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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- No. CAS: 33580-97-1
- Fòrmula: C13H8ClN3O6
- Peso molecular:337.67
-
Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
- Pureza y Documentación
- Referencias
-
Help & FAQs
Actividad biológica
|
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.
-
Cell Line:A549
-
Concentration:0.19, 0.38, 0.75, 1.5, 5 μM
-
Incubation Time:48 h postinfection
-
Result:Reduced ZIKV RNA copy number in a dose-dependent manner in ZIKV-infected A549 cells.
-
Cell Line:A549
-
Concentration:0.19, 0.56, 1.67, 5 μM
-
Incubation Time:48 h postinfection
-
Result:Reduced ZIKV viral E protein production in a dose-dependent manner, as shown by pan-flavivirus anti-E 4G2 antibody staining.
-
Cell Line:A549
-
Concentration:0.19, 0.38, 0.75 μM
-
Incubation Time:48 h postinfection
-
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.
-
Cell Line:iPSC-derived 3D mini-brain organoids
-
Concentration:1.5 μM
-
Incubation Time:5 dpi for PFU assay; 7 dpi for fluorescence imaging
-
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.
-
Animal Model:Four-week-old A129 mice inoculated with 1.7 × 105 PFU PRVABC59 ZIKV[1]
-
Dosage:20 mg/kg/day
-
Administration:Oral gavage (p.o.); once daily; for 3 days postinfection
-
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.
-
Animal Model:Adult female B6 mice [1]
-
Dosage:40 mg/kg/day
-
Administration:Oral gavage (p.o.); once daily; for 7 days
-
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
-
No. CAS 33580-97-1
-
Peso molecular 337.67
-
Fòrmula C13H8ClN3O6
-
SMILES
O=C(C1=CC=CC([N+]([O-])=O)=C1O)NC2=CC=C([N+]([O-])=O)C=C2Cl
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
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