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

CBR-470-1 

Cat. No.: HY-134205A
Handling Instructions

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.

For research use only. We do not sell to patients.

CBR-470-1 Chemical Structure

CBR-470-1 Chemical Structure

CAS No. : 2416095-06-0

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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].

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

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

365.90

Formula

C₁₄H₂₀ClNO₄S₂

CAS No.

2416095-06-0

SMILES

CC(C)CN[[email protected]]([[email protected]@H](S(=O)(C1=CC=C(Cl)C=C1)=O)C2)CS2(=O)=O.[Relative stereochemistry]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

CBR-470-1Keap1-Nrf2glycolyticphosphoglyceratePGK1Nrf2neuronalMPP+cytotoxicity Inhibitorinhibitorinhibit

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CBR-470-1
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HY-134205A
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