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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+.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $35 | In Stock | |
1 mL x 10 mM (in DMSO) | $62 | In Stock |
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 |
Smiles | S(=O)(=O)([C@@H]1[C@@H](NCC(C)C)CS(=O)(=O)C1)C2=CC=C(Cl)C=C2 |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 100 mg/mL (273.30 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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