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Chemical Structure : PKD inhibitor CRT5
CAS No.: 1034297-58-9
Catalog No.: PC-38466Not For Human Use, Lab Use Only.
CRT5 (PKD inhibitor CRT5) is a potent, selective pyrazine benzamide inhibitor of PKD (protein kinase D), inhibits peptide substrate phosphorylation with IC50 of 1, 2 and 1.5 nM for PKD1, PKD2 and PKD3, respectively.
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CRT5 (PKD inhibitor CRT5) is a potent, selective pyrazine benzamide inhibitor of PKD (protein kinase D), inhibits peptide substrate phosphorylation with IC50 of 1, 2 and 1.5 nM for PKD1, PKD2 and PKD3, respectively.
CRT5 (PKD inhibitor CRT5) displays little inhibitory effect on any of the PKC isoforms tested at 1 uM, as well as a panel of other serine/threonine and tyrosine protein kinases.
CRT5 (5 uM treatment) inhibited VEGF-induced phosphorylation of PKD1 at Ser916 and PKD2 at the corresponding site Ser876 in HUVECs, with no effect on PKD phosphorylation at Ser744/Ser748.
CRT5 (PKD inhibitor CRT5) significantly reduced VEGF-induced HSP27 Ser82 phosphorylation in vitro, as well as VEGF-induced CREB phosphorylation.
CRT5 (PKD inhibitor CRT5) also strongly inhibited VEGF-induced HDAC5 phosphorylation at 5 uM.
CRT5 (PKD inhibitor CRT5) markedly inhibited VEGF-induced migration, proliferation and in vitro angiogenesis.
| M.Wt | 454.574 | |
| Formula | C28H30N4O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
3-[6-amino-5-(6-ethoxy-2-naphthalenyl)-3-pyridinyl]-N-[2-(dimethylamino)ethyl]-benzamide |
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1. Evans IM, et al. Biochem J. 2010 Aug 1;429(3):565-72.
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