JMX0207
JMX0207 is an orally active flavivirus NS2B-NS3 protease inhibitor. JMX0207 showed an IC50-SLC of 1.3 μM for blocking NS2B-NS3 protein interaction and an IC50-pro of 8.2 μM for inhibiting protease catalytic activity.. JMX0207 directly binds viral NS3 protease at the NS2B-NS3 interface with a Kd of 1.1 μM, blocks viral polyprotein precursor processing, suppresses viral RNA replication and viral protein production. JMX0207 can be used for the study of Zika virus infection and Dengue virus infection.
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- CAS No.: 33580-97-1
- Formule: C13H8ClN3O6
- Masse moléculaire:337.67
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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DENV2 NS3 protease 1.1 μM (Kd) |
JMX0207 inhibits the molecular interaction between viral NS3 and its cofactor NS2B in the split luciferase complementation assay, with an IC50-SLC of 1.3 μM[1].
JMX0207 inhibits DENV2 NS2B-NS3 activity with an IC50-pro of 8.2 μM[1].
JMX0207 directly binds viral NS3 protease with a Kd of 1.1 μM in the SPR assay, and protein thermal shift assay shows that JMX0207 binding stabilizes viral NS3 protease with a 0.75 ℃ increase in Tm[1].
JMX0207 (0.01-10 μM; 48 h) inhibits DENV2 infectivity in A549 cells with an EC50-DN2 of 0.31 μM, and shows a CC50 of 31.9 μM[1].
JMX0207 (0.19-5 μM) reduces ZIKV RNA copy number and viral E antigen production in ZIKV-infected A549 cells in a dose-dependent manner, with an EC50-ZK of 0.30 μM[1].
JMX0207 (0.03-7.5 μM) reduces ZIKV viral protein expression and viral RNA synthesis in human neural progenitor cells (HNPCs) in a dose-dependent manner[1].
JMX0207 (1.5 μM) protects iPSC-derived 3D mini-brain organoids from ZIKV infection and reduces ZIKV production[1].
JMX0207 (0.75 μM; 0-24 h) remains effective when added up to 24 h postinfection, indicating that JMX0207 inhibits viral replication rather than viral entry[1].
JMX0207 inhibits DENV2 replication in a DENV2 replicon cell line with an EC50-DN2 of 1.1 μM[1].
JMX0207 (0.19-0.75 μM; 48 h postinfection) reduces ZIKV NS3 protein production and increases high-molecular-weight unprocessed viral polyprotein precursor in ZIKV-infected A549 cells in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549
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Concentration:0.19, 0.38, 0.75, 1.5, 5 μM
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Incubation Time:48 h postinfection
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Result:Reduced ZIKV RNA copy number in a dose-dependent manner in ZIKV-infected A549 cells.
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Cell Line:A549
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Concentration:0.19, 0.56, 1.67, 5 μM
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Incubation Time:48 h postinfection
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Result:Reduced ZIKV viral E protein production in a dose-dependent manner, as shown by pan-flavivirus anti-E 4G2 antibody staining.
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Cell Line:A549
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Concentration:0.19, 0.38, 0.75 μM
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Incubation Time:48 h postinfection
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Result:Reduced ZIKV NS3 protein production in a dose-dependent manner.
Increased accumulation of high-molecular-weight unprocessed viral polyprotein precursor recognized by anti-ZIKV NS3 antibody.
Supported inhibition of viral protease function and viral polyprotein precursor processing.
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Cell Line:iPSC-derived 3D mini-brain organoids
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Concentration:1.5 μM
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Incubation Time:5 dpi for PFU assay; 7 dpi for fluorescence imaging
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Result:Showed no obvious toxic effect on 3D organoids and maintained organoid morphology.
Nearly completely protected 3D mini-brain organoids from ZIKV infection.
Reduced ZIKV antigen production across organoid layers and significantly decreased ZIKV production from the organoids.
| Species | Dose | Route | Tmax | Cmax | T1/2 | AUC0-∞ |
|---|---|---|---|---|---|---|
| Mice[1] | 40 mg/kg | p.o. | 1.2 h | 145 μM | 11 h | 2719 μM/L·h |
JMX0207 (40 mg/kg/day; p.o.; once daily; for 7 days) shows no signs of toxicity in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Four-week-old A129 mice inoculated with 1.7 × 105 PFU PRVABC59 ZIKV[1]
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Dosage:20 mg/kg/day
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Administration:Oral gavage (p.o.); once daily; for 3 days postinfection
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Result:Significantly reduced ZIKV-induced viremia compared with vehicle control.
Viremia was measured by plaque forming unit (PFU) assay on day 3 postinfection.
Showed in vivo antiviral activity against ZIKV after oral administration.
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Animal Model:Adult female B6 mice [1]
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Dosage:40 mg/kg/day
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Administration:Oral gavage (p.o.); once daily; for 7 days
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Result:Displayed no sign of toxicity during repeated oral dosing.
Supported low toxicity and acceptable in vivo tolerability at 40 mg/kg/day.
Chemical Information
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CAS No. 33580-97-1
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Masse moléculaire 337.67
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Formule C13H8ClN3O6
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SMILES
O=C(C1=CC=CC([N+]([O-])=O)=C1O)NC2=CC=C([N+]([O-])=O)C=C2Cl
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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.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
JMX0207 Related Classifications
HY-184048 Related Classifications
Powered by Bioz
- JMX0207
- 33580-97-1
- JMX 0207
- JMX-0207
- Flavivirus
- Virus Protease
- Dengue Virus
- Zika virus
- Dengue virus
- DENV2
- ZIKV
- viral NS3 protease
- NS2B-NS3 interaction
- viral polyprotein precursor processing
- A549
- HNPC
- human neural progenitor cells
- iPSC-derived 3D mini-brain organoids
- DENV2 replicon cell line
- viral RNA
- viral E protein
- viral NS3 protein
- A129 ZIKV mouse model
- PRVABC59
- viremia
- oral gavage
- improved pharmacokinetics
- Inhibitor
- inhibitor
- inhibit