CRT5

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. CRT5 is a pyrazine benzamide that prevents activation of all three isoforms of PKD in endothelial cells treated with VEGF (IC50s = 1, 2, and 1.5 nM for PKD1, PKD2, and PKD3, respectively). It has little effect on a panel of additional kinases when given at 1 µM. CRT5 blocks phosphorylation of PKD1 on Ser916 and PKD2 on Ser876, but does not affect PKC-dependent PKD phosphorylation or PKD autophosphorylation. It also decreases VEGF-induced endothelial migration, proliferation, and tubulogenesis.Formal Name: 3-[6-amino-5-(6-ethoxy-2-naphthalenyl)-3-pyridinyl]-N-[2-(dimethylamino)ethyl]-benzamide. CAS Number: 1034297-58-9. Synonyms: CRT0066051. Molecular Formula: C28H30N4O2. Formula Weight: 454.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 0.25 mg/ml, DMF:PBS(pH7.2) (1:2): 0.33 mg/ml, DMSO: 2.5 mg/ml. lambdamax: 234, 333 nm. SMILES: CCOC1=CC=C2C(C=CC(C3=CC(C4=CC(C(NCCN(C)C)=O)=CC=C4)=CN=C3N)=C2)=C1. InChi Code: InChI=1S/C28H30N4O2/c1-4-34-25-11-10-20-14-22(9-8-21(20)16-25)26-17-24(18-31-27(26)29)19-6-5-7-23(15-19)28(33)30-12-13-32(2)3/h5-11,14-18H,4,12-13H2,1-3H3,(H2,29,31)(H,30,33). InChi Key: XBDRAUPLGHAFCU-UHFFFAOYSA-N.