- Inhibitory Selectivity
|Catalog No.||Product Name||Solubility(25°C)|
|S8790||ML385||<1 mg/mL||74 mg/mL||<1 mg/mL|
|S1848||Curcumin||<1 mg/mL||73 mg/mL||<1 mg/mL|
|S7864||Oltipraz||<1 mg/mL||39 mg/mL||<1 mg/mL|
|S3784||Obacunone||-1 mg/mL||90 mg/mL||-1 mg/mL|
|S5929||4-Octyl Itaconate||<1 mg/mL||48 mg/mL||48 mg/mL|
|S4990||TBHQ||-1 mg/mL||33 mg/mL||-1 mg/mL|
- Nrf2 Inhibitors (8)
- New Nrf2 Products
|Catalog No.||Information||Product Use Citations||Product Validations|
ML385 is a novel and specific NRF2 inhibitor with an IC50 of 1.9 μM. It inhibits the downstream target gene expression of NRF2.
Curcumin is the principal curcuminoid of the popular Indian spice turmeric, which is a member of the ginger family (Zingiberaceae). It is an inhibitor of p300 histone acetylatransferase（IC50~25 μM） and Histone deacetylase; activates Nrf2 pathway and supresses the activation of transcription factor NF-κB.
Effect of NC1, NC1-CUR, NC2 and NC2-CUR on SH-SY5Y cell viability. The cells were treated for 24 h with different dilutions(1:1, 1:2 and 1:4) of empty nanocapsules (NC1 and NC2) and nanocapsules containing curcumin (NC1-CUR and NC2-CUR) followed by measurement of cell viability by MTT reduction assay (panel A) and cell toxicity by LDH release assay (panel B). Data after normalization to vehicle-treated cells (100%, MTT assay) or to total LDH release (TritonX100-treated cells, 100%) are presented as a mean±SEM from 3-8 independent experiments with five replicates. *p < 0.05, **p < 0.01 and ***p<0.001 versus vehicle-treated cells; &&&p<0.001 NC1 versus NC1-CUR.
Oltipraz is a potent Nrf2 activator and a potent inducer of Phase II detoxification enzymes, most notably glutathione-S-transferase (GST). Phase 3.
Effects of p21 depletion and Nrf2 activation on dexamethasone-induced apoptosis in MC3T3-E1 cells. Cells were transfected with control siRNA or p21 siRNA. Subsequently, transfected cells were pre incubated with oltipraz (20 μM) for 1 h, and then co-incubated with 1 μM dexamethasone for 24 h. Apoptosis was measured by flow cytometry, followed by Annexin V-FITC/PI double staining. Effects of p21 depletion and Nrf2 activation on dexamethasone-induced apoptosis in MC3T3-E1 cells. Cells were transfected with control siRNA or p21 siRNA. Subsequently, transfected cells were pre-incubated with oltipraz (20 μM) for 1 h, and then co-incubated with 1 μM dexamethasone for 24 h. Apoptosis was measured by flow cytometry, followed by Annexin V-FITC/PI double staining.
Sulforaphane is a naturally occurring isothiocyanate derived from the consumption of cruciferous vegetables, such as broccoli, cabbage, and kale. It is an inducer of Nrf2.
Obacunone, a natural compound present in citrus fruits, has been demonstrated for various biological activities including anti-cancer and anti-inflammatory properties. It significantly inhibits aromatase activity in an in vitro enzyme assay with an IC50 value of 28.04 μM; also a novel activator of Nrf2.
4-Octyl Itaconate activates Nrf2 signaling to inhibit the production of pro-inflammatory cytokines in human macrophages and systemic lupus erythematosus (SLE) patient-derived PBMCs.
Tert-butylhydroquinone (TBHQ) is an antioxidant compound which is used to prevent lipid peroxidation and shows multiple cytoprotective actions. It is an activator of Nrf2.
Diethylmaleate is the diethyl ester of maleic acid and a glutathione-depleting compound that inhibits NF-kB.