2. Anti-infection
  3. SARS-CoV
  4. SARS-CoV-2 nsp14-IN-10

SARS-CoV-2 nsp14-IN-10 is a highly potent and selective NSP14 (IC50 = 0.34 µM) S-adenosylmethionine (SAM) binding pocket inhibitor. SARS-CoV-2 nsp14-IN-10 demonstrates robust antiviral activity against SARS-CoV-2. SARS-CoV-2 nsp14-IN-10 exhibits broad-spectrum activity against other betacoronaviruses and inhibits SARS-CoV-2 at the replication stage. SARS-CoV-2 nsp14-IN-10 suppresses viral translation and exhibits immunostimulatory effects. SARS-CoV-2 nsp14-IN-10 specifically reverses NSP14-mediated alterations inhost transcriptome. SARS-CoV-2 nsp14-IN-10 can be used for the study of SARS-CoV-2.

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SARS-CoV-2 nsp14-IN-10

SARS-CoV-2 nsp14-IN-10 Chemical Structure

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SARS-CoV-2 nsp14-IN-10 Related Antibodies

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Description

SARS-CoV-2 nsp14-IN-10 is a highly potent and selective NSP14 (IC50 = 0.34 µM) S-adenosylmethionine (SAM) binding pocket inhibitor. SARS-CoV-2 nsp14-IN-10 demonstrates robust antiviral activity against SARS-CoV-2. SARS-CoV-2 nsp14-IN-10 exhibits broad-spectrum activity against other betacoronaviruses and inhibits SARS-CoV-2 at the replication stage. SARS-CoV-2 nsp14-IN-10 suppresses viral translation and exhibits immunostimulatory effects. SARS-CoV-2 nsp14-IN-10 specifically reverses NSP14-mediated alterations inhost transcriptome. SARS-CoV-2 nsp14-IN-10 can be used for the study of SARS-CoV-2[1].

In Vitro

SARS-CoV-2 nsp14-IN-10 (Compound C10) (20-500 µM) specifically binds to the SAM recognition pocket of NSP14 (KD = 187 nM) in a competitive manner with SAM[1].
SARS-CoV-2 nsp14-IN-10 (5-25 μM, 8 h) enhances the thermostability of NSP14 protein in HEK293-NSP14 cells, indicating that it binds to the target in living cells[1].
SARS-CoV-2 nsp14-IN-10 (24 h) significantly reduces the infection rates of the original SARS-CoV-2 strain, Delta, and Omicron variants in A549-ACE2 cells (EC50 values of 0.31 μM, 0.50 μM and 0.06 μM, respectively)[1].
SARS-CoV-2 nsp14-IN-10 (10 µM, 24 h) potently inhibits the replication phase of SARS-CoV-2 in HeLa cells[1].
SARS-CoV-2 nsp14-IN-10 (3-20 μM, 0-24 h) shows strong inhibitory activity in A549-ACE2 cells infected with SARS-CoV-2 trVLP during both full-time and post-entry treatments, while entry treatment shows no significant inhibition[1].
SARS-CoV-2 nsp14-IN-10 (20-40 μM, 8 h) inhibits the translation initiation of SARS-CoV-2 mRNA in A549-ACE2 cells infected with trVLP, specifically by cap maturation, selectively impairing[1].
SARS-CoV-2 nsp14-IN-10 (20-40 µM, 8 h) selectively inhibits viral translation in A549-ACE2 cells infected with SARS-CoV-2 trVLP[1].
SARS-CoV-2 nsp14-IN-10 (20 μM, 24 h) significantly reduced the expression levels of Spike mRNA and protein in A549-ACE2 cells infected with SARS-CoV-2 trVLP[1].
SARS-CoV-2 nsp14-IN-10 (20 μM, 24 h) upregulates the expression of interferon-stimulated genes (ISGs) such as RSAD2, IFI6, and IRF7 in A549-ACE2 cells[1].
SARS-CoV-2 nsp14-IN-10 (5-20 μM, 48 h) reverses host transcriptome changes induced by NSP14 expression in HEK293-NSP14 cells[1].

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

SARS-CoV-2 nsp14-IN-10 Related Antibodies

Western Blot Analysis[1]

Cell Line: HEK293-NSP14 cells
Concentration: 5 μM, 10 μM, 15 μM, 20 μM, 25 μM
Incubation Time: 8 h
Result: Enhanced the thermal stability of NSP14 protein.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-t
Mice[1] 50 mg/kg i.p. 2.96 h 0.5 h 8463.59 ng/mL 9999.12 ng·h/mL
Mice[1] 70 mg/kg i.p. 1.71 h 1 h 19450.11 ng/mL 37779.33 ng·h/mL
Mice[1] 70 mg/kg p.o. 0.36 h 0.25 h 2345.9 ng/mL 999.02 ng·h/mL
In Vivo

SARS-CoV-2 nsp14-IN-10 (Compound C10) (60-180 mg/kg, i.p., twice daily for 3 days) effectively reduces SARS-CoV-2 replication and pathological damage in the lungs of K18-hACE2 transgenic mice infected with SARS-CoV-2, with a broad safety margin[1].

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

Animal Model: The six- to eight-week-old male K18-hACE2 transgenic mice (18-20 g) were inoculated intranasally with 5 × 103 focus-forming units of SARS-CoV-2 nCoV-SH01 strain[1].
Dosage: 60 mg/kg, 120 mg/kg, 180 mg/kg
Administration: I.p., twice daily for 3 days
Result: 120 mg/kg significantly reduced pulmonary viral titer.
60 mg/kg showed a decreasing trend, but the effect was not statistically significant.
Reduced alveolar wall thickening, congestion, and inflammatory infiltration.
The positive signal of the SARS-CoV-2 nucleocapsid protein was significantly reduced.
Molecular Weight

545.54

Formula

C24H22F3N7O3S
SMILES

O=C(NC1CCN(C2=C3N=CNC3=NC=N2)CC1)C4=CC=CC(NS(=O)(C5=CC=C(C(F)(F)F)C=C5)=O)=C4
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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SARS-CoV-2 nsp14-IN-10 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:

SARS-CoV-2 nsp14-IN-10SARS-CoVSARS coronavirusSARS-CoV-2NSP14N7-methyltransferaseAntiviral inhibitorViral mRNA cappingRNA virus replicationInhibitorinhibitorinhibit

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