Nafamostat
Based on 19 publication(s) in Google Scholar
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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- CAS No.: 81525-10-2
- Formule: C19H17N5O2
- Masse moléculaire:347.37
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Publications Citing Use of MedChemExpress (MCE) Nafamostat
More- Cell Res. 2020 Mar;30(3):269-271. [Abstract]
- Nat Commun. 2024 Jun 27;15(1):5458. [Abstract]
- Exp Mol Med. 2024 Dec;56(12):2631-2641. [Abstract]
- Nat Chem Biol. 2022 Sep;18(9):963-971. [Abstract]
- Nucleic Acids Res. 2021 Jan 8;49(D1):D1113-D1121. [Abstract]
- Adv Healthc Mater. 2025 Aug 1:e02156. [Abstract]
- Cells. 2022 Jan 18;11(3):319. [Abstract]
- Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
- Eur J Pharmacol. 2023 Jan 5:938:175394. [Abstract]
- Eur J Pharmacol. 2022 Mar 15:919:174795. [Abstract]
- Biomolecules. 2022 Jul 31;12(8):1063. [Abstract]
- Sci Rep. 2026 May 16. [Abstract]
- Antiviral Res. 2023 Jun:214:105606. [Abstract]
- Viruses. 2022 Sep 12;14(9):2017. [Abstract]
- ChemMedChem. 2026 Mar 31;21(7):e202501099.
- bioRxiv. 2026 Jan 24.
- Res Sq. 2025 Apr 07.
- bioRxiv. 2024 October 09.
- Patent. US20230210807A1.
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Activité biologique
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I-kappaBalpha |
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Cell Line
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Type | Value | Description | References |
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| MDA-MB-231 | EC50 |
0.49 μM
Compound: nafamostat
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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
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[PMID: 25408834] |
| Sf9 | IC50 |
0.15 μM
Compound: Nafamostat
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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
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[PMID: 25882520] |
| Vero | CC50 |
>100 μM
Compound: Nafamostat
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Cytotoxicity against african green monkey Vero cells
Cytotoxicity against african green monkey Vero cells
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[PMID: 32563814] |
| Vero C1008 | CC50 |
>100 μM
Compound: 49
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Cytotoxicity against African green monkey Vero E6 cells by the CCK8 assay
Cytotoxicity against African green monkey Vero E6 cells by the CCK8 assay
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[PMID: 32845145] |
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.
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Cell Line:MDAPanc-28 cells
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Concentration:80 μg/mL
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Incubation Time:24 h, 48 h
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Result:Substantially reduced the cell viability of MDAPanc-28 cells at both 24 hours and 48 hours.
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Cell Line:Panc-1 cells
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Concentration:0.1 μM, 1 μM, 10 μM
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Incubation Time:24 h
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Result:Observed significant inhibition in Panc-1-Try clones at concentrations as low as 0.1 mM.
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Cell Line:MDAPanc-28 cells
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Concentration:10 μg/mL, 20 μg/mL ,40 μg/mL, 80 μg/mL
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Incubation Time:3 h, 8 h, 24 h, 48 h
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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.
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.
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Animal Model:A129 mice[3]
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Dosage:10 mg/kg
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Administration:Intraperitoneal injection (i.p.)
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Result:Exhibit delayed lethality and improved survival (40%).
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Animal Model:Balloon injury of the rat carotid wall[4]
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Dosage:0.5 mg/mL, 1 mg/mL, 2 mg/mL (dissolved in saline)
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Administration:Intraperitoneal injection (i.p.)
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Result:Showed smaller ratios of the neointima/medial area.
Showed positive but reduced immunoreactivity of the cells in the neointimal.
Chemical Information
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CAS No. 81525-10-2
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Masse moléculaire 347.37
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Formule C19H17N5O2
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SMILES
O=C(OC1=CC=C2C=C(C(N)=N)C=CC2=C1)C3=CC=C(NC(N)=N)C=C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (19)
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Journal Impact Factor
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Most Recent
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Cell Res
Remdesivir and chloroquine effectively inhibit the recently emerged novel coronavirus (2019-nCoV) in vitro. [Abstract]2020 Mar;30(3):269-271. PMID: 32020029 -
Nat Commun
Structural basis for potent neutralization of human respirovirus type 3 by protective single-domain camelid antibodies. [Abstract]2024 Jun 27;15(1):5458. PMID: 38937429 -
Exp Mol Med
Distribution and impact of p16INK4A+ senescent cells in elderly tissues: a focus on senescent immune cell and epithelial dysfunction. [Abstract]2024 Dec;56(12):2631-2641. PMID: 39617789 -
Nat Chem Biol
2022 Sep;18(9):963-971. PMID: 35676539 -
Nucleic Acids Res
COVID19 Drug Repository: text-mining the literature in search of putative COVID19 therapeutics. [Abstract]2021 Jan 8;49(D1):D1113-D1121. PMID: 33166390 -
Adv Healthc Mater
Self-Assembling Multi-Antigen T Cell Hybridizers for Precision Immunotherapy of Multiple Myeloma. [Abstract]2025 Aug 1:e02156. PMID: 40747784
Nafamostat purchased from MedChemExpress. Usage Cited in: Adv Healthc Mater. 2025 Aug 1:e02156. [Abstract]
Targeted inhibition of granzyme B with Z‐AAD‐CMK and granzyme A with Nafamostat mesylate (NFM) attenuates cell death.
