DA3003-1 (SPS8I1, NSC 663284)

Chemical Structure : DA3003-1

CAS No.: 383907-43-5

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货号: 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.

规格	价格	库存
5 mg	￥780	In stock
10 mg	￥1180	In stock
25 mg	￥1980	In stock
50 mg		Get quote
100 mg		Get quote

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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).

物理化学性质&存储条件

分子量	321.8
分子式	C15H16ClN3O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	6-chloro-7-[[2-(4-morpholinyl)ethyl]amino]-5,8-quinolinedione

参考文献

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.