2. Anti-infection Apoptosis NF-κB Metabolic Enzyme/Protease
  3. Flavivirus TNF Receptor NF-κB Apoptosis Ser/Thr Protease
  4. Nafamostat

Nafamostat, an anticoagulant, is a synthetic serine protease inhibitor. Nafamostat has anticancer and antivirus effect. Nafamostat induce apoptosis by up-regulating the expression of tumor necrosis factor receptor-1 (TNFR1). Nafamostat can be used in the development of the pathological thickening of the arterial wall.

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Nafamostat Chemical Structure

Nafamostat Chemical Structure

CAS No. : 81525-10-2

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Nafamostat Related Antibodies

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Nafamostat, an anticoagulant, is a synthetic serine protease inhibitor. Nafamostat has anticancer and antivirus effect. Nafamostat induce apoptosis by up-regulating the expression of tumor necrosis factor receptor-1 (TNFR1). Nafamostat can be used in the development of the pathological thickening of the arterial wall[1][2][3][4].

IC50 & Target

I-kappaBalpha

 

Cellular Effect
Cell Line Type Value Description References
MDA-MB-231 EC50
0.49 μM
Compound: nafamostat
Inhibition of HGFA in human MDA-MB-231 cells assessed as inhibition of c-MET phosphorylation after 15 mins by immunoblotting
Inhibition of HGFA in human MDA-MB-231 cells assessed as inhibition of c-MET phosphorylation after 15 mins by immunoblotting
[PMID: 25408834]
Sf9 IC50
0.15 μM
Compound: Nafamostat
Inhibition of recombinant N-terminal His-tagged HGFA (unknown origin) expressed in baculovirus-infected Sf9 cells incubated for 30 mins prior to cromogenic substrate addition by spectrophotometry
Inhibition of recombinant N-terminal His-tagged HGFA (unknown origin) expressed in baculovirus-infected Sf9 cells incubated for 30 mins prior to cromogenic substrate addition by spectrophotometry
[PMID: 25882520]
Vero C1008 CC50
> 100 μM
Compound: 49
Cytotoxicity against African green monkey Vero E6 cells by the CCK8 assay
Cytotoxicity against African green monkey Vero E6 cells by the CCK8 assay
[PMID: 32845145]
In Vitro

Nafamostat (10-80 μg/mL, 3-48 h) inhibits NF-κB activity by blocking IκBα phosphorylation in MDAPanc-28 cells[1].
Nafamostat (80 μg/mL, 24-48 h) induces apoptosis by up-regulating the expression of tumor necrosis factor receptor-1 (TNFR1) in MDAPanc-28 cells[1].
Nafamostat (0.1-10 μM, 24 h) has suppressive effect on invasiveness in Panc-1 cells[2].

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

Nafamostat Related Antibodies

Cell Viability Assay[1]

Cell Line: MDAPanc-28 cells
Concentration: 80 μg/mL
Incubation Time: 24 h, 48 h
Result: Substantially reduced the cell viability of MDAPanc-28 cells at both 24 hours and 48 hours.

Cell Invasion Assay[2]

Cell Line: Panc-1 cells
Concentration: 0.1 μM, 1 μM, 10 μM
Incubation Time: 24 h
Result: Observed significant inhibition in Panc-1-Try clones at concentrations as low as 0.1 mM.

Western Blot Analysis[1]

Cell Line: MDAPanc-28 cells
Concentration: 10 μg/mL, 20 μg/mL ,40 μg/mL, 80 μg/mL
Incubation Time: 3 h, 8 h, 24 h, 48 h
Result: Inhibited NF-κB DNA-binding activity and the degradation of IκBα in a dose-dependent manner as well as in a time-dependent manner.
Inhibited phosphorylation of IκBα in a time-dependent manner.
In Vivo

Nafamostat (10 mg/kg, Intraperitoneal injection, once a day for 18 days) exhibits favourable antiviral effects against Zika virus (ZIKV) infection in A129 mice[3].
Nafamostat (0.5-2.0 mg/mL (dissolved in saline), Intraperitoneal injection, once a day for 7 consecutive days) has inhibitory effect on neointimal formation after balloon injury of the rat carotid wall[4].

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

Animal Model: A129 mice[3]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Exhibit delayed lethality and improved survival (40%).
Animal Model: Balloon injury of the rat carotid wall[4]
Dosage: 0.5 mg/mL, 1 mg/mL, 2 mg/mL (dissolved in saline)
Administration: Intraperitoneal injection (i.p.)
Result: Showed smaller ratios of the neointima/medial area.
Showed positive but reduced immunoreactivity of the cells in the neointimal.
Clinical Trial
Molecular Weight

347.37

Formula

C19H17N5O2
CAS No.
SMILES

O=C(OC1=CC=C2C=C(C(N)=N)C=CC2=C1)C3=CC=C(NC(N)=N)C=C3
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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Nafamostat 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:

Nafamostat81525-10-2FlavivirusTNF ReceptorNF-κBApoptosisSer/Thr ProteaseTumor Necrosis Factor ReceptorTNFRNuclear factor-κBNuclear factor-kappaBSerine proteasesSerine endopeptidasesThreonine proteasesMDAPanc-28 cellsPanc-1 cellsA129 miceBalloon injury of the rat carotid wallInhibitorinhibitorinhibit

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