| Bioactivity | 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]. | ||||||||||||
| Target | Keap1-Nrf2 | ||||||||||||
| Invitro | 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]. Western Blot Analysis[1] Cell Line: | ||||||||||||
| Name | CBR-470-1 | ||||||||||||
| CAS | 2416095-06-0 | ||||||||||||
| Formula | C14H20ClNO4S2 | ||||||||||||
| Molar Mass | 365.90 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Bollong MJ, et, al. A metabolite-derived protein modification integrates glycolysis with KEAP1-NRF2 signalling. Nature. 2018 Oct;562(7728):600-604. [2]. Zheng J, et, al. PGK1 inhibitor CBR-470-1 protects neuronal cells from MPP+. Aging (Albany NY). 2020 Jul 10;12(13):13388-13399. |
CBR-470-1
CAS: 2416095-06-0 F: C14H20ClNO4S2 W: 365.90
CBR-470-1 is an inhibitor of the glycolytic enzyme phosphoglycerate kinase 1 (PGK1). CBR-470-1 is also a non-covalent Nr
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