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CBR-470-1

Catalog No. T40063   CAS 2416095-06-0

CBR-470-1 is a potent inhibitor of glycolytic phosphoglycerate kinase 1 (PGK1) that activates NRF2 by increasing methylglyoxal levels. CBR-470-1 is a non-covalent Nrf2 activator with neuroprotective activity that protects SH-SY5Y neuronal cells from MPP+-induced cytotoxicity by activating the Keap1-Nrf2 cascade. cytotoxicity induced by MPP+.

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CBR-470-1 Chemical Structure
CBR-470-1, CAS 2416095-06-0
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1 mg In stock $ 30.00
5 mg In stock $ 78.00
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1 mL * 10 mM (in DMSO) In stock $ 62.00
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Purity: 98.03%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description CBR-470-1 is a potent inhibitor of glycolytic phosphoglycerate kinase 1 (PGK1) that activates NRF2 by increasing methylglyoxal levels. CBR-470-1 is a non-covalent Nrf2 activator with neuroprotective activity that protects SH-SY5Y neuronal cells from MPP+-induced cytotoxicity by activating the Keap1-Nrf2 cascade. cytotoxicity induced by MPP+.
Targets&IC50 ARE-LUC:962 nM (EC50)
In vitro In IMR32 cells, CBR-470-1, when applied for 24 hours at concentrations ranging from 0.01 to 10 μM, demonstrates an EC50 of 962 nM in the ARE-LUC reporter assay[1].Furthermore, CBR-470-1 induces a dose- and time-dependent accumulation of Nrf2 protein in IMR32 cells when administered at concentrations between 0.5 and 20 μM over a period of 1 to 24 hours[1].In SH-SY5Y cells, a 4-hour treatment with CBR-470-1 at 10 μM activates the Nrf2 signaling cascade[2].Moreover, a 2-hour exposure to CBR-470-1 at 10 μM inhibits MPP+-induced oxidative injury in SH-SY5Y neuronal cells[2].
Molecular Weight 365.9
Formula C14H20ClNO4S2
CAS No. 2416095-06-0

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL(273.30 mM), Sonication is recommended.

TargetMolReferences and Literature

1. Zheng J, et, al. PGK1 inhibitor CBR-470-1 protects neuronal cells from MPP+. Aging (Albany NY). 2020 Jul 10;12(13):13388-13399. 2. Bollong MJ, et, al. A metabolite-derived protein modification integrates glycolysis with KEAP1-NRF2 signalling. Nature. 2018 Oct;562(7728):600-604.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Immunology/Inflammation Compound Library

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Keywords

CBR-470-1 2416095-06-0 Immunology/Inflammation Nrf2 CBR4701 CBR 470 1 inhibitor inhibit

 

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