pkd-2

N-Cyclohexyl-4-[1-(1-piperazinyl)-2,6-naphthyridin-3-yl]-2-pyridinamine is a novel 2,6-naphthyridine identified by high throughput screen (HTS) as a dual protein kinase C/D (PKC/PKD) inhibitor[1].

CRT0066101 dihydrochloride is an effective and selective PKD inhibitor (IC50s: 1, 2.5 and 2 nM for PKD1, 2, and 3).

PROTAC EED degrader-2 is a PROTAC targeting EED (pKD of 9.27) and an inhibitor of polycomb repressive complex 2 (PRC2) with a pIC50 of 8.11.

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.

kb NB 142-70 is a selective protein kinase D (PKD) inhibitor with IC50 values of 28.3 nM, 58.7 nM, and 53.2 nM for PKD1, PKD2, and PKD3 respectively.

CRT5, a pyrazine benzamide, is a potent and selective PKD inhibitor. It inhibits VEGF-induced phosphorylation of three PKD substrates (IC50s = 1, 2, and 1.5 nM for PKD1, PKD2, and PKD3, respectively), histone deacetylase 5, CREB (cAMP-response-element-binding protein), and HSP27 (heat-shock protein 27) at Ser82. Additionally, CRT5 decreases VEGF-induced endothelial migration, proliferation, and tubulogenesis[1].

PROTAC EED degrader-1, a PROTAC targeting EED (pKD = 9.02), is an inhibitor of polycomb repressive complex 2 (PRC2) with a pIC50 of 8.17.

ANQ-11125 TFA is a potent, selective motilin antagonist, exhibiting a pKd of 8.24. It effectively inhibits motilide-induced contractions in rabbit models, as demonstrated in vitro [1] [2].