| Bioactivity | TH1217 (ZINC1775962367) is a potent and selective dCTPase pyrophosphatase 1 (dCTPase) inhibitor, with an IC50 of 47 nM. TH1217 enhances the cytotoxic effect of cytidine analogues in leukemia cells. TH1217 also could modulate SARS-Cov-2 interactors, so it shows activity of against COVID-19[1][2]. | |||||||||
| Target | IC50: 47 nM (dCTPase) | |||||||||
| Invitro | TH1217 (compound 30) inhibits dCTPase and enhances aqueous solubility (>100 μM) and improves plasma stability in vitro(t4h=86%)[1].TH1217 presents suitable mouse microsomal half-lives (109 minutes)[1].TH1217 displays well cell permeability (8.66×10-6/1.30×10-3 cm/s) and CYP inhibition[1]. | |||||||||
| Name | TH1217 | |||||||||
| CAS | 1862212-48-3 | |||||||||
| Formula | C20H17BCl2N4O6 | |||||||||
| Molar Mass | 491.09 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
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| Reference | [1]. Llona-Minguez S, et, al. Discovery of the First Potent and Selective Inhibitors of Human dCTP Pyrophosphatase 1. Med Chem. 2016 Feb 11; 59(3): 1140-1148. [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. |
TH1217
CAS: 1862212-48-3 F: C20H17BCl2N4O6 W: 491.09
TH1217 (ZINC1775962367) is a potent and selective dCTPase pyrophosphatase 1 (dCTPase) inhibitor, with an IC50 of 47 nM.
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