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WS-383

CAS No. : 2247544-02-9

產(chǎn)品活性：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.

研究領(lǐng)域：Metabolic Enzyme/Protease

作用靶點(diǎn)：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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