CBR-470-1 是糖酵解磷酸甘油酸激酶1 (PGK1) 的抑制剂。 CBR-470-1 也是一种非共价的?Nrf2?激活剂。CBR-470-1 通过激活 Keap1-Nrf2 级联反应，保护 SH-SY5Y 神经元细胞免受 MPP+?诱导的细胞毒性。
货号:ajcx12134
CAS:2416095-06-0
分子式:C??H??ClNO?S?
分子量：365.90
溶解度:DMSO : 200 mg/mL (546.60 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

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:	IMR32 cells
Concentration:	0.5, 1, 5, 10, 20 μM
Incubation Time:	1, 2, 4, 8, 24 h
Result:	Increased the Nrf2 protein in a dose- and time-dependent manner. Increased both mRNA and protein levels of the Nrf2-responsive genes?NQO1?and?HMOX1.