TargetMol

NSC 663284

Product Code:
 
TAR-T16357
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
1 / 1
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Further Information

Bioactivity:
NSC 663284 is a cell-permeable and irreversible Cdc25 dual specificity phosphatase inhibitor (IC50 for Cdc25B2: 0.21 μM). NSC 663284 inhibits NSD2 (IC50 of 170 nM) through direct interaction with the catalytic SET domain (Kd of 370 nM). NSC 663284 displays mixed competitive kinetics against Cdc25A, Cdc25B(2), and Cdc25C with Ki values of 29, 95, and 89 nM, respectively.
CAS:
383907-43-5
Formula:
C15H16ClN3O3
Molecular Weight:
321.76
Pathway:
Membrane transporter/Ion channel; Metabolism
Purity:
0.98
SMILES:
ClC1=C(NCCN2CCOCC2)C(=O)c2ncccc2C1=O
Target:
Calcium Channel

References

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. 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. 3. 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.