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Description: PGK1 inhibitor; activates Nrf2
Chemical Name: (3R,4S)-rel-4-[(4-Chlorophenyl)sulfonyl]tetrahydro-N-(2-methylpropyl)-3-thiophenamine-1,1-dioxide
Purity: ≥98% (HPLC)

Biological Activity for CBR-470-1

CBR-470-1 is a phosphoglycerate kinase 1 (PGK1) inhibitor. CBR-470-1 promotes accumulation of the reactive metabolites methylglyoxal (MGO) resulting in KEAP1 modification and dimerization, which in turn leads to activation of the Nrf2 transcriptional program. CBR-470-1 protects SH-SY5Y neuroblastoma cells from MPP+-induced cytotoxicity via the Keap1-Nrf2 cascade.

Compound Libraries for CBR-470-1

CBR-470-1 is also offered as part of the Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for CBR-470-1

M. Wt 365.89
Formula C14H20ClNO4S2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2416095-06-0
PubChem ID 20898025
Smiles CC(CN[C@H]1CS(=O)(C[C@@H]1S(=O)(C2=CC=C(C=C2)Cl)=O)=O)C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for CBR-470-1

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 36.59 100
ethanol 7.32 20

Preparing Stock Solutions for CBR-470-1

The following data is based on the product molecular weight 365.89. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.73 mL 13.67 mL 27.33 mL
5 mM 0.55 mL 2.73 mL 5.47 mL
10 mM 0.27 mL 1.37 mL 2.73 mL
50 mM 0.05 mL 0.27 mL 0.55 mL

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References for CBR-470-1

References are publications that support the biological activity of the product.

Bollong et al (2018) A metabolite-derived protein modification integrates glycolysis with KEAP1-NRF2 signalling. Nature 562 600 PMID: 30323285

Zheng et al (2020) PGK1 inhibitor CBR-470-1 protects neuronal cells from MPP+. Aging (Albany NY) 12 13388 PMID: 32649311

If you know of a relevant reference for CBR-470-1, please let us know.

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Keywords: CBR-470-1, CBR-470-1 supplier, phosphoglycerate, kinase, 1, (PGK1), inhibitor, cytoprotection, NRF2, activator, KEAP1, Other, Kinases, Nrf2, 7018, Tocris Bioscience

Citations for CBR-470-1

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