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Nrf2-IN-1

Catalog No. T12253   CAS 1610022-76-8

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).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Nrf2-IN-1 Chemical Structure
Nrf2-IN-1, CAS 1610022-76-8
Pack Size Availability Price/USD Quantity
1 mg In stock $ 116.00
5 mg In stock $ 289.00
10 mg In stock $ 396.00
25 mg In stock $ 656.00
50 mg In stock $ 913.00
100 mg In stock $ 1,250.00
500 mg In stock $ 2,480.00
1 mL * 10 mM (in DMSO) In stock $ 317.00
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Purity: 99.68%
Purity: 99.36%
Purity: 95.00%
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Biological Description
Chemical Properties
Storage & Solubility Information
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).
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[1].
In vivo Nrf2-IN-1 inhibits tumor growth in chicken eggs?via apoptosis?[1].
Molecular Weight 383.87
Formula C21H22ClN3O2
CAS No. 1610022-76-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

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

TargetMolReferences and Literature

1. Zhang J, et al. Discovery of a novel Nrf2 inhibitor that induces apoptosis of human acute myeloid leukemia cells. Oncotarget. 2017 Jan 31;8(5):7625-7636.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library NF-κB Signaling Compound Library Ferroptosis Compound Library Antioxidant Compound Library Bioactive Compound Library Anti-Obesity Compound Library Hematonosis Compound Library Oxidation-Reduction Compound Library Immunology/Inflammation Compound Library Bioactive Compounds Library Max

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Keywords

Nrf2-IN-1 1610022-76-8 Immunology/Inflammation Others Nrf2 inhibit Acute leukemia AML myeloid Inhibitor Nrf2IN1 Keap1-Nrf2 Nrf-2-IN-1 Nrf2 IN 1 inhibitor

 

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