| Name | Nrf2-IN-1 |
| Description | Nrf2-IN-1 is an nuclear factor-erythroid 2-related factor 2 (Nrf2) inhibitor. Nrf2-IN-1 is developed for the research of acute myeloid leukemia (AML). |
| In vitro | Nrf2-IN-1 (Compound 4f), that inhibited Nrf2 activity.?4f had a profound growth-inhibitory effect on three AML cell lines, THP-1, HL-60 and U937, and a similar anti-growth effect in a chick embryo model.?Moreover, flow cytometry of AML cells revealed increased apoptosis with 4f (10 μM) treatment for 48 h. The protein levels of cleaved caspase-3 and cleaved poly (ADP-ribose) polymerase were enhanced in all three AML cell types.?Furthermore, Nrf2 protein level was downregulated by 4f.?Upregulation of Nrf2 by tert-butylhydroquinone (tBHQ) or Nrf2 overexpression could ameliorate 4f-induced growth inhibition and apoptosis.?Treatment with 4f reduced both B-cell lymphoma-2 (Bcl-2) expression and Bcl-2/Bcl-2-associated X protein (Bax) ratio, which indicated that 4f induced apoptosis, at least in part, via mitochondrial-dependent signaling.?Therefore, as an Nrf2 inhibitor, the pyrazolyl hydroxamic acid derivative 4f may be a promising agent in AML therapy[1].
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| In vivo | Nrf2-IN-1 inhibits tumor growth in chicken eggs?via apoptosis?[1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 260 mg/mL (677.31 mM), Sonication is recommended.
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| Keywords | Nrf2-IN-1 | Nrf-2-IN-1 | Nrf2IN1 | Nrf2 IN 1 | Nrf2 | myeloid | leukemia | Keap1-Nrf2 | Inhibitor | inhibit | AML | Acute |
| Inhibitors Related | TBHQ | L-Cystine dihydrochloride | Mangiferin | Methyl 3,4-dihydroxybenzoate | Pyridoxine | Resveratrol | Luteolin | CDDO-Im | Curcumin | Ezetimibe | Oltipraz | Pyridoxine hydrochloride |
| Related Compound Libraries | Apoptosis Compound Library | Bioactive Compound Library | Anti-Obesity Compound Library | Hematonosis Compound Library | Antioxidant Compound Library | Inhibitor Library | NO PAINS Compound Library | PPI Inhibitor Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Oxidation-Reduction Compound Library | Transcription Factor-Targeted Compound Library |
United States
