死亡相关蛋白激酶(Death-associated protein kinase, DAPK)是新近分类的丝氨酸/苏氨酸激酶家族的创始成员,其成员不仅在催化结构域具有显著的同源性,而且具有共同的细胞死亡相关功能。DAPK是一种肿瘤抑制基因,其表达在多种肿瘤类型中缺失,这一认识激发了人们对该激酶家族的兴趣,并产生了关于其功能、调节和与疾病的联系的大量文献。DAPK家族与几个细胞死亡相关的信号通路有关,也有人提出了细胞死亡以外的功能。
Drak2-in-1, a potent, selective and ATP-competitive DRAK2 inhibitor, has an IC50 and KIvalue of 3 nM and 0.26 nM, respectively.Drak2-in-1 also had an effect on DRAK1 (IC50=51 nM).
CK156 is a potent inhibitor of death-associated protein kinase (DAPK), demonstrating high selectivity. In the DRAK1 NanoBRET assay, CK156 exhibits IC50 values of 182 nM, 34 μM, and 39 μM for DRAK1, CK2a1, and CK2a2, respectively. This compound is valuable for studying autoimmune and inflammatory diseases [1].