Cat. #152544
Protein Kinase D inhibitor CRT5 (CRT0066051) Small Molecule (Tool Compound)
Cat. #: 152544
Sub-type: Inhibitor
Availability: Please enquire for quantities and pricing
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.
This fee is applicable only for non-profit organisations. If you are a for-profit organisation or a researcher working on commercially-sponsored academic research, you will need to contact our licensing team for a commercial use license.
Contributor
Inventor: Mark Charles
Institute: Cancer Research Technology
Tool Details
*FOR RESEARCH USE ONLY (for other uses, please contact the licensing team)
- Tool name: Protein Kinase D inhibitor CRT5 (CRT0066051) Small Molecule (Tool Compound)
- Research fields: Cell signaling and signal transduction
- Molecular formula: C28H30N4O2
- Tool sub type: Inhibitor
- Primary target: Protein Kinase D (PDK)
- 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 ...
- 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
- Selectivity: It has little effect on a panel of additional kinases when given at 1 ÂľM.
- Solubility: DMSO
Handling
- Storage conditions: Ambient in DMSO (12mM)
- Shipping conditions: Dry Ice
Target Details
- Primary target: Protein Kinase D (PDK)
- Ic50: IC50s = 1, 2, and 1.5 nM for PKD1, PKD2, and PKD3, respectively
Application Details
- 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.
Related Tools
- Related tools: Protein Kinase D inhibitor CRT0066101 Small Molecule (Tool Compound)
References
- Sharlow et al. 2011. PLoS One. 6(10):e25134. PMID: 21998636. Evans et al. 2010. Biochem J. 429(3):565-72. PMID: 20497126.
