NSC 663284

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

Product Name Alternative

DA-3003-1

UNSPSC

12352005

Hazard Statement

H315, H319, H335

Target

Histone Methyltransferase; Phosphatase

Type

Reference compound

Related Pathways

Epigenetics; Metabolic Enzyme/Protease

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/NSC_663284.html

Purity

99.56

Solubility

DMSO : ≥ 100 mg/mL

Smiles

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

Molecular Formula

C15H16ClN3O3

Molecular Weight

321.76

Precautions

H315, H319, H335

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.