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PMD-026 (PMD026) is an oral, reversible small molecule inhibitor of ribosomal S6 kinase (RSK1-4) with IC50 of 2 nM (RSK1), 0.7 nM (RSK2), 0.9 nM (RSK3) and 2 nM (RSK4).PMD-026 decreased YB-1 phosphorylation as well as AR V7 mRNA and AR variants expressions in 22Rv1 cells.PMD-026 suppressed cell proliferation alone and in combination with the second-generation antiandrogens enzalutamide and darolutamide by inducing cellular apoptosis and G2/M arrest.PMD-026 suppressed tumor growth, and the combination of PMD-026 and enzalutamide inhibited tumor growth more prominently than single treatment in mouse xenograft models.
PMD-026 (PMD026) is an oral, reversible small molecule inhibitor of ribosomal S6 kinase (RSK1-4) with IC50 of 2 nM (RSK1), 0.7 nM (RSK2), 0.9 nM (RSK3) and 2 nM (RSK4).PMD-026 decreased YB-1 phosphorylation as well as AR V7 mRNA and AR variants expressions in 22Rv1 cells.PMD-026 suppressed cell proliferation alone and in combination with the second-generation antiandrogens enzalutamide and darolutamide by inducing cellular apoptosis and G2/M arrest.PMD-026 suppressed tumor growth, and the combination of PMD-026 and enzalutamide inhibited tumor growth more prominently than single treatment in mouse xenograft models.
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