| Identification | Back Directory | [Name]
3-Thiophenamine, 4-[(4-chlorophenyl)sulfonyl]tetrahydro-N-(2-methylpropyl)-, 1,1-dioxide, (3R,4S)-rel- | [CAS]
2416095-06-0 | [Synonyms]
CBR-470-1
3-Thiophenamine, 4-[(4-chlorophenyl)sulfonyl]tetrahydro-N-(2-methylpropyl)-, 1,1-dioxide, (3R,4S)-rel- | [Molecular Formula]
C14H20ClNO4S2 | [MOL File]
2416095-06-0.mol | [Molecular Weight]
365.89 |
| Chemical Properties | Back Directory | [Boiling point ]
592.4±50.0 °C(Predicted) | [density ]
1.39±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
Soluble to 100 mM in DMSO and to 20 mM in ethanol | [form ]
Solid | [pka]
6.28±0.40(Predicted) | [color ]
White to yellow |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
CBR-470-1 is an Inhibitor of the glycolytic enzyme PGK1 th at induces Nrf2 activity. PGK1 inhibition results in acculumation of methylglyoxalyl (MGO)a toxicreactive metabolite removed by other enzymes. The accumulated MGO then irreversibly reacts with Keap1 forming inactive Keap1 dimersresulting in accumulation of Nrf2. | [storage]
Store at -20°C | [References]
[1] Bollong MJ, et, al. A metabolite-derived protein modification integrates glycolysis with KEAP1-NRF2 signalling. Nature. 2018 Oct;562(7728):600-604. DOI:10.1038/s41586-018-0622-0
[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. DOI:10.18632/aging.103443 |
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