CBR-470-1
目录号: PL03394 纯度: ≥98%
CAS No. :2416095-06-0
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中文名称
CBR-470-1
英文名称
CBR-470-1
英文别名
(3R,4S)-3-((4-Chlorophenyl)sulfonyl)-4-(isobutylamino)tetrahydrothiophene 1,1-dioxide;rel-(3R,4S)-3-((4-Chlorophenyl)sulfonyl)-4-(isobutylamino)tetrahydrothiophene 1,1-dioxide;(3R,4S)-3-[(4-chlorophenyl)sulfonyl]-4-(isobutylamino)tetrahydro-1H-1lambda-thiophene-1,1-dione;Schembl21033073;CBR-470-1
Cas No.
2416095-06-0
分子式
C14H20ClNO4S2
分子量
365.90
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
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。
生物活性
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.
性状
Solid
IC50 & Target[1][2]
Keap1-Nrf2
体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Bollong MJ, et, al. A metabolite-derived protein modification integrates glycolysis with KEAP1-NRF2 signalling. Nature. 2018 Oct;562(7728):600-604.
[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.
溶解度数据
In Vitro: DMSO : 200 mg/mL (546.60 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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