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  • DC Chemicals Limited
  • China
  • Product Name: GRI 977143
  • Price: $700.0/100mg $1150.0/250mg $2200.0/500mg $220.0/10ml
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao


325850-81-5

325850-81-5 structure
325850-81-5 structure
  • Name: GRI 977143
  • Chemical Name: 2-[3-(1,3-dioxobenzo[de]isoquinolin-2-yl)propylsulfanyl]benzoic acid
  • CAS Number: 325850-81-5
  • Molecular Formula: C22H17NO4S
  • Molecular Weight: 391.44000
  • Catalog: Signaling Pathways Apoptosis Caspase
  • Create Date: 2019-01-01 17:14:42
  • Modify Date: 2024-01-10 19:19:51
  • GRI977143 is a specific LPA2 receptor agonist, with an EC50 of 3.3 μM [1].

Name 2-[3-(1,3-dioxobenzo[de]isoquinolin-2-yl)propylsulfanyl]benzoic acid
Synonyms f0223-0003
unii-m3l07r4zep
GRI 977143
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.

Molecular Formula C22H17NO4S
Molecular Weight 391.44000
Exact Mass 391.08800
PSA 101.67000
LogP 3.83330
Symbol GHS07 GHS09
GHS07, GHS09
Signal Word Warning
Hazard Statements H302-H410
Precautionary Statements P273-P501
RIDADR UN 3077 9 / PGIII
HS Code 2933990090
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%