| Description | TH1217, a potent and selective inhibitor of dCTPase pyrophosphatase 1 (dCTPase), demonstrates an IC50 value of 47 nM. It amplifies the cytotoxic impact of cytidine analogues on leukemia cells and exhibits potential against COVID-19 by modulating SARS-CoV-2 interactors. |
| In vitro | TH1217 抑制dCTPase，增强水溶性(>100 μM)并在体外提高血浆稳定性(t4h=86%)。TH1217展现出适宜的小鼠微粒体半衰期(109分钟)。此外，TH1217具有良好的细胞渗透性(8.66×10^-6/1.30×10^-3 cm/s)和CYP抑制作用[1]。 |
| Target activity | TPase:47 nM (IC50) |
| Synonyms | TH 1217 |
| molecular weight | 491.09 |
| Molecular formula | C20H17BCl2N4O6 |
| CAS | 1862212-48-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 117 mg/mL (238.2 mM), Sonication is recommended. |
| References | 1. Llona-Minguez et al (2016) Discovery of the first potent and selective inhibitors of human dCTP pyrophosphatase 1. J.Med.Chem. 59 1140 2. Gordon DE, et, al. A SARS-CoV-2-Human Protein-Protein Interaction Map Reveals Drug Targets and Potential Drug-Repurposing. bioRxiv. 2020 Mar 22; 2020.03.22.002386. |