Product Name :
CRT5
Description:
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 .
CAS:
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)
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.{{Fucoxanthin} web|{Fucoxanthin} Anti-infection|{Fucoxanthin} Protocol|{Fucoxanthin} Formula|{Fucoxanthin} custom synthesis|{Fucoxanthin} Cancer}
Shelf Life:
≥12 months if stored properly.{{Sildenafil} medchemexpress|{Sildenafil} Apoptosis|{Sildenafil} Technical Information|{Sildenafil} In Vivo|{Sildenafil} supplier|{Sildenafil} Epigenetics}
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
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.PMID:23008002 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.|
