E3330 is a potent and selective APE1 (Ref-1) inhibitor, which suppressed NF-kappa B DNA-binding activity.
E3330 细胞实验
Cell Line
Concentration
Treated Time
Description
References
XPA1 cells
20-30 µM
72 hours
E3330 significantly inhibits the growth of XPA1 cells
Mol Cancer Ther. 2008 Jul;7(7):2012-21.
PANC1 cells
20-30 µM
72 hours
E3330 significantly inhibits the growth of PANC1 cells
Mol Cancer Ther. 2008 Jul;7(7):2012-21.
Dental Papilla Cells (DPCs)
10 µM
1 day, 3 days, 6 days, 9 days
E3330 promotes the osteo/odontogenic differentiation capacity of DPCs by inhibiting the redox function of Ape1 and activating the canonical Wnt signaling pathway.
Sci Rep. 2015 Dec 7;5:17483.
HepG2 cells
10-100 µM
12 hours
E3330 synergistically increased cytotoxicity when combined with TRAIL, TNFα, and Fas ligand
World J Gastroenterol. 2005 Oct 28;11(40):6258-61.
SKHep1 cells
10-100 µM
12 hours
E3330 synergistically increased cytotoxicity when combined with TRAIL, TNFα, and Fas ligand
World J Gastroenterol. 2005 Oct 28;11(40):6258-61.
HLE cells
10-100 µM
12 hours
E3330 decreased NFκB levels in a dose-dependent manner in HLE cells stimulated by TNFα and TRAIL
World J Gastroenterol. 2005 Oct 28;11(40):6258-61.
Retinal vascular endothelial cells (RVECs)
10, 25, 50, 100 µM
2 days
Evaluated the effect of E3330 on RVEC proliferation, showing dose-dependent inhibition of RVEC growth
Antioxid Redox Signal. 2008 Nov;10(11):1853-67.
FLO-1 cells
40 µM
20 minutes
To investigate the effect of E3330 on ABS-induced E-cadherin cleavage and EMT, results showed that E3330 downregulated MMP14 and abrogated ABS-induced EMT.
Gut. 2023 Dec 7;73(1):47-62.
OE19 cells
40 µM
20 minutes
To investigate the effect of E3330 on ABS-induced E-cadherin cleavage and EMT, results showed that E3330 downregulated MMP14 and abrogated ABS-induced EMT.
Gut. 2023 Dec 7;73(1):47-62.
OE33 cells
40 µM
20 minutes
To investigate the effect of E3330 on ABS-induced E-cadherin cleavage and EMT, results showed that E3330 downregulated MMP14 and abrogated ABS-induced EMT.
Gut. 2023 Dec 7;73(1):47-62.
OE33 cells
100 µM
20 minutes
To investigate the inhibitory effect of E3330 on APE1 redox function, it was found that E3330 treatment led to a significant decrease in NRF2 transcriptional activity.
Redox Biol. 2021 Jul;43:101970.
FLO1 cells
100 µM
20 minutes
To investigate the inhibitory effect of E3330 on APE1 redox function, it was found that E3330 treatment led to a significant decrease in NRF2 transcriptional activity.
Redox Biol. 2021 Jul;43:101970.
CPB cells
100 µM
20 minutes
To investigate the inhibitory effect of E3330 on APE1 redox function, it was found that E3330 treatment led to a significant decrease in NRF2 transcriptional activity.
Redox Biol. 2021 Jul;43:101970.
Bone marrow-derived dendritic cells (BMDCs)
50 µM
24 hours
E3330 up-regulated IL-12 p35 and p40 gene expression but decreased IL-12 secretion
J Biol Chem. 2016 Nov 4;291(45):23672-23680.
Primate choroid endothelial cells (CECs)
25-100 µM
24 hours
E3330 dose-dependently suppressed CEC proliferation, migration, and tube formation without noticeable cell toxicity.
Invest Ophthalmol Vis Sci. 2014 Jun 26;55(7):4461-9.
3T3-L1 cells
50 µM
24 hours
E3330 inhibited the redox function of APE1/Ref-1, increasing the mRNA and protein levels of C/EBP-α, PPAR-γ, and aP2, promoting adipocyte differentiation.
Int J Mol Sci. 2023 Feb 7;24(4):3251.
Lin-negative bone marrow cells
0.5 µM
36~48 hours
E3330 treatment of Tet2-KO Lin-negative bone marrow cells inhibits IL-6 induced cell survival
Cell Stem Cell. 2018 Dec 6;23(6):833-849.e5.
Non-small cell lung cancer (NSCLC) cell lines
1.55 µM
4 days
To evaluate the sensitivity of NSCLC cell lines to 6-thio-dG, finding 73/77 cell lines were sensitive and 4/77 were resistant.
Mol Cancer Ther. 2017 Jul;16(7):1401-1411.
