NSC-663284

Aliases: NSC-663284, 6-Chloro-7-[[2-(4-morpholinyl)ethyl]amino]-5,8-quinolinedione
Catalog No: 14122 Format: 25 mg $420 Buy
Catalog No: 14123 Format: 5 mg $105 Buy
Application: Histone Methylation (HMT & HDM)

Chemical Properties

MW = 321.8
C15H16ClN3O3
CAS 383907-43-5
>98% (TLC); NMR (Conforms)

Description

Potent and selective inhibitor of the protein lysine methyltransferase SETD8 (IC50 = 0.21 µM) which efficiently suppresses cellular H4K20me1 at doses lower than 5 µM (ref 1). Also inhibits CDC25 phosphatases (ref 2). Arrests cells at G1 and G2/M and inhibits cdk1 and 2 activation (ref 3). Inhibits the growth of a variety of human tumor cell lines (ref 4).

Contents

Red powder. May be dissolved in DMSO (15 mg/ml); or ethanol (55 mg/ml).

Storage Conditions

Store desiccated as supplied at -20° for up to 2 years. Store solutions at -20°C for up to 1 month.

References

1. G Blum et al. ACS Chem. Biol. 2014, 9:2471
2. JS Lazo et al. J. Med. Chem. 2001, 44:4042
3. L Pu et al. J. Biol. Chem. 2002, 277:46877
4. Y Han et al. J. Pharmacol. Exp. Ther. 2004, 309:64

 
Chemical structure of NSC-663284.

Chemical structure of NSC-663284.