E3330 (APX-3330) 是一种直接,口服有效的,选择性的 Ape-1 (无嘌呤/嘧啶内切酶 1)/Ref-1 (氧化还原因子 -1) 氧化还原的抑制剂。E3330 能抑制胰腺癌组织中 NF-κB、AP-1、HIF-1α 的活性。E3330 具有抗癌活性。 Information E3330 E3330 (APX-3330) is a potent and selective APE1(Ref-1) inhibitor, which suppressed NF-kappa B DNA-binding activity. Targets NF-κB ; APE1(Ref-1) In vitro 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. 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. Cell Research(from reference) Cell lines:PANC1 cells Concentrations:~30 μM Incubation Time:72 hours
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E3330
Dangerous GoodsCAS number:136164-66-4 molecular formula:C21H30O6
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Specs
| Chinese alias | - | ||
| English alias | E3330 | E-3330 | EX-A2212 | Undecanoic acid, 2-((4,5-dimethoxy-2-methyl-3,6-dioxo-1,4-cyclohexadien-1-yl)methylene)-, (E)- | (2E)-2-[(4,5-Dimethoxy-2-methyl-3,6-dioxo-1,4-cyclohexadien-1-yl)methylene]undecanoic acid | (2E)-2-[(4,5-Dimethoxy-2-methyl-3,6-d | ||
| CAS number | 136164-66-4 | molecular formula | C21H30O6 |
| molecular weight | 378.46 g/mol | Exact mass | 10mM in DMSO |
| PSA | 89.900 Ų | logp | 5.3 |
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Safety information
Hazard Statement:
H413: 可能对水生生物造成长期的有害影响
Statement of Preventive Measures:
P273: 避免释放到环境中。 P501: 将内容物/容器处理到。。。
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