Nrf2-IN-1

产品编号 T12253Cas号 1610022-76-8

Nrf2-IN-1 是 Nrf2抑制剂，可用于研究急性髓性白血病药物。

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产品编号 T12253Cas号 1610022-76-8

Nrf2-IN-1 是 Nrf2抑制剂，可用于研究急性髓性白血病药物。

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生物活性

产品描述	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).
体外活性	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].
体内活性	Nrf2-IN-1 inhibits tumor growth in chicken eggs?via apoptosis?[1].

化学信息

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

溶解度信息

DMSO: 260 mg/mL (677.31 mM), Sonication is recommended.

溶液配制表

DMSO