Chemical Structure : DA3003-1
CAS No.: 383907-43-5
Catalog No.: PC-62679Not For Human Use, Lab Use Only.
NSC 663284 (SPS8I1, DA3003-1) is a potent inhibitor of the dual specificity protein phosphatase Cdc25 with Ki of 9/95//89 nM for Cdc25A/Cdc25B2/Cdc25C, also inhibits NSD2 catalytic SET domain with IC50/Ki of 170/370 nM.
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NSC 663284 (SPS8I1, DA3003-1) is a potent inhibitor of the dual specificity protein phosphatase Cdc25 with Ki of 9/95//89 nM for Cdc25A/Cdc25B2/Cdc25C, also inhibits NSD2 catalytic SET domain with IC50/Ki of 170/370 nM.
NSC 663284 displays 20- and 450-fold more selective over VHR or PTP1B phosphatases.
NSC 663284 (SPS8I1, DA3003-1) blocks cellular Erk dephosphorylation caused by ectopic Cdc25A expression.
NSC 663284 (SPS8I1, DA3003-1) also shows to be a potent and selective SETD8 inhibitor with apparent IC50 of 0.21 uM.
NSC 663284 (SPS8I1, DA3003-1) shows 2.5-fold lower than SMYD2, >6-fold lower than other PMTs (IC50=1.3-100 uM).
M.Wt | 321.8 | |
Formula | C15H16ClN3O3 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
6-chloro-7-[[2-(4-morpholinyl)ethyl]amino]-5,8-quinolinedione |
1. Lazo JS, et al. J Med Chem. 2001 Nov 22;44(24):4042-9.
2. Pu L, et al. J Biol Chem. 2002 Dec 6;277(49):46877-85.
3. Blum G, et al. ACS Chem Biol. 2014 Nov 21;9(11):2471-8.
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