2. Anti-infection
  3. HCV
  4. GSK5852

GSK5852  (Synonyms: GSK2485852)

目录号: HY-150760
产品使用指南

摩尔计算器

GSK5852 (GSK2485852) 是一种 HCV NS5B RdRp 聚合酶抑制剂。GSK5852 抑制 NS5B, IC50 为50 nM。GSK5852 具有抗病毒活性，抑制丙型肝炎病毒 (HCV) 的 EC50 为 3.0 nM (GT1a) 和 1.7 nM (GT1b)。

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GSK5852 Chemical Structure

GSK5852 Chemical Structure

CAS No. : 1331942-30-3

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Customer Review

GSK5852 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Huh-7 EC50
1.4 nM
Compound: 3, GSK5852
Antiviral activity against wild type Hepatitis C virus genotype 1b harboring C316Y mutant infected in human HuH7 cells assessed as inhibition of viral replication after 72 hrs by Bright-glo luciferase reporter gene assay
Antiviral activity against wild type Hepatitis C virus genotype 1b harboring C316Y mutant infected in human HuH7 cells assessed as inhibition of viral replication after 72 hrs by Bright-glo luciferase reporter gene assay
[PMID: 23672667]
Huh-7 EC50
1.7 nM
Compound: 3, GSK5852
Antiviral activity against wild type Hepatitis C virus genotype 1b infected in human HuH7 cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay
Antiviral activity against wild type Hepatitis C virus genotype 1b infected in human HuH7 cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay
[PMID: 23672667]
Huh-7 EC50
1.9 nM
Compound: 3, GSK5852
Antiviral activity against wild type Hepatitis C virus genotype 1b harboring C316N mutant infected in human HuH7 cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay
Antiviral activity against wild type Hepatitis C virus genotype 1b harboring C316N mutant infected in human HuH7 cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay
[PMID: 23672667]
Huh-7 EC50
3 nM
Compound: 3, GSK5852
Antiviral activity against wild type Hepatitis C virus genotype 1a infected in human HuH7 cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay
Antiviral activity against wild type Hepatitis C virus genotype 1a infected in human HuH7 cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay
[PMID: 23672667]
Huh-7 EC50
3.2 nM
Compound: 3, GSK5852
Antiviral activity against wild type Hepatitis C virus genotype 1a harboring C316Y mutant infected in human HuH7 cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay
Antiviral activity against wild type Hepatitis C virus genotype 1a harboring C316Y mutant infected in human HuH7 cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay
[PMID: 23672667]
Huh-7 EC50
3.8 nM
Compound: 3, GSK5852
Antiviral activity against wild type Hepatitis C virus genotype 1b harboring C316F mutant infected in human HuH7 cells assessed as inhibition of viral replication after 72 hrs by Bright-glo luciferase reporter gene assay
Antiviral activity against wild type Hepatitis C virus genotype 1b harboring C316F mutant infected in human HuH7 cells assessed as inhibition of viral replication after 72 hrs by Bright-glo luciferase reporter gene assay
[PMID: 23672667]
Huh-7 EC50
4.2 nM
Compound: 3, GSK5852
Antiviral activity against wild type Hepatitis C virus genotype 1b harboring S365T mutant infected in human HuH7 cells assessed as inhibition of viral replication after 72 hrs by Bright-glo luciferase reporter gene assay
Antiviral activity against wild type Hepatitis C virus genotype 1b harboring S365T mutant infected in human HuH7 cells assessed as inhibition of viral replication after 72 hrs by Bright-glo luciferase reporter gene assay
[PMID: 23672667]
体外研究
(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].

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

GSK5852 相关抗体:

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
分子量

554.37

Formula

C27H25BF2N2O6S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

GSK5852 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

GSK58521331942-30-3GSK2485852GSK 5852GSK-5852GSK 2485852GSK-2485852HCVHepatitis C virusnonstructural protein 5BNS5BRNA-dependent RNA polymeraseRdRpfluoro derivativeantiviralInhibitorinhibitorinhibit

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