Remodelin hydrobromide

Remodelin HBr salt is a novel potent and selective inhibitor of the acetyl-transferase protein NAT10.IC50 value:Target: NAT10 inhibitorRemodelin can improve nuclear architecture, chromatin organization, and fitness of both human lamin A/C-depleted cells and HGPS-derived patient cells, and decrease markers of DNA damage in these cells. Using a combination of chemical, cellular, and genetic approaches, acetyl-transferase protein NAT10 was identified as the target of Remodelin that mediated nuclear shape rescue in laminopathic cells via microtubule reorganization. Down-regulation and mutations of the nuclear-architecture proteins lamin A and C cause misshapen nuclei and altered chromatin organization associated with cancer and laminopathies, including the premature-aging disease Hutchinson-Gilford progeria syndrome (HGPS). Remodelin is a useful chemical tool to study how NAT10 affects nuclear architecture and suggest alternative strategies for treating laminopathies and aging.

Signaling Pathways >> Epigenetics >> Histone Acetyltransferase

Research Areas >> Cancer

[1]. Larrieu D, et al. Chemical inhibition of NAT10 corrects defects of laminopathic cells. Science. 2014 May 2;344(6183):527-32.

A 485 | Curcumin | C646 | CPI-637 | SGC-CBP30 | GNE-272 | MG149 | WM 1119 | anacardic acid | I-CBP 112 | MOZ-IN-3 | Histone Acetyltransferase Inhibitor II | PF-CBP1 hydrochloride | TPOP146 | GNE-781