPA mediating antiapoptotic signaling. Here we describe the results of a virtual screen using single-reference similarity searching that yielded compounds 2-((9-oxo-9H-fluoren-2-yl)carbamoyl)benzoic acid (NSC12404), 2-((3-(1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl)propyl)thio)benzoic acid (GRI977143), 4,5-dichloro-2-((9-oxo-9H-fluoren-2-yl)carbamoyl)benzoic acid (H2L5547924), and 2-((9,10-dioxo-9,10-dihydroanthracen-2-yl)carbamoyl) benzoic acid (H2L5828102), novel nonlipid and drug-like compounds that are specific for the LPA(2) receptor subtype. We characterized the antiapoptotic action of one of these compounds, GRI977143, which was effective in reducing activation of caspases 3, 7, 8, and 9 and inhibited poly(ADP-ribose)polymerase 1 cleavage and DNA fragmentation in different extrinsic and intrinsic models of apoptosis in vitro. Furthermore, GRI977143 promoted carcinoma cell invasion of human umbilical vein endothelial cell monolayers and fibroblast proliferation. The antiapoptotic cellular signaling responses were present selectively in mouse embryonic fibroblast cells derived from LPA(1&2) double-knockout mice reconstituted with the LPA(2) receptor and were absent in vector-transduced control cells. GRI977143 was an effective stimulator of extracellular signal-regulated kinase 1/2 activation and promoted the assembly of a macromolecular signaling complex consisting of LPA(2), Na(+) - H(+) exchange regulatory factor 2, and thyroid receptor interacting protein 6, which has been shown previously to be a required step in LPA-induced antiapoptotic signaling. The present findings indicate that nonlipid LPA(2)-specific agonists represent an excellent starting point for development of lead compounds with potential therapeutic utility for preventing the programmed cell death involved in many types of degenerative and inflammatory diseases.

Description

Selective LPA2 agonist; antiapoptotic

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