产品
编 号:F564636
分子式:C18H20ClN9S2
分子量:461.99
产品类型
结构图
CAS No: 2247543-65-1
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产品详情
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.
体外研究:
WS-383?(10 μM) is against a panel ofkinases 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.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.