Hypothemycin

一种具有多种生物活性的二羟基苯甲酸内酯聚酮化合物；抑制MEK（IC50=15nM）和其他在ATP结合域中含有保守半胱氨酸残基的蛋白激酶，包括ERK、PDGFR、VEGF、PKD1和MAPKAP5/MK5；抑制TAK1（IC50=33nM）；抑制A549、MV-4-11和EOL1细胞的增殖（IC50分别为6、0.006和0.0004µM）；以每天25mg/kg的剂量降低Ma44和HCT116小鼠异种移植模型中的肿瘤生长。A resorcylic acid lactone polyketide with diverse biological activities; inhibits MEK (IC50 = 15 nM) and other protein kinases containing a conserved cysteine residue in the ATP-binding domain, including ERK, PDGFR, VEGF, PKD1, and MAPKAP5/MK5; inhibits TAK1 (IC50 = 33 nM); inhibits proliferation of A549, MV-4-11, and EOL1 cells (IC50s = 6, 0.006, and 0.0004 µM, respectively); reduces tumor growth in Ma44 and HCT116 mouse xenograft models at 25 mg/kg per day.