crt 0066101

CRT0066101 dihydrochloride 是一种选择性PKD 有效抑制剂，对PKD1、2和3的IC50值分别为1、2.5和2 nM。

PKD-IN-1 是 PKD 的抑制剂。

CRT0066101是一种有效的具有口服活性的PKD抑制剂，对PKD1、PKD2和PKD3的IC50值分别为1 nM、2.5 nM和2 nM。CRT0066101也是一种有效的PIM2抑制剂，IC50约为135.7 nM。CRT0066101具有抗癌作用。

Protein kinase D (PKD), a serine threonine protein kinase activated by diacylglycerol downstream of PKC signaling, has three human isoforms that modulate cell proliferation, survival, invasion, and protein transport. CRT0066101 acts as an inhibitor of these three PKD isoforms, with IC50 values of 1, 2.5, and 2 nM for PKD1, PKD2, and PKD3, respectively. It demonstrates selectivity for PKD over a range of more than 90 protein kinases, including PKCα, PKBα, MEK, ERK, c-Raf, c-Src, and c-Abl. This specificity allows CRT0066101 to inhibit cell proliferation, induce apoptosis, and notably reduce the viability of pancreatic cancer cells both in vitro and in vivo.

PKD-IN-1 dihydrochloride 是 PKD 的抑制剂。