Nrf2-IN-1

Research use only, not for human use.

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.

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.

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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Nuclear Receptor/Transcription Factor

Keap1-Nrf2

Nrf2

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1610022-76-8

383.87

C21H22ClN3O2

>98% (HPLC)

DMSO:260 mg/mL (677.31 mM; Need ultrasonic)

O=C(NO)C1=CC(C2=CC=C(Cl)C=C2)=NN1CC3=CC=C(C(C)(C)C)C=C3

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(-20℃)

With Ice Pack

≥ 2 years