2. Autophagy NF-κB
  3. p62 Keap1-Nrf2
  4. K67

K67 is a selective the interaction between Keap1 and S349 phosphorylated p62 inhibitor, with an IC50 of 1.5 μM. K67 has a weaker inhibitory effect on the interaction between Keap1 and Nrf2 (IC50 is 6.2 μM). K67 competitively binds to the binding site of Keap1 with p-p62, blocking the abnormal activation of the p62-dependent Nrf2 pathway. K67 inhibits tumor cell proliferation and enhances the sensitivity of hepatocellular carcinoma (HCC) to chemotherapeutic drugs by restoring Keap1-mediated ubiquitination and degradation of Nrf2.

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K67 Chemical Structure

K67 Chemical Structure

CAS No. : 2046250-48-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

K67 Related Antibodies

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  • Purity & Documentation

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Description

K67 is a selective the interaction between Keap1 and S349 phosphorylated p62 inhibitor, with an IC50 of 1.5 μM. K67 has a weaker inhibitory effect on the interaction between Keap1 and Nrf2 (IC50 is 6.2 μM). K67 competitively binds to the binding site of Keap1 with p-p62, blocking the abnormal activation of the p62-dependent Nrf2 pathway. K67 inhibits tumor cell proliferation and enhances the sensitivity of hepatocellular carcinoma (HCC) to chemotherapeutic drugs by restoring Keap1-mediated ubiquitination and degradation of Nrf2[1][2].

In Vitro

K67 (50 μM; 24-72 h) significantly inhibits the proliferation of Huh1 cells and Huh7 cells expressing phospho-mimetic p62 in cell viability assays1.
K67 (50 μM; 12-48 h) inhibits the expression of Nrf2 target genes in Huh1 cells1.
K67 (50 μM; 4-36 h respectively) significantly reduces the content of Nrf2 in the nucleus and cytoplasm of Huh1 cells and Keap1 accumulates in a time-dependent manner1.
K67 (50 μM; treated for 12 h) significantly inhibits the interaction between phosphorylated p62 and Keap1 and promotes the interaction between Nrf2 and Keap1 in immunoprecipitation assays in Huh1 cells1.
K67 (50 μM; treated for 4 h + 8 h (with the addition of the proteasome inhibitor lactacystin)) significantly promotes the ubiquitination of Nrf2 in Huh7 cells (expressing S351E)1.

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

K67 Related Antibodies

Cell Viability Assay[1]

Cell Line: Huh1 cells
Concentration: 50 μM
Incubation Time: 24 h, 48 h, 72 h
Result: Significantly inhibited the proliferation of Huh1 cells.

RT-PCR[1]

Cell Line: Huh1 cells
Concentration: 50 μM
Incubation Time: 12 h, 24 h, 48 h
Result: Inhibited the expression of Nrf2 target genes in Huh1 cells.

Western Blot Analysis[1]

Cell Line: Huh1 cells
Concentration: 50 μM
Incubation Time: 4 h, 12 h, 24 h, 36 h
Result: Increased the content of Nrf2 in both nuclear and cytosolic fractions of Huh1 cells decreased significantly. Meanwhile, Keap1 accumulated in a time-dependent manner.

Western Blot Analysis[1]

Cell Line: Huh1 cells
Concentration: 50 μM
Incubation Time: 12 h
Result: The interaction between phosphorylated p62 and Keap1 in Huh1 cells was significantly inhibited, while the interaction between Nrf2 and Keap1 was promoted.
Molecular Weight

582.69

Formula

C29H30N2O7S2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CC(CC1=CC(NS(C2=CC=C(C=C2)OCC)(=O)=O)=C3C=CC=CC3=C1NS(C4=CC=C(C=C4)OCC)(=O)=O)=O
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 (171.62 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 1.7162 mL 8.5809 mL 17.1618 mL
5 mM 0.3432 mL 1.7162 mL 3.4324 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.

  • Molarity Calculator

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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

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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    90% Corn Oil

    Solubility: ≥ 10 mg/mL (17.16 mM); Clear solution

    This protocol yields a clear solution of ≥ 10 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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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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 1.7162 mL 8.5809 mL 17.1618 mL 42.9045 mL
5 mM 0.3432 mL 1.7162 mL 3.4324 mL 8.5809 mL
10 mM 0.1716 mL 0.8581 mL 1.7162 mL 4.2904 mL
15 mM 0.1144 mL 0.5721 mL 1.1441 mL 2.8603 mL
20 mM 0.0858 mL 0.4290 mL 0.8581 mL 2.1452 mL
25 mM 0.0686 mL 0.3432 mL 0.6865 mL 1.7162 mL
30 mM 0.0572 mL 0.2860 mL 0.5721 mL 1.4301 mL
40 mM 0.0429 mL 0.2145 mL 0.4290 mL 1.0726 mL
50 mM 0.0343 mL 0.1716 mL 0.3432 mL 0.8581 mL
60 mM 0.0286 mL 0.1430 mL 0.2860 mL 0.7151 mL
80 mM 0.0215 mL 0.1073 mL 0.2145 mL 0.5363 mL
100 mM 0.0172 mL 0.0858 mL 0.1716 mL 0.4290 mL
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K67 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:

K672046250-48-8K 67K-67p62Keap1-Nrf2Sequestosome-1SQSTM1Inhibitorinhibitorinhibit

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