Nrf2-IN-1

SKU: orb1309323

Description

Nrf2-IN-1 is a small molecule inhibitor of the transcription factor Nrf2, developed for research into acute myeloid leukemia (AML). It is utilized in both in vitro and in vivo experimental models to investigate the role of Nrf2 signaling in cancer cell proliferation and chemoresistance.

Research Area

Immunology & Inflammation

Key Properties

• CAS Number: 1610022-76-8
• MW: 383.87
• Purity: 99.68%
• Formula: C₂₁H₂₂ClN₃O₂
• SMILES: CC(C)(C)c1ccc(Cn2nc(cc2C(=O)NO)-c2ccc(Cl)cc2)cc1
• Target: Nrf2
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (13.03 mM);DMSO:260 mg/mL (677.31 mM)

Bioactivity

• In Vivo:
  Nrf2-IN-1 inhibits tumor growth in chicken eggs via apoptosis .
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AML, Acute, Keap1-Nrf2, Nrf2, Nrf2 IN 1, Nrf2IN1, Nrf-2-IN-1, Nrf2-IN-1, inhibit, myeloid, leukemia, Inhibitor

Compound Identifiers

PubChem CID

76900951