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WSB1 Degrader 1
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WSB1 Degrader 1
CAS No. : 2306039-66-5
MCE 站:WSB1 Degrader 1
产品活性:WSB1 Degrader 1 是一种有效的具有口服活性的 WSB1 (WD repeat and SOCS box-containing 1) 降解剂。WSB1 Degrader 1 具有抗癌转移作用。
研究领域:Metabolic Enzyme/Protease
作用靶点:E1/E2/E3 Enzyme
In Vitro: WSB1 Degrader 1 (compound 4; 0.25-2500 nM; 2-24 hours; H1299-WSB1 cells) treatment indues WSB1 degradation in time-dependent and dose-dependent manners.
WSB1 Degrader 1 (compound 4) exhibits potent antimigration efficacy in both KHOS and H460 cell lines with IC50 values of 39.1 μM and 24.47 μM, respectively.
WSB1 Degrader 1 (compound 4) significantly inhibits cancer cell migration under normoxia and hypoxia in KHOS cells. WSB1 Degrader 1 (5 μM) treatment elevates the levels of the RhoGDI2 protein in KHOS cells under hypoxia.
The wound-healing of H1299-WSB1 cells is significantly inhibited by treating with WSB1 Degrader 1. WSB1 Degrader 1 can only block the wound-healing capability of wild-type A2780 (A2780-WT) cells but not the A2780-WSB1/KO cells.
In Vivo: WSB1 Degrader 1 (compound 4; 100 mg/kg; p.o.; daily; for 28 days) treatment can effectively inhibit the pulmonary metastasis of cancer cells.
In rats, after 100 mg/kg oral dosing or 160 mg/kg intraperitoneal dosing of WSB1 Degrader 1 (compound 4), the two ways of administration are observed with quick absorption (Tmax), but the former dosing displayed a fast clearance (T1/2). Moreover, Cmax and AUC0-t values of WSB1 Degrader 1 in oral or intraperitoneal dosing groups showed acceptable blood exposure.
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