CBR-470-1

Name: CBR-470-1
Brand: Tocris Bioscience
SKU: 7018

Tocris Bioscience, part of Bio-Techne | Catalog # 7018

Citations (2)

COA / SDS

PGK1 inhibitor; activates Nrf2

Key Product Details

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)
Molecular Weight:	365.89

View Full Technical Details for CBR-470-1

Technical Data
Citations

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
InChi Key	NFEQFEDSWINARK-KBPBESRZSA-N
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 for CBR-470-1

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	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.

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.

Zheng PGK1 inhibitor CBR-470-1 protects neuronal cells from MPP+. Aging (Albany NY) 2020 PMID: 32649311
Bollong A metabolite-derived protein modification integrates glycolysis with KEAP1-NRF2 signalling. Nature 2018 PMID: 30323285