383907-43-5
Chemical Structure
NSC 663284
Synonym(s): DA-3003-1
- CAS No.: 383907-43-5
- Formula:C15H16ClN3O3
- Molecular Weight:321.76
IUPAC Name: 6-chloro-7-((2-morpholinoethyl)amino)quinoline-5,8-dione
InChIKey: BMKPVDQDJQWBPD-UHFFFAOYSA-N
SMILES: O=C(C(Cl)=C1NCCN2CCOCC2)C3=C(N=CC=C3)C1=O
Biological Activity: 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].
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NSC 663284 | 99.29% | 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. NSC 663284 inhibits NSD2 (IC50 of 170 nM) through a direct interaction with the catalytic SET domain (Kd of 370 nM). | ||||||||||||||||||||
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NSC 663284 (Standard) | ≥98% | 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. NSC 663284 inhibits NSD2 (IC50 of 170 nM) through a direct interaction with the catalytic SET domain (Kd of 370 nM). | ||||||||||||||||||||
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- [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. [Content Brief]
- [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. [Content Brief]
Keywords
