GRI 977143
Modify Date: 2024-01-10 19:19:51
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 |
Signal Word | Warning | |
Use of GRI 977143GRI977143 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 |
|---|---|
| Synonym | More Synonyms |
| 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 |
| Molecular Formula | C22H17NO4S |
|---|---|
| Molecular Weight | 391.44000 |
| Exact Mass | 391.08800 |
| PSA | 101.67000 |
| LogP | 3.83330 |
| Symbol |
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% |
| f0223-0003 |
| unii-m3l07r4zep |
| GRI 977143 |