GRI 977143| CAS 325850-81-5|DC Chemicals

Cas No.:	325850-81-5
Chemical Name:	2-((3-(1,3-Dioxo-1H-benzo[de]isoquinolin-2(3H)-yl)propyl)thio)benzoic acid
Synonyms:	2-((3-(1,3-Dioxo-1H-benzo[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;2-[3-(1,3-Dioxo-1H,3H-benzo[de]isoquinolin-2-yl)-propylsulfanyl]-benzoic acid;2-[3-(1,3-dioxobenzo[de]isoquinolin-2-yl)propylsulfanyl]benzoic acid;GRI 977143;AC1MJMO4;CCG-21963;F0223-0003;GRI-977143;MolPort-000-691-587;STK806571;UNII-M3L07R4ZEP;2-[[3-(1,3-Dioxo-1H-benz[de]isoquinolin-2(3H)-yl)propyl]thio]-benzoic acid
SMILES:	O=C1C2C3C(=CC=CC=3C(=O)N1CCCSC1C=CC=CC=1C(O)=O)C=CC=2
Formula:	C₂₂H₁₇NO₄S
M.Wt:	391.43968
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	A potent, specific and nonlipid agonist of LPA2 receptor with EC50 of 3.3 uM, does not activate any of the other LPA GPCRs (>10 uM); also inhibits LPA3 with IC50 of 6.6 uM; reduces the activation of caspases 3, 7, 8 and 9 and inhibits PARP1 cleavage and DNA fragmentation in different extrinsic and intrinsic models of apoptosis in vitro; promotes carcinoma cell invasion of human umbilical vein endothelial cell monolayers and fibroblast proliferation.
Target:	LPA2 Receptor:3.3 μM (EC50)
In Vitro:	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[1]. 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[1]. Cell Proliferation Assay[1] Cell Line: Vector- and LPA2-transduced MEF cells (2 × 104)[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[1]. 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.
References:	[1]. Gyöngyi N. Kiss, et al. Virtual Screening for LPA2-Specific Agonists Identifies a Nonlipid Compound with Antiapoptotic Actions. Mol Pharmacol. 2012 Dec; 82(6): 1162–1173. [2]. Gyöngyi Nagyné Kiss, et al. PHARMACOLOGICAL AND CELLULAR CHARACTERIZATION OF GRI977143, A NOVEL NONLIPID LPA2 RECEPTOR AGONIST IDENTIFIED BY VIRTUAL SCREENING.

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