CBR-470-1

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.

Product information

CAS Number: 2416095-06-0

Molecular Weight: 365.90

Formula: C14H20ClNO4S2

Chemical Name: (3R,4S)-3-(4-chlorobenzenesulfonyl)-4-[(2-methylpropyl)amino]-1λ⁶-thiolane-1,1-dione

Smiles: CC(C)CN[C@H]1CS(=O)(=O)C[C@@H]1S(=O)(=O)C1=CC=C(Cl)C=C1

InChiKey: NFEQFEDSWINARK-KBPBESRZSA-N

InChi: InChI=1S/C14H20ClNO4S2/c1-10(2)7-16-13-8-21(17,18)9-14(13)22(19,20)12-5-3-11(15)4-6-12/h3-6,10,13-14,16H,7-9H2,1-2H3/t13-,14-/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 200 mg/mL (546.60 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

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.

Products are for research use only. Not for human use.