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PKD inhibitor CRT5

Chemical Structure : PKD inhibitor CRT5

CAS No.: 1034297-58-9

PKD inhibitor CRT5 (CRT5, CRT0066051)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 454.574
分子式 C28H30N4O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-[6-amino-5-(6-ethoxy-2-naphthalenyl)-3-pyridinyl]-N-[2-(dimethylamino)ethyl]-benzamide

参考文献

1. Evans IM, et al. Biochem J. 2010 Aug 1;429(3):565-72.

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