WS-383 free base

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

WS-383 free base 

WS-383 free base 是一种有效、选择性、可逆的 DCN1-UBC12 相互作用抑制剂，IC50 值为 11 nM。WS-383 free base 抑制 Cul3/1 的类泛素化修饰，引起 p21，p27 和 NRF2 的积累。

WS-383 free base

WS-383 free base Chemical Structure

CAS No. : 2247543-65-1

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WS-383 free base 的其他形式现货产品:

WS-383

生物活性

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

IC50 & Target

IC50: 11 nM (DCN1–UBC12 interaction)[1]
体外研究
(In Vitro)

WS-383 (10 μM) is against a panel of kinases such as BTK, CDKs, and EGFR [L858R] using staurosporine and afatinib 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[1].
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[1].
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[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

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[1]

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.

分子量

461.99

Formula

C18H20ClN9S2
CAS 号

2247543-65-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
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.

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