2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. 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.

GRI918013

GRI918013 Chemical Structure

CAS No. : 313685-55-1

Size Price Stock Quantity
5 mg Get quote 2 - 3 weeks 1 - 2 Weeks 3 - 4 weeks 2 - 3 weeks
10 mg Get quote 2 - 3 weeks 1 - 2 Weeks 3 - 4 weeks 2 - 3 weeks
25 mg Get quote 2 - 3 weeks 1 - 2 Weeks 3 - 4 weeks 2 - 3 weeks
50 mg Get quote 2 - 3 weeks 1 - 2 Weeks 3 - 4 weeks 2 - 3 weeks
100 mg Get quote 2 - 3 weeks 1 - 2 Weeks 3 - 4 weeks 2 - 3 weeks
200 mg   Get quote  
500 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

GRI918013 Related Antibodies

Top Publications Citing Use of Products

View All Phosphodiesterase (PDE) Isoform Specific Products:

View All Isoforms
PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

IC50 & Target

Autotaxin

 

In Vitro

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.

GRI918013 Related Antibodies

Cell Invasion Assay[1]

Cell Line: A2058 human melanoma cells
Concentration: 0.01, 0.1, 1, 10 μM
Incubation Time: 16 hours
Result: Dose-dependently inhibited ATX-dependent A2058 cell invasion with an IC50 of 118.79 nM.
In Vivo

GRI918013 (30 µg/mouse; i.p.; daily; 10 days) reduces lung metastasis in female C57BL/6 mice with B16-F10 melanoma[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice (female, 8–12 weeks old)[1]
Dosage: 30 µg/mouse
Administration: i.p.; daily; 10 days
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.
Molecular Weight

433.28

Formula

C17H15Cl2FN2O4S
CAS No.
SMILES

O=C(NC=1C=CC=C(F)C1)C=2C=C(C(Cl)=CC2Cl)S(=O)(=O)N3CCOCC3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

GRI918013 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GRI918013313685-55-1GRI 918013GRI-918013Phosphodiesterase (PDE)A2058 cellATXmicefemale C57BL/6 miceLPA receptorsADMAN-LPC hydrolysisB16-F10 melanomaY83A mutantNPP6sphingosine 1-phosphate receptorsFS-3 hydrolysisF275A ATX mutantcancer cellsNPP7melanomaAutotaxinInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
GRI918013
Cat. No.:
HY-119601
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.