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    PKD (Protein kinase D) is an evolutionarily conserved protein kinase family with structural, enzymological, and regulatory properties different from the PKC family members. Signaling through PKD is induced by a remarkable number of stimuli, including G-protein-coupled receptor agonists and polypeptide growth factors.




    PKD (Protein kinase D) family of serine/threonine protein kinases has three members: PKD1, PKD2, PKD3. PKD1, the most studied member of the family, is increasingly implicated in the regulation of a complex array of fundamental biological processes, including signal transduction, cell proliferation and differentiation, membrane trafficking, secretion, immune regulation, cardiac hypertrophy and contraction, angiogenesis, and cancer. PKD mediates such a diverse array of normal and abnormal biological functions via dynamic changes in its spatial and temporal localization, combined with its distinct substrate specificity.

Cat. No. Product Name CAS No. Information
GY02899

CRT0066101 dihydrochloride

1883545-60-5

A potent, specific, orally active pan-PKD (protein kinase D) inhibitor with biochemical IC50 of 1, 2.5 and 2 nM for PKD1, 2, and 3 respectively; shows selectivity against a panel of > 90 protein kinases including PKCα/PKBα/MEK/ERK/c-Raf/c-Src/c-Abl; reduces bromodeoxyuridine incorporation, increases apoptosis, blocks neurotensin-induced PKD1/2 activation and reduces neurotensin-induced, PKD-mediated Hsp27 phosphorylation, attenuated PKD1-mediated NF-kappaB activation in pancreatic cancer cells; potently blocks tumor growth in vivo.

GY02277

kb-NB-142-70

1233533-04-4

kb-NB142-70 is a potent and selective PKD inhibitor with IC50 of 28.3 nM; displays 10-fold increase in the in vitro PKD1 inhibitory potency versus CID755673; inhibits PC-3, PANC-1, CFPAC-1 cellular growth with IC50 of 5-30 uM.

GY01947

CID755673

521937-07-5

The first potent and selective cell-active pan-PKD inhibitor with IC50s of 182/280/227 nM for PKD1/2/3 respectively; exhibits selectivity for PKD1 versus AKT, PLK1, CAK, CAMKIIα and three PKC isoforms; blockes phorbol ester-induced endogenous PKD1 activation in LNCaP cells and inhibits prostate cancer cell proliferation, cell migration and invasion.

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