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DA3003-1

Chemical Structure : DA3003-1

CAS No.: 383907-43-5

DA3003-1 (SPS8I1;NSC 663284)

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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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).

Physicochemical Properties

M.Wt 321.8
Formula C15H16ClN3O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

6-chloro-7-[[2-(4-morpholinyl)ethyl]amino]-5,8-quinolinedione

References

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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