化合物PSI6206 T2117

Product Introduction
Bioactivity


英文名: PSI-6206

描述: PSI-6206 (RO 2433) 是 PSI-6130 的脱氨衍生物，PSI-6206 是一种选择性 HCV RNA 聚合酶抑制剂，低效抑制HCV 复制，EC90为 >100 μM。PSI-6130 是一种有效的选择性 HCV NS5B 聚合酶抑制剂。

激酶实验: Protein Kinase Assays: The in vitro kinase assays are performed in 96-well plates (30 μL) at ambient temperature for 15–45 min using the recombinant glutathione S-transferase-fused kinase domains (4-100 ng, depending on specific activity). [γ33P]ATP is used as phosphate donor and polyGluTyr-(4:1) peptide as acceptor. With the exception of protein kinase C-α, cyclin-dependent kinase 1/cycB and protein kinase A are protamine sulfate (200 μg/mL), histone H1 (100 μg/mL), and the heptapeptide Leu-Arg-Arg-Ala-Ser-Leu-Gly (known as Kemptide Bachem) respectively and are used as peptide substrates. Assays are optimized for each kinase using the following ATP concentrations: 1.0 μM (c-Kit, c-Met, c-Fms, c-Raf-1, and RET), 2.0 μM (EGFR, erbB2, ErbB3, and ErbB4), 5.0 μM (c-abl), 8.0 μM (Flt-1, Flt-3, Flt-4, Flk, KDR, FGFR-1, and Tek), 10.0 μM (PDGFR-β, protein kinase C-α, and cyclin-dependent kinase 1), and 20.0 μM (c-Src and protein kinase A). The reaction is terminated by the addition of 20 μL 125 mM EDTA. Thirty μL (c-abl, c-Src, insulin-like growth factor-1R, RET-Men2A, and RET-Men2B) or 40 μL (all other kinases) of the reaction mixture is transferred onto Immobilon-polyvinylidene difluoride membrane, presoaked with 0.5% H3PO4 and mounted on a vacuum manifold. Vacuum is then applied and each well rinsed with 200 μL 0.5% H3PO4. Membranes are removed and washed four times with 1.0% H3PO4 and once with ethanol. Dried membranes are counted after mounting in a Packard TopCount 96-well frame and with the addition of 10 μL/well of Microscint. IC50 values (±SE) are calculated by linear regression analysis of the percentage inhibition and are averages of at least three determinations.

体外活性: PSI-6206 (RO2433) is tested for anti-HCV activity in both a cell-based quantitative real-time RT-PCR assay and surrogate bovine viral diarrhea virus (BVDV) assays and demonstrates no activity or cytoxicity in any assay[1]. The formation of the 5′-triphosphate (TP) of PSI-6130 (PSI-6130-TP) and RO2433 (RO2433-TP) increases with time and reached steady state levels at 48 h. RO2433-TP also inhibits RNA synthesis by the native HCV replicase isolated from HCV replicon cells and the recombinant HCV polymerase NS5B[2]. PSI-6206 (RO2433) is the deaminated derivative of PSI-6130, which is a potent and selective inhibitor of HCV NS5B polymerase[3].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 60 mg/mL (230.57 mM)


关键字: Inhibitor | Hepatitis C virus | PSI 6206 | RO-2433 | inhibit | RO2433 | PSI6206 | PSI-6206 | GS 331007 | HCV | GS331007

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相关库: Nucleotide Compound Library | Anti-Aging Compound Library | Anti-COVID-19 Compound Library | Mini Electrophilic Heterocyclic Fragment Library | Bioactive Compounds Library Max | Inhibitor Library | Featured Fragment Library | High Solubility Fragment Library | Anti-Viral Compound Library | Anti-Infection Compound Library

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