2. Cytoskeleton Metabolic Enzyme/Protease Immunology/Inflammation Protein Tyrosine Kinase/RTK
  3. Exosomes MAGL Interleukin Related VEGFR
  4. AM9928

AM9928 is a monoacylglycerol lipase (MAGL) inhibitor with IC50 and Ki values of 8.9 nM and 7.3 nM, respectively. AM9928 blocks the adhesion and migration of triple-negative breast cancer (TNBC) cells, and inhibits the secretion of IL-6, IL-8 and VEGF-A by TNBC cells. AM9928 suppresses the activation of human brain microvascular endothelial cells (HBMECs) induced by TNBC-derived exosomes, and reduces the secretion of IL-8 and VEGF-A by HBMECs. AM9928 attenuates changes in blood-brain barrier permeability, inhibits tumor growth in the mammary fat pad, and reduces brain colonization of TNBC. AM9928 can be used in studies related to triple-negative breast cancer.

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AM9928

AM9928 Chemical Structure

CAS No. : 1869033-49-7

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AM9928 Related Antibodies

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Description

AM9928 is a monoacylglycerol lipase (MAGL) inhibitor with IC50 and Ki values of 8.9 nM and 7.3 nM, respectively. AM9928 blocks the adhesion and migration of triple-negative breast cancer (TNBC) cells, and inhibits the secretion of IL-6, IL-8 and VEGF-A by TNBC cells. AM9928 suppresses the activation of human brain microvascular endothelial cells (HBMECs) induced by TNBC-derived exosomes, and reduces the secretion of IL-8 and VEGF-A by HBMECs. AM9928 attenuates changes in blood-brain barrier permeability, inhibits tumor growth in the mammary fat pad, and reduces brain colonization of TNBC. AM9928 can be used in studies related to triple-negative breast cancer[1][2][3].

IC50 & Target[1]

IL-6

 

IL-8

 

In Vitro

AM9928 (100 ng/mL; 10-30 min) blocks adhesion of MDA-MB-BrM2 TNBC cells to HBMEC monolayers at 10 and 30 minutes[1].
AM9928 (100 ng/mL; 5 h) significantly inhibits transmigration of MDA-MB-231 and MDA-MB-BrM2 TNBC cells across HBMEC monolayers[1].
AM9928 (250 nM; 72 h) significantly inhibits secretion of IL-6, IL-8, and VEGF-A from MDA-MB-231 and MDA-MB-BrM2 TNBC cells[1].
AM9928 (250 nM; 24 h) alters MDA-MB-231 and MDA-MB-BrM2 TNBC cells to produce exosomes that significantly inhibit IL-8 and VEGF-A secretion from activated HBMECs[1].
AM9928 (range of concentrations; 15 min pre-incubation, 4 hr reaction) inhibits truncated rat fatty acid amide hydrolase (ΔTM rFAAH) with IC50 values of 23 nM and 27 nM[3].

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

AM9928 Related Antibodies

Cell Migration Assay [1]

Cell Line: MDA-MB-231, MDA-MB-BrM2 (human TNBC cell lines)
Concentration: 100 ng/mL
Incubation Time: 5 h
Result: Significantly inhibited transmigration of MDA-MB-231 and MDA-MB-BrM2 TNBC cells across HBMEC monolayers by approximately 50%.

ELISA Assay[1]

Cell Line: MDA-MB-231, MDA-MB-BrM2 (human TNBC cell lines)
Concentration: 250 nM
Incubation Time: 72 h
Result: Reduced IL-6, IL-8 and VEGF-A secretion.

ELISA Assay[1]

Cell Line: MDA-MB-231, MDA-MB-BrM2 (human TNBC cell lines), human brain microvascular endothelial cells (HBMECs)
Concentration: 250 nM (TNBC cell treatment)
Incubation Time: 24 h (TNBC cell treatment); 6 h (exosome-HBMEC incubation)
Result: Reduced HBMEC IL-8 and VEGF-A secretion.
In Vivo

AM9928 (10 mg/kg; i.v.; twice weekly; 3 weeks) significantly reduces triple negative breast cancer tumor growth in mammary fat pads, lowers BBB permeability, and decreases brain metastasis colonization in BALB/c mice[1].

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

Animal Model: BALB/c (female, 6 weeks old, triple negative breast cancer model via GFP-4T1-BrM5 mammary tumor cell injection into mammary fat pads)[1]
Dosage: 10 mg/kg
Administration: i.v.; twice weekly; 3 weeks
Result: Significantly reduced mammary fat pad tumor growth compared to vehicle controls.
Significantly lowered average sum of GFP intensity (measure of brain tumor colonization) compared to vehicle controls.
Significantly decreased BBB permeability (measured by Evans blue dye content in brain tissue) compared to tumor-bearing vehicle controls.
Increased average sum of intensity for ZO-1 tight junction protein expression to 610,920 (vs. 582,096 in vehicle controls).
Increased average sum of intensity for Claudin-5 expression to 681,457 (vs. 518,599 in vehicle controls).
Reduced the number of mice with mammary tumors and brain tumors compared to vehicle controls.
Increased the number of mice alive at day 28 compared to vehicle controls.
Molecular Weight

396.44

Formula

C24H20N4O2
CAS No.
SMILES

N#CC1=CC(OC(N2CCN(C3C4=C(C5=C3C=CC=C5)C=CC=C4)CC2)=O)=NC=C1
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
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AM9928 Related Classifications

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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:

AM99281869033-49-7AM 9928AM-9928ExosomesMAGLInterleukin RelatedVEGFRMonoacylglycerol lipaseILVascular endothelial growth factor receptortriple negative breast cancermonoacylglycerol lipaseMDA-MB-BrM2IL-6TNBCHBMECsIL-8VEGF-Ahuman MAGLMDA-MB-231Inhibitorinhibitorinhibit

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