U937 monocyte-like cells
100 µM
4 hours
To investigate the effects of E3330 on inflammatory response in U937 cells, results showed that E3330 treatment reduced cell viability and expression of pro-inflammatory cytokines.
Front Cell Dev Biol. 2021 Sep 20;9:731588.
SKOV-3X ovarian cancer cells
80 µM (IC50)
40 hours
To evaluate the inhibitory effect of E3330 and its analogues on NF-κB activity, results showed that E3330 and its analogues could inhibit NF-κB activation in a dose-dependent manner
Overexpression of SLC43A3 in H1693 cells increased sensitivity to 6-thio-dG.
Mol Cancer Ther. 2017 Jul;16(7):1401-1411.
HCC4017 NSCLC cells
10 µM
4-7 days
Knockdown of SLC43A3 by siRNA resulted in resistance to 6-thio-dG in HCC4017 cells.
Mol Cancer Ther. 2017 Jul;16(7):1401-1411.
Panc-1 cells
87 µM (ED50)
48 hours
To evaluate the effect of E3330 on the proliferation of pancreatic cancer cells, results showed that E3330 significantly slowed cell growth in a dose-dependent manner.
Mol Cancer Ther. 2011 Sep;10(9):1698-708.
CD4+ T cells
50 µM
72 hours
E3330 had no significant effect on the induction of IFN-γ-producing T cells in the absence of APCs
J Biol Chem. 2016 Nov 4;291(45):23672-23680.
OT-II mouse splenocytes
50 µM
72 hours
E3330 significantly increased the induction of IFN-γ-producing OT-II T cells
J Biol Chem. 2016 Nov 4;291(45):23672-23680.
PaCa-2 cells
135 µM (ED50)
72 hours
To evaluate the effect of E3330 on the proliferation of pancreatic cancer cells, results showed that E3330 significantly slowed cell growth in a dose-dependent manner.
Mol Cancer Ther. 2011 Sep;10(9):1698-708.
HPNE cells
50 µM
72 hours
E3330 has no suppressive effects on the growth of HPNE cells
Mol Cancer Ther. 2008 Jul;7(7):2012-21.
Panc-1 cells
67.5 µM
8-12 hours
To evaluate the effect of E3330 on the adhesion ability of pancreatic cancer cells, results showed that E3330 significantly inhibited cell adhesion.
Mol Cancer Ther. 2011 Sep;10(9):1698-708.
PaCa-2 cells
67.5 µM
8-12 hours
To evaluate the effect of E3330 on the adhesion ability of pancreatic cancer cells, results showed that E3330 significantly inhibited cell adhesion.
Mol Cancer Ther. 2011 Sep;10(9):1698-708.
H2087 NSCLC cells
3 µM
9-18 days
Established acquired resistance model in H2087 cells, finding downregulation of SLC43A3 in resistant clones.
Mol Cancer Ther. 2017 Jul;16(7):1401-1411.
OE33 cells
100 µM
Overnight
E3330 inhibited ABS-mediated increase in YAP1 protein levels
J Exp Clin Cancer Res. 2022 Sep 1;41(1):264.
FLO-1 cells
100 µM
Overnight
E3330 inhibited ABS-mediated increase in YAP1 protein levels
J Exp Clin Cancer Res. 2022 Sep 1;41(1):264.
Hey-C2 ovarian cancer cells
38.9 µM (LD50)
To evaluate the effect of E3330 and its analogues on cell growth, results showed that E3330 and its analogues could inhibit cell growth
To investigate the effect of E3330 on PDX tumor growth and invasion, results showed that E3330 suppressed tumor growth and invasion and restored E-cadherin expression levels.
Gut. 2023 Dec 7;73(1):47-62.
Mice
Tet2-KO mice
Oral gavage
20 mg/kg
Daily for 12 weeks
Long-term treatment of juvenile Tet2-KO mice with E3330 rescues multiple phenotypic defects associated with Tet2 deficiency
E3330 significantly suppressed laser-induced CNV development without causing tissue toxicity.
Invest Ophthalmol Vis Sci. 2014 Jun 26;55(7):4461-9.
C57BL/6J mice
Laser-induced choroidal neovascularization (CNV) model
Intravitreal injection
200 μM (1 μL )
Single injection, lasted for 2 weeks
A single intravitreal injection of E3330 significantly reduced the area of laser-induced CNV lesions, indicating that E3330 attenuated damage to the RPE-Bruch's membrane complex in vivo.
Redox Biol. 2014 Feb 21;2:485-94
NOD/SCID mice
Pancreatic cancer xenograft model
Intraperitoneal injection
25 mg/kg
Twice daily for 10-12 days
To evaluate the effect of E3330 on tumor growth in pancreatic cancer xenograft models in vivo, results showed that E3330 significantly inhibited tumor growth.
搜索
