2. NF-κB
  3. Keap1-Nrf2
  4. CBR-470-1

CBR-470-1 is an inhibitor of the glycolytic enzyme phosphoglycerate kinase 1 (PGK1). CBR-470-1 is also a non-covalent Nrf2 activator. CBR-470-1 protects SH-SY5Y neuronal cells against MPP+-induced cytotoxicity through activation of the Keap1-Nrf2 cascade.

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CBR-470-1 Chemical Structure

CBR-470-1 Chemical Structure

CAS No. : 2416095-06-0

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Customer Review

Based on 1 publication(s) in Google Scholar

CBR-470-1 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE CBR-470-1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

CBR-470-1 is an inhibitor of the glycolytic enzyme phosphoglycerate kinase 1 (PGK1). CBR-470-1 is also a non-covalent Nrf2 activator. CBR-470-1 protects SH-SY5Y neuronal cells against MPP+-induced cytotoxicity through activation of the Keap1-Nrf2 cascade[1][2].

IC50 & Target

Keap1-Nrf2[2]
In Vitro

CBR-470-1 (0.01-10 μM; 24 h) has an EC50 of 962 nM in ARE-LUC reporter assay of IMR32 cells[1].
CBR-470-1 (0.5-20 μM; 1-24 h) results in a dose- and time-dependent accumulation of Nrf2 protein in IMR32 cells[1].
CBR-470-1 (10 μM; 4 h) activates Nrf2 signaling cascade in SH-SY5Y cells[2].
CBR-470-1 (10 μM; 2 h) inhibits MPP+-induced oxidative injury in SH-SY5Y neuronal cells[2].

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

CBR-470-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: IMR32 cells
Concentration: 0.5, 1, 5, 10, 20 μM
Incubation Time: 1, 2, 4, 8, 24 h
Result: Increased the Nrf2 protein in a dose- and time-dependent manner.
Increased both mRNA and protein levels of the Nrf2-responsive genes NQO1 and HMOX1.
Molecular Weight

365.89

Formula

C14H20ClNO4S2
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

CC(C)CN[C@H]([C@@H](S(=O)(C1=CC=C(Cl)C=C1)=O)C2)CS2(=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 : 200 mg/mL (546.61 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 2.7331 mL 13.6653 mL 27.3306 mL
5 mM 0.5466 mL 2.7331 mL 5.4661 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

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

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: ≥ 5 mg/mL (13.67 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 5 mg/mL (13.67 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
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 2.7331 mL 13.6653 mL 27.3306 mL 68.3265 mL
5 mM 0.5466 mL 2.7331 mL 5.4661 mL 13.6653 mL
10 mM 0.2733 mL 1.3665 mL 2.7331 mL 6.8327 mL
15 mM 0.1822 mL 0.9110 mL 1.8220 mL 4.5551 mL
20 mM 0.1367 mL 0.6833 mL 1.3665 mL 3.4163 mL
25 mM 0.1093 mL 0.5466 mL 1.0932 mL 2.7331 mL
30 mM 0.0911 mL 0.4555 mL 0.9110 mL 2.2776 mL
40 mM 0.0683 mL 0.3416 mL 0.6833 mL 1.7082 mL
50 mM 0.0547 mL 0.2733 mL 0.5466 mL 1.3665 mL
60 mM 0.0456 mL 0.2278 mL 0.4555 mL 1.1388 mL
80 mM 0.0342 mL 0.1708 mL 0.3416 mL 0.8541 mL
100 mM 0.0273 mL 0.1367 mL 0.2733 mL 0.6833 mL
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CBR-470-1 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:

CBR-470-12416095-06-0Keap1-Nrf2glycolyticphosphoglyceratePGK1Nrf2neuronalMPP+cytotoxicity Inhibitorinhibitorinhibit

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