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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Keap1-Nrf2-CBR-470-1
CBR-470-1

Chemical Structure : CBR-470-1

CAS No.: 2416095-06-0

CBR-470-1

货号: PC-24727Not For Human Use, Lab Use Only.

CBR-470-1 is a small molecule inhibitor of glycolytic enzyme phosphoglycerate kinase 1 (PGK1), activates NRF2 signaling in vitro and in vivo.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

CBR-470-1 is a small molecule inhibitor of glycolytic enzyme phosphoglycerate kinase 1 (PGK1), activates NRF2 signaling in vitro and in vivo.
CBR-470-1 induces transcript levels of NQO1 and HMOX1, as well as enhances NRF2 protein stabilization in HEK293T, SH-SY5Y, and primary human lung fibroblasts.
CBR-470-1 induces methylglyoxal modification of Keap1, Keap1-Nrf2 disassociation, and increases expression of Nrf2 responsive genes.
CBR-470-1 potently attenuates MPP+-induced oxidative injury and SH-SY5Y cell apoptosis.
CBR-470-1 neuroprotection is dependent upon Nrf2, as Nrf2 shRNA or CRISPR/Cas9-mediated Nrf2 knockout, abolished CBR-470-1-induced SH-SY5Y cytoprotection against MPP+.

物理化学性质&存储条件

分子量 365.89
分子式 C14H20ClNO4S2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

rel-(3R,4S)-3-((4-Chlorophenyl)sulfonyl)-4-(isobutylamino)tetrahydrothiophene 1,1-dioxide

参考文献

1. Bollong MJ, et, al. Nature. 2018 Oct;562(7728):600-604.

2. Zheng J, et al. Aging (Albany NY). 2020 Jul 10;12(13):13388-13399.

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