Remodelin, Acetyl-transferase NAT10 Inhibitor

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

Product information

CAS Number: 949912-58-7

Molecular Weight: 282.36

Formula: C15H14N4S

Chemical Name: 4-(2-(2-cyclopentylidenehydrazinyl)thiazol-4-yl)benzonitrile

Smiles: N#CC1=CC=C(C=C1)C1=CSC(NN=C2CCCC2)=N1

InChiKey: XAEJIFARBQJLML-UHFFFAOYSA-N

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)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

Remodelin was used at 1-10 µM in vitro and cellular assays.

In Vivo:

n/a

References:

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

Products are for research use only. Not for human use.