CRT5 is a novel and specific PKD inhibitor . PKDs (Protein kinase Ds) are DAG (diacylglycerol)-stimulated serine/threonine protein kinases . Three known PKD isoforms have been identified: PKD1–PKD3. PKD acted as an mediator implicated in diverse cellular functions, including proliferation, cellular trafficking, survival and regulation of transcription . In vitro: The non-linear regression analysis revealed that LD50 value of CRT5 was 17 μM. The biochemical IC50 value of CRT5 for PKD1, PKD2 and PKD3 were 1, 2 and 1.5 nM, respectively . CRT5 (1 μM) completely inhibited PKD1 and PKD2, but showed little inhibitory effect on the PKC isoforms. CRT5 significantly reduced VEGF-induced phosphorylation of HSP27 at the position Ser82. CRT5 significantly reduced the migratory response towards VEGF by 42–51%. CRT5 decreased the proliferation of control cells not treated with VEGF to a less extent. VEGF increased HUVEC tubule formation in a collagen-based assay. CRT5 markedly inhibited VEGF-induced tubulogenesis .

Product information

CAS Number: 1034297-58-9

Molecular Weight: 454.56

Formula: C28H30N4O2

Chemical Name: 3-[6-amino-5-(6-ethoxynaphthalen-2-yl)pyridin-3-yl]-N-[2-(dimethylamino)ethyl]benzamide

Smiles: CCOC1=CC2C=CC(=CC=2C=C1)C1=CC(=CN=C1N)C1=CC(=CC=C1)C(=O)NCCN(C)C

InChiKey: XBDRAUPLGHAFCU-UHFFFAOYSA-N

InChi: 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)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.