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Protein kinase D (PKD) is a serine/threonine protein kinase that is activated by diacylglycerol, commonly downstream of PKC signaling. The three human PKD isoforms target a variety of proteins to alter cell proliferation, survival, invasion, and protein transport. CRT0066101 is an inhibitor of all three PKD isoforms (IC50s = 1, 2.5, and 2 nM for PKD1, PKD2, and PKD3, respectively).1 It exhibits selectivity for PKD against a panel of >90 protein kinases, including PKCα, PKBα, MEK, ERK, c-Raf, c-Src, and c-Abl.1 It can block cell proliferation, induce apoptosis, and reduce the viability of pancreatic cancer cells both in vitro and in vivo.1 | [References]
1. Harikumar, K.B., Kunnumakkara, A.B., Ochi, N., et al. A novel small-molecule inhibitor of protein kinase D blocks pancreatic cancer growth in vitro and in vivo Mol. Cancer Ther. 9(5),1136-1146(2010). |
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Company Name: |
Key Organics Ltd.
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+44 (0) 1840-212137 |
Website: |
www.keyorganics.net |
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