949912-58-7

949912-58-7 structure

Name: Remodelin
Chemical Name: Benzonitrile, 4-[2-(2-cyclopentylidenehydrazinyl)-4-thiazolyl]
CAS Number: 949912-58-7
Molecular Formula: C₁₅H₁₄N₄S
Molecular Weight: 282.363
Catalog: Signaling Pathways Epigenetics Histone Acetyltransferase
Create Date: 2018-12-06 18:07:12
Modify Date: 2024-01-02 17:10:02
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.

Name	Benzonitrile, 4-[2-(2-cyclopentylidenehydrazinyl)-4-thiazolyl]
Synonyms	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

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.