货号	规格	价格	上海	北京	珠海	重庆	武汉
S89172-5mg促销	98.20%	￥1200.00 ￥960.00 S89172-5mg ￥960.00 现货	6 6	-	-	-	-
S89172-10mg促销	98.20%	￥1800.00 ￥1440.00 S89172-10mg ￥1440.00 现货	6 6	-	-	-	-
S89172-25mg促销	98.20%	￥3600.00 ￥2880.00 S89172-25mg ￥2880.00 现货	5 5	-	-	-	-
S89172-100mg促销	≥98%	￥10800.00 ￥8640.00 S89172-100mg ￥8640.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

WS-383 is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2

靶点：

IC50: 11 nM (DCN1-UBC12 interaction);E1/E2/E3Enzyme

体外研究：

WS-383 (10 μM) is against a panel of kinases such as BTK, CDKs, and EGFR [L858R] using staurosporine and BIBW 2992 as the positive controls. WS-383 showed weak inhibitory activity at 10.0 μM,it is selective to the DCN1-UBC12 interaction over the selected kinasesr. WS-383 (0.03-3 μM;24 hours) blocks Cul3 neddylation at 3 μM and also has certain inhibition of Cul1 neddylation at 10 μM but was not effective in inhibiting neddylation of other cullin members. WS-383 (0.03-3 μM;24 hours) increases Cul1, Skp1 (adaptor protein), F-box protein, and RBX1/RBX2 RING protein form SCF E3 complex. Cyclin dependent kinase inhibitor 1A (p21) and cyclin dependent kinase inhibitor 1B (p27) expression in a dose-dependent manner in MGC-803 and KYSE70 manner. Western Blot Analysis Cell Line: MGC-803 cells Concentration: 0.03 μM; 0.3 μM; 3 μM; 10 μM Incubation Time: 24 hours Result: Decreased N8-Cul1 and N8-Cul2 protein expression. Western Blot Analysis Cell Line: MGC-803 and KYSE70 cells Concentration: 0.03 μM; 0.3 μM; 3 μM; 10 μM Incubation Time: 24 hours Result: Induced accumulation of p21, p27, and NRF2 in MGC-803 cells.

参考文献：

1. Wang S, et al. Development of Highly Potent, Selective, and Cellular Active Triazolo[1,5- a]pyrimidine-Based Inhibitors Targeting the DCN1-UBC12 Protein-Protein Interaction. J Med Chem. 2019 Mar 14;62(5):2772-2797.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.006 ml	10.031 ml	20.062 ml
5 mM	0.401 ml	2.006 ml	4.012 ml
10 mM	0.201 ml	1.003 ml	2.006 ml
50 mM	0.04 ml	0.201 ml	0.401 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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