货号	规格	价格	上海	北京	珠海	重庆	武汉
S87867-5mg买3赠1	99.20%	￥260.00 S87867-5mg ￥260.00 现货（买3赠1）	2 2	-	-	-	-
S87867-10mg买3赠1	99.20%	￥450.00 S87867-10mg ￥450.00 现货（买3赠1）	4 4	-	-	-	-
S87867-25mg买3赠1	99.20%	￥970.00 S87867-25mg ￥970.00 现货（买3赠1）	5 5	-	-	-	-
S87867-50mg买3赠1	≥98%	￥1650.00 S87867-50mg ￥1650.00 2-3天（买3赠1）	0 货期：2-3天	-	-	-	-
S87867-100mg买3赠1	≥98%	￥2620.00 S87867-100mg ￥2620.00 2-3天（买3赠1）	0 货期：2-3天	-	-	-	-

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产品描述：

NAcM-OPT is a specific, reversible inhibitor targeting N-Acetyl-UBE2M interaction with DCN1 （IC50: 79 nM).

靶点：

NEDD8; E1/E2/E3 Enzyme;NEDD8

体外研究：

NAcM-OPT inhibits neddylation in and prevents anchorage-independent growth of a DCN1 amplified cell line without causing changes in protein homeostasis

体内研究：

NAcM-OPT has an oral bioavailability of 88% (calculated using IV dose at 1.5 mg/kg and PO dose at 50 mg/kg)

细胞实验：

Exponentially growing cells were plated in 6-well plates at 0.4 × 10^6 cells/well in 2 ml of media and incubated overnight at 37 °C in a humidified 5% CO2 incubator. 24 and 48 hrs after plating, the media was aspirated and replenished with 2 ml fresh media containing either 4 μL of DMSO or a 500× compound DMSO stock solution. The cells were harvested after 72 hrs via trypsinization, thoroughly washed with PBS, pelleted, flash frozen in liquid N2, and stored at ?80 °C. Cell pellets were thawed on ice and lysed by harvested resuspension in 30–40 μL of lysis buffer [50 mM Tris, 150 mM NaCl, 0.5% NP-40, 0.1% SDS, 6.5 M Urea, 2 mM 1,10-orthophenanthroline, 1× Halt Protease and Phosphatase inhibitor cocktail, 0.25 kU Universal Nuclease, pH 7.5]. Cell suspensions were incubated on ice for 25 minutes with occasional mixing by pipetting up and down. Lysates were cleared by centrifugation at 13,000 rpm for 20 minutes and the supernatant collected. The protein concentration of total cell lysate was determined by BCA ass

参考文献：

1. Scott DC, et al. Blocking an N-terminal acetylation-dependent protein interaction inhibits an E3 ligase. Nat Chem Biol. 2017 Aug;13(8):850-857. 2. Hammill JT, et al. Discovery of an Orally Bioavailable Inhibitor of Defective in Cullin Neddylation 1 (DCN1)-Mediated Cullin Neddylation. J Med Chem. 2018 Apr 12;61(7):2694-2706.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.302 ml	11.51 ml	23.02 ml
5 mM	0.46 ml	2.302 ml	4.604 ml
10 mM	0.23 ml	1.151 ml	2.302 ml
50 mM	0.046 ml	0.23 ml	0.46 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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