GRI918013
GRI918013 (compound 1) is a selective and competitive autotaxin (ATX/NPP2) inhibitor with anti-invasive and anti-metastatic activity. GRI918013 competitively binds to ATX, blocking lipid substrates such as lysophosphatidylcholine (LPC) from entering the ATX active site, thereby inhibiting ATX-mediated hydrolysis of LPC to lysophosphatidic acid (LPA), and consequently inhibiting ATX-LPA axis-related tumor cell invasion and metastasis. GRI918013 inhibits ATX-mediated hydrolysis of the LPL substrate FS-3 (IC50=31.42 nM, Ki=12.98 nM). GRI918013 can be used in research on cancer invasion and metastasis, such as melanoma, and can also serve as a tool compound for ATX-LPA axis-related diseases such as fibrotic diseases, neuropathic pain, and cholestatic pruritus.
For research use only. We do not sell to patients.
- CAS No.: 313685-55-1
- Formula: C17H15Cl2FN2O4S
- Molecular Weight:433.28
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Autotaxin |
GRI918013 (10 µM; 3 h) competitively inhibits ATX-mediated FS-3 hydrolysis (IC50=31.42 nM; Ki=12.98 nM), but does not inhibit the hydrolysis of the phosphodiesterase (PDE) substrate pNP-TMP, and has no effect on NPP6, NPP7, or LPA and S1P receptors[1].
GRI918013 (10 µM; 2 h) inhibits the hydrolysis of four substrates, LPC 14:0, LPC 16:0, LPC 18:0, and LPC 18:1, mediated by ATX, with inhibition rates of 41.0%, 55.4%, 43.6%, and 51.8%, respectively[1].
GRI918013 dose-dependently inhibits ATX-dependent A2058 cell invasion (IC50 = 118.79 nM, 16 h)[1].
GRI918013 has reduced inhibitory potency on ATXF275A mutant (IC50 >10 μM vs ATXWT 3.0 μM) and maintains potency on ATXY83A mutant (IC50=0.15 μM)[1].
GRI918013 (10 µM; 4 h) inhibits ATX-mediated ADMAN-LPC hydrolysis by 89.0%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A2058 human melanoma cells
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Concentration:0.01, 0.1, 1, 10 μM
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Incubation Time:16 hours
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Result:Dose-dependently inhibited ATX-dependent A2058 cell invasion with an IC50 of 118.79 nM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice (female, 8–12 weeks old)[1]
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Dosage:30 µg/mouse
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Administration:i.p.; daily; 10 days
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Result:Significantly reduced the number of lung metastatic nodules when administered 1 day before or 1 day after tumor cell inoculation compared to vehicle-treated controls.
Chemical Information
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CAS No. 313685-55-1
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Molecular Weight 433.28
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Formula C17H15Cl2FN2O4S
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SMILES
O=C(NC=1C=CC=C(F)C1)C=2C=C(C(Cl)=CC2Cl)S(=O)(=O)N3CCOCC3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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