SAICAR is an intermediate of de novo purine nucleotide biosynthesis, activates pyruvate kinase isoform M2 (PKM2) in an isozyme-selective manner (EC50: 0.3 mM).
Multi-target kinase-IN-9 是一种具有抗增殖和抗血管生成活性的多靶点酶抑制剂,对肝癌细胞显示显著选择性。其可广泛结合 DNA 聚合酶 β、丙酮酸激酶 (Pyruvate Kinase)M2(PKM2) 等关键酶的活性位点或 ATP 结合区域,破坏 DNA 修复与复制、糖酵解、染色质动态及转录程序,并抑制癌症干细胞自我更新,进而导致基因组不稳定性、溶酶体功能障碍及自噬流中断,诱导肿瘤细胞死亡,抑制肿瘤增殖、侵袭、转移与血管生成,并显著降低异种移植模型中的肿瘤体积,可用于肝癌相关研究。
ZINC08383544 is a specific pyruvate kinase M2 activator which promotes the formation of PKM2 tetramer. ZINC08383544 effectively blocks PKM2 nuclear translocation, and inhibits the growth of tumor.
TLN-232, also known as CAP-232, is a synthetic cyclic heptapeptide with potential antineoplastic activity. Pyruvate kinase (PK) inhibitor TLN-232 targets pyruvate kinase M2 (M2PK), which may disrupt tumor cell anaerobic glycolysis. M2PK is a dimeric isoform of PK and the predominant PK isoform found in tumor cells.