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Nrf2-IN-3

🥰Excellent
Catalog No. T78841Cas No. 6325-13-9

Nrf2-IN-3 is a mKEAP1-selective NRF2 inhibitor that selectively binds KEAP1 mutants and restores their NRF2 inhibitory function by repairing the disrupted KEAP1/NRF2 interaction, and selectively sensitizes cisplatin in xenografts of mouse mKEAP1 cancer cells.

Nrf2-IN-3

Nrf2-IN-3

🥰Excellent
Purity: 98.07%
Catalog No. T78841Cas No. 6325-13-9
Nrf2-IN-3 is a mKEAP1-selective NRF2 inhibitor that selectively binds KEAP1 mutants and restores their NRF2 inhibitory function by repairing the disrupted KEAP1/NRF2 interaction, and selectively sensitizes cisplatin in xenografts of mouse mKEAP1 cancer cells.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$56In StockIn Stock
5 mg$135In StockIn Stock
10 mg$218In StockIn Stock
25 mg$413In StockIn Stock
50 mg$569In StockIn Stock
100 mg$786-In Stock
200 mg$1,130-In Stock
1 mL x 10 mM (in DMSO)$148In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:98.07%
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Product Introduction

Bioactivity
Description
Nrf2-IN-3 is a mKEAP1-selective NRF2 inhibitor that selectively binds KEAP1 mutants and restores their NRF2 inhibitory function by repairing the disrupted KEAP1/NRF2 interaction, and selectively sensitizes cisplatin in xenografts of mouse mKEAP1 cancer cells.
In vitro
Nrf2-IN-3 is a small-molecule NRF2 inhibitor that selectively binds KEAP1 mutants and restores their NRF2-inhibitory function by repairing the disrupted KEAP1/NRF2 interactions. Nrf2-IN-3 substantially sensitizes KEAP1-mutated tumor cells to cisplatin and gefitinib, but does not do so for wild-type KEAP1 cells, and sensitizes KEAP1 G333C-mutated xenograft to cisplatin. [1]
Chemical Properties
Molecular Weight442.53
FormulaC22H26N4O4S
Cas No.6325-13-9
SmilesO=C(NN=CC=1C=CC=CC1O)CCCSCCCC(=O)NN=CC=2C=CC=CC2O
Storage & Solubility Information
Storagestore at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 100 mg/mL(225.97 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.2597 mL11.2987 mL22.5973 mL112.9867 mL
5 mM0.4519 mL2.2597 mL4.5195 mL22.5973 mL
10 mM0.2260 mL1.1299 mL2.2597 mL11.2987 mL
20 mM0.1130 mL0.5649 mL1.1299 mL5.6493 mL
50 mM0.0452 mL0.2260 mL0.4519 mL2.2597 mL
100 mM0.0226 mL0.1130 mL0.2260 mL1.1299 mL

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Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | 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 DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2OTargetMol | reagent mix well and clarify
For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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Keywords

NRF2
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