Nrf2-IN-1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Nrf2-IN-1 是一种核因子-红细胞 2 相关因子 2 (Nrf2) 抑制剂。 Nrf2-IN-1 是为研究急性髓系白血病 (AML) 而开发的。Nrf2-IN-1（化合物 4f）可抑制 Nrf2 活性。 4f 对三种 AML 细胞系 THP-1、HL-60 和 U937 具有显着的生长抑制作用，并且在鸡胚模型中具有类似的抗生长作用。

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.

——

——

Nuclear Receptor/Transcription Factor

Keap1-Nrf2

Nrf2

——

——

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

——

(-20℃)

With Ice Pack

≥ 2 years