CRT0066101

CRT0066101 is a potent, selective small molecule inhibitor of protein kinase D (PKD), targeting all three PKD isoforms (PKD1, PKD2, PKD3). It is orally bioavailable and has demonstrated efficacy in preclinical models of multiple cancers—including pancreatic, breast, colorectal, and bladder cancer—by blocking tumor growth, inducing apoptosis, inhibiting proliferation, and abrogating NF-κB-dependent pro-survival signals[1][2][3]. It also suppresses inflammatory cytokine production through inhibition of the TLR4/MyD88 pathway, NLRP3 inflammasome activation, and downstream signaling involving NF-κB, ERK, and JNK phosphorylation[1]. CRT0066101 has shown significant anti-inflammatory actions in models of acute lung injury. The drug is mainly studied for experimental and translational cancer therapy, with ongoing research into its mechanisms and further potential clinical applications.

Other names

CRT0066101CRT-0066101CRT 0066101