1. GPCR/G Protein
    Apoptosis
  2. LPL Receptor
    Caspase
  3. GRI977143

GRI977143 

Cat. No.: HY-100676
Handling Instructions

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

For research use only. We do not sell to patients.

GRI977143 Chemical Structure

GRI977143 Chemical Structure

CAS No. : 325850-81-5

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Description

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

IC50 & Target[1].

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.
Molecular Weight

391.44

Formula

C₂₂H₁₇NO₄S

CAS No.

325850-81-5

SMILES

O=C(O)C1=CC=CC=C1SCCCN(C(C2=CC=CC3=CC=CC4=C23)=O)C4=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

GRI977143GRI 977143GRI-977143LPL ReceptorCaspaseLysophospholipid ReceptorInhibitorinhibitorinhibit

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