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Remodelin

Names

[ CAS No. ]:
949912-58-7

[ Name ]:
Remodelin

[Synonym ]:
Benzonitrile, 4-[2-(2-cyclopentylidenehydrazinyl)-4-thiazolyl]-
4-[2-(2-Cyclopentylidenehydrazino)-1,3-thiazol-4-yl]benzonitrile
4-[2-(2-cyclopentylidenehydrazinyl)-1,3-thiazol-4-yl]benzonitrile
Remodelin

Biological Activity

[Description]:

Remodelin 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.

[Related Catalog]:

Signaling Pathways >> Epigenetics >> Histone Acetyltransferase
Research Areas >> Cancer

[References]

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


[Related Small Molecules]

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 | Remodelin hydrobromide | TPOP146

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
498.9±47.0 °C at 760 mmHg

[ Molecular Formula ]:
C15H14N4S

[ Molecular Weight ]:
282.363

[ Flash Point ]:
255.5±29.3 °C

[ Exact Mass ]:
282.093903

[ PSA ]:
89.31000

[ LogP ]:
2.16

[ Vapour Pressure ]:
0.0±1.3 mmHg at 25°C

[ Index of Refraction ]:
1.702

[ Storage condition ]:
2-8℃

Related Compounds