GRI 977143

Modify Date: 2025-08-25 18:39:57

GRI 977143 Structure
GRI 977143 structure
Common Name GRI 977143
CAS Number 325850-81-5 Molecular Weight 391.44000
Density N/A Boiling Point N/A
Molecular Formula C22H17NO4S Melting Point N/A
MSDS USA Flash Point N/A
Symbol GHS07 GHS09
GHS07, GHS09
Signal Word Warning

 Use of GRI 977143


GRI977143 is a specific LPA2 receptor agonist, with an EC50 of 3.3 μM [1].

 Names

Name 2-[3-(1,3-dioxobenzo[de]isoquinolin-2-yl)propylsulfanyl]benzoic acid
Synonym More Synonyms

 GRI 977143 Biological Activity

Description GRI977143 is a specific LPA2 receptor agonist, with an EC50 of 3.3 μM [1].
Related Catalog
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.

 Chemical & Physical Properties

Molecular Formula C22H17NO4S
Molecular Weight 391.44000
Exact Mass 391.08800
PSA 101.67000
LogP 3.83330

 Safety Information

Symbol GHS07 GHS09
GHS07, GHS09
Signal Word Warning
Hazard Statements H302-H410
Precautionary Statements P273-P501
RIDADR UN 3077 9 / PGIII
HS Code 2933990090

 Customs

HS Code 2933990090
Summary 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Synonyms

f0223-0003
unii-m3l07r4zep
GRI 977143
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