Protein Kinase D inhibitor CRT5 (CRT0066051) Small Molecule (Tool Compound)

CRT5, a novel specific PKD inhibitor, will greatly facilitate the study of the role of PKD signalling mechanisms in angiogenesis.

Contributors

Inventor Institute
Mark Charles Cancer Research Technology
Cat. #: 152544
Tool sub type: Inhibitor
Research Fields: Cell signaling and signal transduction
Application: PLEASE NOTE THAT THIS COMPOUND IS TOXIC IN VIVO. CRT5 blocks phosphorylation of PKD1 on Ser916 and PKD2 on Ser876, but does not affect PKC-dependent PKD phosphorylation or PKD autophosphorylation.1 It also decreases VEGF-induced endothelial migration, proliferation, and tubulogenesis.
Purpose: Inhibitor
Product description: CRT5, a novel specific PKD inhibitor, will greatly facilitate the study of the role of PKD signalling mechanisms in angiogenesis. To better understand the role of PKD in VEGF-mediated endothelial function, we characterized the effects of a novel pyrazine benzamide PKD inhibitor CRT5 in HUVECs (human umbilical vein endothelial cells). The activity of the isoforms PKD1 and PKD2 were blocked by this inhibitor as indicated by reduced phosphorylation, at Ser916 and Ser876 respectively, after VEGF …
Selectivity: It has little effect on a panel of additional kinases when given at 1 ÂľM.
Primary target: Protein Kinase D (PDK)
Storage conditions: Ambient in DMSO (12mM)
Shipping conditions: Dry Ice
Solubility: DMSO
References:

Sharlow et al. 2011. PLoS One. 6(10):e25134. PMID: 21998636. Evans et al. 2010. Biochem J. 429(3):565-72. PMID: 20497126.

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