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Key Documents

5.31066

Sigma-Aldrich

Remodelin

Synonyme(s) :

Remodelin, Cyclopentylidene-(4-(4-cyanophenyl)thiazol-2-yl)hydrazine, HBr, 4-(4-Chlorophenyl)-2-(2-cyclopentylidenehydrazinyl)thiazole, HBr, 4-(2-(2-Cyclopentylidenehydrazino)-1,3-thiazol-4-yl)benzonitrile, HBr

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About This Item

Formule empirique (notation de Hill):
C15H14N4S · xHBr
Numéro CAS:
Poids moléculaire :
282.36 (free base basis)
Code UNSPSC :
12352200
ID de substance PubChem :

Pureté

≥94% (HPLC)

Niveau de qualité

Forme

powder

Fabricant/nom de marque

Calbiochem®

Conditions de stockage

OK to freeze
desiccated (hygroscopic)
protect from light

Couleur

tan

Solubilité

DMSO: 50 mg/mL

Température de stockage

2-8°C

Chaîne SMILES 

C1CCC(=NNC2=NC(=CS2)C3=CC=C(C=C3)C#N)C1.Br

Description générale

A cell-permeable, potent, and stable analog of CPTH2 (Cat. No. 382111) that restores nuclear shape and chromatin compactin in AG11498 and AG06297 progeric fibroblasts from Hutchinson-Gilford progeria syndrome (HGPS) patients and in lamin A/C-depleted U2OS cells by inhibiting the activity of N-acetyltransferase 10 (NAT10; 10-50 µM). However, it does not affect non-laminopathic Werner syndrome cells. Improves DNA replication and enhances cell proliferation capacity. Also shown to prevent farnesyltransferase inhibitor-induced nuclear shape defects in normal fibroblasts and in U2OS cells and improves nuclear morphology in siLMNA (lamin A/C depletion by small interfering RNA transfection) treated cells. Does not affect Golgi apparatus integrity or tubulin polymer assembly and its effects are independent of mitosis.
A cell-permeable, potent, and stable analog of CPTH2 (Cat. No. 382111) that restores nuclear shape and chromatin compactin in AG11498 and AG06297 progeric fibroblasts from Hutchinson-Gilford progeria syndrome (HGPS) patients and in lamin A/C-depleted U2OS cells by inhibiting the activity of N-acetyltransferase 10 (NAT10; 10-50 µM). However, it does not affect non-laminopathic Werner syndrome cells. Improves DNA replication and enhances cell proliferation capacity. Also shown to prevent farnesyltransferase inhibitor-induced nuclear shape defects in normal fibroblasts and in U2OS cells and improves nuclear morphology in siLMNA (lamin A/C depletion by small interfering RNA transfection) treated cells. Does not affect Golgi apparatus integrity or tubulin polymer assembly and its effects are independent of mitosis.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Actions biochimiques/physiologiques

Cell permeable: yes
Primary Target
NAT10
Reversible: yes

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Autres remarques

Larrieu, D., et al. 2014. Science344, 527.

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable


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Consulter la Bibliothèque de documents

Delphine Larrieu et al.
Science (New York, N.Y.), 344(6183), 527-532 (2014-05-03)
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). Here, we identified the small molecule "Remodelin" that improved

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