NSC 663284 (Standard)

NSC 663284 (Standard) is the analytical standard of NSC 663284 (HY-100034) . This product is intended for research and analytical applications. NSC 663284 (DA-3003-1) is a potent, cell-permeable, and irreversible Cdc25 dual specificity phosphatase inhibitor, has an IC50 for Cdc25B2 of 0.21 μM. NSC 663284 exhibits mixed competitive kinetics against Cdc25A, Cdc25B (2), and Cdc25C with Ki values of 29, 95, and 89 nM, respectively[1]. NSC 663284 inhibits NSD2 (IC50 of 170 nM) through a direct interaction with the catalytic SET domain (Kd of 370 nM) [2].

Product Specifications

CAS Number

[383907-43-5]

Target

Histone Methyltransferase; Phosphatase; Reference Standards

Related Pathways

Epigenetics; Metabolic Enzyme/Protease; Others

Field of Research

Cancer

Smiles

O=C(C(Cl)=C1NCCN2CCOCC2)C3=C(N=CC=C3)C1=O

Molecular Formula

C15H16ClN3O3

Molecular Weight

321.76

References & Citations

[1]Lazo JS, et al. Discovery and biological evaluation of a new family of potent inhibitors of the dual specificity protein phosphatase Cdc25. J Med Chem. 2001 Nov 22;44 (24) :4042-9.|[2]Guo J, et al. Pharmacology and antitumor activity of a quinolinedione Cdc25 phosphatase inhibitor DA3003-1 (NSC 663284) . Anticancer Res. 2007 Sep-Oct;27 (5A) :3067-73.|[3]Coussens NP, et al. High-throughput screening with nucleosome substrate identifies small-molecule inhibitors of the human histone lysine methyltransferase NSD2. J Biol Chem. 2018 Aug 31;293 (35) :13750-13765.