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TH 1217

Names

[ CAS No. ]:
1862212-48-3

[ Name ]:
TH 1217

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cancer
Research Areas >> Infection
Signaling Pathways >> Anti-infection >> SARS-CoV

[Target]

IC50: 47 nM (dCTPase)[1]


[In Vitro]

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].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C20H17BCl2N4O6

[ Molecular Weight ]:
491.09

[ Storage condition ]:
-20°C

Related Compounds