CBR-470-1

Research use only, not for human use.

CBR-470-1 is a potent inhibitor of glycolytic phosphoglycerate kinase 1 (PGK1) that activates NRF2 by increasing methylglyoxal levels.

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.

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

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Nuclear Receptor/Transcription Factor

Keap1-Nrf2

Nrf2

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2416095-06-0

365.9

C14H20ClNO4S2

>98% (HPLC)

In Vitro:?DMSO : 200 mg/mL (546.60 mM; Ultrasonic )

S(=O)(=O)([C@@H]1[C@@H](NCC(C)C)CS(=O)(=O)C1)C2=CC=C(Cl)C=C2

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(-20℃)

With Ice Pack

≥ 2 years