product name E3330
Description: E3330 is a potent and selective APE1(Ref-1) inhibitor, which suppressed NF-kappa B DNA-binding activity. E3330 affects hemangioblast development in vitro via inhibition of Ape1 redox activity. E3330 inhibits the growth of human pancreatic cancer cell line PANC1, XPA1, MIAPACA, BxPC3, and PK9. E3330 also promotes exit of cell cycle in PANC1 cells, inhibits the DNA-Binding activity of HIF-1α and migration of pancreatic cancer cells.
References: Blood. 2007 Mar 1;109(5):1917-22; J Pharmacol Exp Ther. 1992 Jul;262(1):145-50.
378.46
Formula
C21H30O6
CAS No.
136164-66-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 75 mg/mL (198.2 mM)
Water: 75 mg/mL (198.2 mM)
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19411760
| In Vitro |
In vitro activity: E3330 affects hemangioblast development in vitro via inhibition of Ape1 redox activity. E3330 inhibits the growth of human pancreatic cancer cell line PANC1, XPA1, MIAPACA, BxPC3, and PK9. E3330 also promotes exit of cell cycle in PANC1 cells, inhibits the DNA-Binding activity of HIF-1α and migration of pancreatic cancer cells. In JHH6 cells, E3330 prevents the functional activation of NF-κB via the alteration of APE1 subcellular trafficking and reduces IL-6 and IL-8 expression induced by TNF-α and FAs accumulation through blockage of the redox-mediated activation of NF-κB. Kinase Assay: Cell Assay: PANC1 cells are placed in one well of a 12-well plate and treated with 5 to 30 μM E3330. After a 24, 48, and 72 h of culture, the cells are washed with PBS and stained with trypan blue, and cell viability is examined by counting the live cell numbers. |
|---|---|
| In Vivo | In mice with endotoxin-mediated hepatitis, E3330 (300 mg/kg, p.o.) attenuates the elevation of plasma tumor necrosis factor activity and protectes mice from liver injury. In Rat model, E3330 (100 mg/kg, p.o.) also protectes rats from severe liver injury induced with endotoxin plus galactosamine. |
| Animal model | Mice with endotoxin-mediated hepatitis |
| Formulation & Dosage | Suspended in 0.5% methylcellulose solution; 300 mg/kg; p.o. |
| References | Blood. 2007 Mar 1;109(5):1917-22; J Pharmacol Exp Ther. 1992 Jul;262(1):145-50. |
