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GSK5852

CAS No. : 1331942-30-3

MCE 國際站：GSK5852

產(chǎn)品活性：GSK5852 (GSK2485852) 是一種 HCV NS5B RdRp 聚合酶抑制劑。GSK5852 抑制 NS5B, IC₅₀ 為50 nM。GSK5852 具有抗病毒活性，抑制丙型肝炎病毒 (HCV) 的 EC₅₀ 為 3.0 nM (GT1a) 和 1.7 nM (GT1b)。

研究領(lǐng)域：Anti-infection

作用靶點：HCV

In Vitro: Nonstructural protein 5B (NS5B) RNA-dependent RNA polymerase (RdRp) is a component of HCV, for researching HCV infection-related diseases.
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.
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.
GSK5852 displays an excellent resistance profile and shows a <5-fold potency loss across the clinically important NS5B resistance mutations.
GSK5852 shows no cross-resistance against known resistance mutations in NS5B.
GSK5852 (compound 3) (0-10 μM) blocks the initiation step of NS5B polymerase cycle.
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.
GSK5852 (0.6, 10 μM; 15 min) inhibits NS5B?21 1b 316N with an IC₅₀ value of 130 nM.

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Trending products：Recombinant Proteins? |? Bioactive Screening Libraries? |? Natural Products? |? Dye Reagents? |? PROTAC? |? Isotope-Labeled Compounds

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