TH5427 hydrochloride

Names

[ Name ]:
TH5427 hydrochloride

Biological Activity

[Description]:

TH5427 hydrochloride is a potent, selective NUDT5 inhibitor (IC50=29 nM). TH5427 hydrochloride shows an apparent 690-fold selectivity for NUDT5 over MTH1. TH5427 hydrochloride blocks progestin-dependent, PAR-derived nuclear ATP synthesis and subsequent chromatin remodeling, gene regulation and proliferation in breast cancer cells[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> DNA/RNA Synthesis

[In Vitro]

TH5427 hydrochloride inhibits progestin-dependent nuclear ATP synthesis in breast cancer cells. TH5427 hydrochloride significantly disrupted EGFR and MMTV-luc expression following progestin stimulation. TH5427 hydrochloride abrogates the progestin-dependent proliferation response in T47DWT cells[1].

[References]

[1]. Page BDG, et al. Targeted NUDT5 inhibitors block hormone signaling in breast cancer cells [published correction appears in Nat Commun. 2019 Nov 1;10(1):5050]. Nat Commun. 2018;9(1):250. Published 2018 Jan 17.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₀H₂₁Cl₃N₈O₃

[ Molecular Weight ]:
527.79

Related Compounds

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