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Nrf2-IN-1

Name: Nrf2-IN-1
Brand: TargetMol
SKU: T12253
Price: 71 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T12253Cas No. 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).

Nrf2-IN-1

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Purity: 99.68%

Catalog No. T12253Cas No. 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).

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$71	In Stock	In Stock
5 mg	$172	In Stock	In Stock
10 mg	$242	In Stock	In Stock
25 mg	$403	In Stock	In Stock
50 mg	$565	In Stock	In Stock
100 mg	$788	In Stock	In Stock
200 mg	$1,090	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$317	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products. However, due to objective factors, there is a small probability that the synthesis may not be successful during the R&D process. We appreciate your understanding. If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

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Batch Information

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Purity:99.68%

Resource Download

COA HNMR LCMS

Product Introduction

Bioactivity

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].

Chemical Properties

Molecular Weight	383.87
Formula	C₂₁H₂₂ClN₃O₂
Cas No.	1610022-76-8
Smiles	CC(C)(C)c1ccc(Cn2nc(cc2C(=O)NO)-c2ccc(Cl)cc2)cc1
Relative Density.	1.23 g/cm3 (Predicted)
Color	White
Appearance	Solid

Storage & Solubility Information

Storage

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

Solubility Information

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

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (13.03 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.6050 mL	13.0252 mL	26.0505 mL	130.2524 mL
5 mM	0.5210 mL	2.6050 mL	5.2101 mL	26.0505 mL
10 mM	0.2605 mL	1.3025 mL	2.6050 mL	13.0252 mL
20 mM	0.1303 mL	0.6513 mL	1.3025 mL	6.5126 mL
50 mM	0.0521 mL	0.2605 mL	0.5210 mL	2.6050 mL
100 mM	0.0261 mL	0.1303 mL	0.2605 mL	1.3025 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc