Nrf2-IN-1

SKU: orb1219387

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).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].Nrf2-IN-1 inhibits tumor growth in chicken eggs via apoptosis.

Key Properties

• CAS Number: 1610022-76-8
• MW: 383.87
• Purity: >98% (HPLC)
• Formula: C₂₁H₂₂ClN₃O₂
• SMILES: O=C(NO)C1=CC(C2=CC=C(Cl)C=C2)=NN1CC3=CC=C(C(C)(C)C)C=C3
• Target: Keap1-Nrf2
• Solubility: DMSO:260 mg/mL (677.31 mM; Need ultrasonic)

Bioactivity

• In Vitro:
  Cell Viability Assay Cell line: THP-1 cells, HL-60 cells, U937 cells. Concentration: 1 μM, 5 μM, 10 μM, 20 μM. Incubation time: 48 hours. Result: Inhibited growth of the three AML cell types at 5 μM, 10 μM or 20 μM for 48 hours. Apoptosis Analysis Cell line: THP-1 cells, HL-60 cells, U937 cells. Concentration: 5 μM, 10 μM. Incubation time: 48 hours. Result: Induced apoptosis in AML cells in vitro. Western blot analysis. Cell line: THP-1 cells, HL-60 cells, U937 cells. Concentration: 5 μM, 10 μM. Incubation time: 48 hours. Result: Triggered caspase-dependent apoptotic signaling in AML cells.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Keap1-Nrf2