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Cells
Assessment of FDA-Approved Drugs as a Therapeutic Approach for Niemann-Pick Disease Type C1 Using Patient-Specific iPSC-Based Model Systems. [Abstract]2022 Jan 18;11(3):319. PMID: 35159129 -
Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
Eur J Pharmacol
Mechanisms of acid-sensing ion channels inhibition by nafamostat, sepimostat and diminazene. [Abstract]2023 Jan 5:938:175394. PMID: 36403685
Nafamostat purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2023 Jan 5:938:175394. [Abstract]
Concentration-inhibition curves for Nafamostat mesylate, sepimostat and diminazene aceturate.
Nafamostat purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2023 Jan 5:938:175394. [Abstract]
Representative examples of current inhibition by 1 μM Nafamostat mesylate.
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Eur J Pharmacol
2022 Mar 15:919:174795. PMID: 35122868 -
Biomolecules
The Rabep1-Mediated Endocytosis and Activation of Trypsinogen to Promote Pancreatic Stellate Cell Activation. [Abstract]2022 Jul 31;12(8):1063. PMID: 36008957 -
Sci Rep
Production and characterization of gigastasin, a leech-derived inhibitor of complement and coagulation pathways. [Abstract]2026 May 16. PMID: 42143157 -
Antiviral Res
Omicsynin B4 potently blocks coronavirus infection by inhibiting host proteases cathepsin L and TMPRSS2. [Abstract]2023 Jun:214:105606. PMID: 37076089
Nafamostat purchased from MedChemExpress. Usage Cited in: Antiviral Res. 2023 Jun:214:105606. [Abstract]
Huh7.5 cells was infected with HCoV-229E (MOI = 3.5) and treated with omicsynin B4 (10 μM), E−64d (1 μM) or nafamostat mesylate (40 μM) at the indicated times. Immunofluorescence staining of the dsRNA (green) were merged with the nuclear Hoechst 33342 dye (blue) using a fluorescence microscopy (200 × ). Mock, the cell control. Veh, the vehicle control. Cpd, compound. NH4Cl, ammonium chloride. B4, omicsynin B4. NM, nafamostat mesylate. hpi, hour post infection.
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Viruses
Molecular Analyses of Clinical Isolates and Recombinant SARS-CoV-2 Carrying B.1 and B.1.617.2 Spike Mutations Suggest a Potential Role of Non-Spike Mutations in Infection Kinetics. [Abstract]2022 Sep 12;14(9):2017. PMID: 36146823
Nafamostat purchased from MedChemExpress. Usage Cited in: Viruses. 2022 Sep 12;14(9):2017. [Abstract]
Efficacy of small molecule inhibitors Remdesivir, Nafamostat mesylate, Nirmatrelvir, and Molnupiravir against B.1BAC-V (green), B.1.617.2BAC-V (orange), and corresponding clinical isolates (CI, grey).
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Pureté et documentation
Références
[1]. Uwagawa T, et al. Mechanisms of synthetic serine protease inhibitor (FUT‐175)‐mediated cell death [J]. Cancer: Interdisciplinary International Journal of the American Cancer Society, 2007, 109(10): 2142-2153. [Content Brief]
[2]. Tajima H, et al. Enhanced invasiveness of pancreatic adenocarcinoma cells stably transfected with cationic trypsinogen cDNA [J]. International journal of cancer, 2001, 94(5): 699-704. [Content Brief]
[3]. Yan Y, et al. Nafamostat mesylate as a broad-spectrum candidate for the treatment of flavivirus infections by targeting envelope proteins [J]. Antiviral research, 2022, 202: 105325. [Content Brief]
[4]. Sawada M, et al. Prevention of neointimal formation by a serine protease inhibitor, FUT-175, after carotid balloon injury in rats [J]. Stroke, 1999, 30(3): 644-650. [Content Brief]
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