1. Anti-infection
  2. HCV
  3. GSK5852

GSK5852 (GSK2485852) is an HCV NS5B polymerase inhibitor, with an IC50 value of 50 nM. GSK5852 displays antiviral activity and inhibits HCV with EC50s of 3.0 nM (genotype 1a, GT1a) and 1.7 nM (GT1b), respectively.

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GSK5852 Chemical Structure

GSK5852 Chemical Structure

CAS No. : 1331942-30-3

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Description

GSK5852 (GSK2485852) is an HCV NS5B polymerase inhibitor, with an IC50 value of 50 nM. GSK5852 displays antiviral activity and inhibits HCV with EC50s of 3.0 nM (genotype 1a, GT1a) and 1.7 nM (GT1b), respectively[1][2][3].

IC50 & Target

Target: 50 nM (NS5B, HCV)[1]

In Vitro

Nonstructural protein 5B (NS5B) RNA-dependent RNA polymerase (RdRp) is a component of HCV, for researching HCV infection-related diseases[1].
GSK5852 (compound 87) inhibits aggregation by two mechanisms: 1) stabilizing β-flap in a closed inactive state to inhibit the initiation step of the RdRp RNA replication cycle; 2) disruption of RNA processing channels through direct spatial contact[1].
GSK5852 is a non-nucleoside NS5B inhibitor and exhibits inhibitory effect on HCV mutant variants with EC50s of 3.2 nM (GT1a C316Y), 1.9 nM (GT1b C316N), respectively[1].
GSK5852 displays an excellent resistance profile and shows a <5-fold potency loss across the clinically important NS5B resistance mutations[2].
GSK5852 shows no cross-resistance against known resistance mutations in NS5B[2].
GSK5852 (compound 3) (0-10 μM) blocks the initiation step of NS5B polymerase cycle[3].
GSK5852 (0.6, 10 μM; 0-75 h) shows slow binding kinetics with isolated GT1b 316N protein, and with a dissociation half-life of >40 hours[3].
GSK5852 (0.6, 10 μM; 15 min) inhibits NS5B∆21 1b 316N with an IC50 value of 130 nM[3].

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

Western Blot Analysis[3]

Cell Line: HCV NS5B
Concentration: 0, 0.016, 0.08, 0.4, 2, 10 μM
Incubation Time:
Result: Resulted migration of CTP substrate (at 10 μM), decreased pCpG reaction product with increasing concentrations and significantly decreased at a dosage >2 μM.
Indicated blocking NS5B initiation.
Clinical Trial
Molecular Weight

554.37

Formula

C27H25BF2N2O6S

CAS No.
SMILES

FC1=CC(CN(C2=CC3=C(C=C2C4CC4)C(C(NC)=O)=C(C5=CC=C(C=C5)F)O3)S(C)(=O)=O)=CC=C1B(O)O

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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GSK5852 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.

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Product Name:
GSK5852
Cat. No.:
HY-150760
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