2. NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  3. Keap1-Nrf2 Reactive Oxygen Species
  4. Keap1-Nrf2-IN-14

Keap1-Nrf2-IN-14 (compound 20c) is a KEAP1-NRF2 inhibitor that effectively disrupts the KEAP1-NRF2 interaction (IC50=75 nM) with a Kd value of 24 nM for KEAP1. Keap1-Nrf2-IN-14 induces the expression of NRF2 target genes and enhances the downstream antioxidant and anti-inflammatory activities. Keap1-Nrf2-IN-14 can be used in the study of oxidative stress-related inflammation.

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Keap1-Nrf2-IN-14 Chemical Structure

Keap1-Nrf2-IN-14 Chemical Structure

CAS No. : 1928782-31-3

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Based on 1 publication(s) in Google Scholar

Keap1-Nrf2-IN-14 Related Antibodies

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1 Publications Citing Use of MCE Keap1-Nrf2-IN-14

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Description

Keap1-Nrf2-IN-14 (compound 20c) is a KEAP1-NRF2 inhibitor that effectively disrupts the KEAP1-NRF2 interaction (IC50=75 nM) with a Kd value of 24 nM for KEAP1. Keap1-Nrf2-IN-14 induces the expression of NRF2 target genes and enhances the downstream antioxidant and anti-inflammatory activities. Keap1-Nrf2-IN-14 can be used in the study of oxidative stress-related inflammation[1].

IC50 & Target[1]

KEAP1-NRF2

75 nM (IC50)

In Vitro

Keap1-Nrf2-IN-14 effectively activated NRF2-ARE regulated cytoprotective defense system in both concentration- and time- dependent manner in RAW264.7 cells[1].
Keap1-Nrf2-IN-14 (1, 10 µM; 12 h) enhanced the antioxidant capacity in macrophage RAW 264.7 cells[1].
Keap1-Nrf2-IN-14 (1, 10 µM; 12 h) attenuates LPS-induced production of inflammation factors in RAW 264.7 cells[1].
Keap1-Nrf2-IN-14 shows high metabolic stability (in co-incubation with rat liver microsomes with half-life of 10.5 h), and have no CYP inhibition on 1A2, 2C9, 2C19, 2D6 and 3A4 when at 10 µM.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Keap1-Nrf2-IN-14 Related Antibodies

Cell Viability Assay[1]

Cell Line: RAW264.7 cells (LPS-stimulated)
Concentration: 10 µM
Incubation Time: 12 h
Result: Significantly reduced ROS generation to nearly normal level.

Cell Viability Assay[1]

Cell Line: RAW264.7 cells (LPS-stimulated)
Concentration: 1, 10 µM
Incubation Time: 12 h
Result: Notably restored the SOD and GSH-Px levels.
Markedly attenuated the levels of the inflammatory factors IL-1b, IL-6, TNF-a and NO (induced by LPS) in a concentration-dependent manner, and when at 10 µM, almost reduced these cytokines to the basal level.

RT-PCR[1]

Cell Line: RAW264.7 cells
Concentration: 0.1, 1, 5, 10 µM
Incubation Time: 12 h
Result: Strongly increased the transcription of NRF2 regulated genes in RAW264.7 cells at a concentration-dependent manner.

Western Blot Analysis[1]

Cell Line: RAW264.7 cells
Concentration: 10 µM
Incubation Time: 1, 2, 4, 8, 16, 24 h
Result: Led to nuclear translocation of NRF2 began within 2 h, maximized at 8 h and subsequently declined after 16 h.
Induced NRF2, HO-1, NQO-1 and GCLM protein expression in a time- dependent manner.
In Vivo

Keap1-Nrf2-IN-14 (10 mg/kg; i.p.; single daily for 3 days) reduces the LPS-induced production of the proinflammatory factors in vivo[1].
Keap1-Nrf2-IN-14 (1 mg/kg; i.v.; single) shows half-life of 1.72 h in vivo[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female C57BL/6 mice (18-22 g; LPS-induced inflammation model)[1].
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; single daily for 3 days.
Result: Diminished LPS-induced inflammatory response in vivo.
Animal Model: Female C57BL/6 mice (18-22 g; LPS-induced inflammation model)[1].
Dosage: 1 mg/kg
Administration: Intravenous injection; single.
Result: Led to half-life of 1.72 h.
Molecular Weight

563.62

Formula

C30H29NO8S
CAS No.
Appearance

Solid

Color

Gray to brown

SMILES

O=C(O)C(OC1=C2C=CC=CC2=C(N(CC(O)=O)S(=O)(C3=C(C)C=C(C)C=C3C)=O)C=C1)C4=CC=C(OC)C=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (177.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7742 mL 8.8712 mL 17.7425 mL
5 mM 0.3548 mL 1.7742 mL 3.5485 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.44 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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+
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7742 mL 8.8712 mL 17.7425 mL 44.3561 mL
5 mM 0.3548 mL 1.7742 mL 3.5485 mL 8.8712 mL
10 mM 0.1774 mL 0.8871 mL 1.7742 mL 4.4356 mL
15 mM 0.1183 mL 0.5914 mL 1.1828 mL 2.9571 mL
20 mM 0.0887 mL 0.4436 mL 0.8871 mL 2.2178 mL
25 mM 0.0710 mL 0.3548 mL 0.7097 mL 1.7742 mL
30 mM 0.0591 mL 0.2957 mL 0.5914 mL 1.4785 mL
40 mM 0.0444 mL 0.2218 mL 0.4436 mL 1.1089 mL
50 mM 0.0355 mL 0.1774 mL 0.3548 mL 0.8871 mL
60 mM 0.0296 mL 0.1479 mL 0.2957 mL 0.7393 mL
80 mM 0.0222 mL 0.1109 mL 0.2218 mL 0.5545 mL
100 mM 0.0177 mL 0.0887 mL 0.1774 mL 0.4436 mL
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Keap1-Nrf2-IN-14 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Keap1-Nrf2-IN-141928782-31-3Keap1-Nrf2Reactive Oxygen SpeciesROSinflammationRAW264.7Inhibitorinhibitorinhibit

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