| Name | Dasabuvir |
| Description | Dasabuvir (ABT-333) is a non-nucleoside inhibitor of the hepatitis C virus (HCV) non-structural protein 5B (NS5B), an RNA-dependent RNA polymerase. Upon administration and intracellular uptake, dasabuvir binds HCV NS5B polymerase, blocking viral RNA synthesis and replication. The HCV NS5B protein is essential for the replication of the HCV RNA genome. |
| Kinase Assay | The recombinant HCV polymerases used in this study contain the first 570 amino acids of the 591-amino acid native protein sequence, with a six-histidine tag at the N terminus to facilitate purification by affinity chromatography. Briefly, ABT-333 (Dasabuvir) is incubated with 5 to 50 nM polymerase for 15 min at room temperature, follow by the addition of nucleoside triphosphates (NTPs) and [3H]UTP for 3 h at 30°C. After termination of the reaction, the precipitated RNA is captured by filtration through a GF/B filter. The amount of incorporated [3H]UTP is measured by scintillation counting with a Wallac 1450 MicroBeta counter. The percent inhibition is calculated from the initial rates of inhibited reactions relative to that of the uninhibited control reaction. The mean 50% inhibitory concentration (IC50) and the standard error of the mean (SEM) are calculated via nonlinear regression[1]. |
| In vitro | ABT-333 (Dasabuvir) is at least 7,000-fold selective for the inhibition of HCV genotype 1 polymerases over human/mammalian polymerases. ABT-333 (Dasabuvir) inhibits the polymerase enzymatic activity of genotype 1 laboratory strain enzymes (H77, BK, N, and Con1 strains), as well as enzymes produced from polymerase genes from HCV genotype 1-infected subjects, with IC50s between 2.2 and 10.7 nM. ABT-333 inhibits replication of HCV subgenomic replicons in cell culture assays, with EC50 values of 7.7 and 1.8 nM against genotype 1a (H77) and 1b (Con1), respectively. In the presence of 40% human plasma, there is a 12- to 13-fold decrease in inhibitory potency, yielding EC50s of 99 and 21 nM for HCV genotype 1a (H77) and 1b (Con1) replicons, respectively[1]. |
| Storage | keep away from moisture,store under nitrogen | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 60 mg/mL (121.56 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.05 mM), Sonication is recommended.
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| Keywords | RNA | NS5B polymerase | Inhibitor | inhibit | Hepatitis C virus | HCVProtease | HCV Protease | HCV polymerase | HCV genotype 1 infections | HCV | genotype | DNA/RNA Synthesis | Dasabuvir | ABT333 | ABT 333 |
| Inhibitors Related | 5-Fluorouracil | Adenine hemisulfate | Erythromycin thiocyanate | Methyl 2-amino-5-bromobenzoate | Sofosbuvir | Guanidine hydrochloride | Hexane-1,6-diol | 1,4-Naphthoquinone | Adenine | Carbazole | Thymidine | Usnic Acid |
| Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Pediatric Drug Library | EMA Approved Drug Library | Toxic Compound Library | Drug Repurposing Compound Library | Anti-Viral Compound Library | Inhibitor Library | FDA-Approved Drug Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-COVID-19 Compound Library |
United States
