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WS-383

CAS No. : 2247544-02-9

MCE 站：WS-383

产品活性：WS-383 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 抑制 Cul3/1 的类泛素化修饰，引起 p21，p27 和 NRF2 的积累。

研究领域：Metabolic Enzyme/Protease

作用靶点：E1/E2/E3 Enzyme

In Vitro: 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.

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