Remodelin

• CAT Number: I005642
• CAS Number: 949912-58-7
• Molecular Formula: C₁₅H₁₄N₄S
• Molecular Weight: 282.36
• Purity: ≥95%
• Synonyms: 4-[2-(2-cyclopentylidenehydrazinyl)-4-thiazolyl]-benzonitrile
• Target: NAT10
• Solubility: 10 mM in DMSO
• Storage: -20°C
• InChI: InChI=1S/C15H14N4S/c16-9-11-5-7-12(8-6-11)14-10-20-15(17-14)19-18-13-3-1-2-4-13/h5-8,10H,1-4H2,(H,17,19)
• InChIKey: XAEJIFARBQJLML-UHFFFAOYSA-N
• SMILES: C1CCC(=NNC2=NC(=CS2)C3=CC=C(C=C3)C#N)C1

Remodelin is a novel potent and selective inhibitor of the acetyl-transferase protein NAT10. 


Remodelin 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.

Reference

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