PB2-IN-4
PB2-IN-4 is a potent and orally effective PB2 inhibitor with an IC50 of 82 nM. PB2-IN-4 inhibits viral RNA polymerase activity and gene expression by binding to the PB2 protein, and alleviates the host inflammatory response. PB2-IN-4 can be used for research on influenza A virus.
For research use only. We do not sell to patients.
- CAS No.: 3123220-86-7
- Formula: C22H22FN9O
- Molecular Weight:447.47
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Storage:
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]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
Description
IC50 & Target
[1]|
PB2 82 nM (IC50) |
RNA Polymerase |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 786-0 | CC50 |
>50 μM
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Cytotoxicity against human 786-O cells assessed as reduction in cell viability incubated with the compound followed by CCK-8 solution for 2 hrs at 37 °C under 5% CO2 by CCK-8 assay.
Cytotoxicity against human 786-O cells assessed as reduction in cell viability incubated with the compound followed by CCK-8 solution for 2 hrs at 37 °C under 5% CO2 by CCK-8 assay.
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42720457 |
| A549 | CC50 |
>50 μM
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Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated with the compound followed by CCK-8 solution for 2 hrs at 37 °C under 5% CO2 by CCK-8 assay.
Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated with the compound followed by CCK-8 solution for 2 hrs at 37 °C under 5% CO2 by CCK-8 assay.
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42720457 |
| Hep 3B2 | CC50 |
44.3 μM
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Cytotoxicity against human Hep3B cells assessed as reduction in cell viability incubated with the compound followed by CCK-8 solution for 2 hrs at 37 °C under 5% CO2 by CCK-8 assay.
Cytotoxicity against human Hep3B cells assessed as reduction in cell viability incubated with the compound followed by CCK-8 solution for 2 hrs at 37 °C under 5% CO2 by CCK-8 assay.
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42720457 |
| MDCK | EC50 |
0.048 nM
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Anti-H1N1 cytopathic effect against MDCK cells infected with influenza A/WSN/1933 (H1N1) virus assessed by CCK-8 assay after 36-48 hrs incubation.
Anti-H1N1 cytopathic effect against MDCK cells infected with influenza A/WSN/1933 (H1N1) virus assessed by CCK-8 assay after 36-48 hrs incubation.
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42720457 |
In Vitro
PB2-IN-4 (compound 5B) (1.25-5.0 nM; 24 h) dose-dependently reduces viral NP protein fluorescence expression in H1N1-infected MDCK cells[1].
PB2-IN-4 (48 h) exhibits anti-H1N1 activity in MDCK cells, with an EC50 of 0.048 nM against A/WSN/1933 and a CC50 > 100 μM[1].
PB2-IN-4 (48 h) exhibits broad-spectrum antiviral activity against H1N1, H3N2, Oseltamivir (HY-13317)-resistant (NA-H274Y), and Baloxavir (HY-109025A)-resistant (PA-I38T) influenza strains, with EC50 values ranging from 0.035 to 0.373 nM[1].
PB2-IN-4 (0.5-2 nM; 48 h) significantly inhibits viral RNA-dependent RNA polymerase (RdRp) activity in 293T cells[1].
PB2-IN-4 (0.5-2 nM) inhibits proinflammatory cytokine and interferon expression in H1N1-stimulated A549 cells, and dose-dependently inhibits viral PB2 and NP mRNA expression in H1N1-infected MDCK cells[1].
PB2-IN-4 binds to the PB2 cap-binding domain with an IC50 of 0.082 μM[1].
PB2-IN-4 (48 h) exhibits extremely low cytotoxicity in MDCK, 786-O, A549, and Hep3B cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A/WSN/1933-infected MDCK cells
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Concentration:1.25, 2.5, 5.0 nM
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Incubation Time:24 h
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Result:Significantly decreased NP fluorescence in a dose-dependent manner.
Parmacokinetics
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC0-t | MRT0-t | F |
|---|---|---|---|---|---|---|---|---|
| Mice[1] | 30 mg/kg | p.o. | 1.41 h | 2.00 h | 3180 ng/mL | 11804 ng·h/mL | 3.23 h | 49.6 % |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (six-week-old, evenly distributed by sex)[1]
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Dosage:3 mg/kg, 10 mg/kg, 30 mg/kg
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Administration:p.o.; twice daily; 4 consecutive days
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Result:Achieved a survival rate of 85.7% in all treated groups.
Reduced lung index and pulmonary viral load in a dose-dependent manner.
Markedly suppressed mRNA levels of PB2 and NP in lung tissues.
Significantly attenuated virus-induced elevation of IL-6, IL-10, TNF-α, IP-10, and IFN-β at 30 and 10 mg/kg.
Revealed dose-dependent alleviation of influenza-induced histopathological abnormalities.
Chemical Information
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CAS No. 3123220-86-7
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Molecular Weight 447.47
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Formula C22H22FN9O
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SMILES
N#CNC([C@H]1C2CCC(CC2)[C@@H]1NC3=C(C(C4CC4)=NC(C5=NNC6=C5C=NC=N6)=N3)F)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PB2-IN-4 Related Classifications
HY-189357 Related Classifications
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