In Vitro: Remodelin hydrobromide (10-40 μΜ, 1-7 days) inhibits NAT10 activity and cell proliferation with a dose-dependent manner in both AR-positive and AR-negative prostate cancer cells. Remodelin hydrobromide (20 μΜ, 24 hours) inhibits NAT10 and slows DNA replication in prostate cancer cells. Remodelin hydrobromide (1 μΜ, 7 days) decreases nuclear shape defects and increase genomic stability in LmnaG609G/G609G fibroblasts.
In Vivo: Remodelin hydrobromide (2 or 20 mg/kg, i.p., once every two days for 4 weeks) significantly reduces AR-negative prostate cancer tumor growth in tumor xenograft nude mice model. Remodelin hydrobromide (100 mg/kg, p.o.) inhibits NAT10 and significantly enhances the healthspan in aLmnaG609G/G609G hutchinson-gilford progeria syndrome (HGPS) mouse model. Remodelin hydrobromide (5 mg/kg, p.o.) shows a T1/2 of 1.81 hours and oral bioavailability (F%) of 43.5% in mice. Pharmacokinetic parameters for Remodelin hydrobromide in Mice
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