产品
编 号:F755170
分子式:C22H21ClN6
分子量:404.9
产品类型
结构图
CAS No: 2741856-68-6
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生物活性:
Synucleozid hydrochloride (NSC 377363 hydrochloride) is a potent inhibitor of the?SNCA?mRNA?that encodes α-synuclein protein. Synucleozid selectively?targets the?α-synuclein?mRNA 5′ UTR at the designed IRE site, decreases the amount of?SNCA?mRNA loaded into polysomes and thereby inhibits?SNCA?translation. Synucleozid has the potential for the investigation of Parkinson’s disease.
体外研究:
Synucleozid (0.25-1 μM; 24 hours) abrogates cytotoxicity induced by α-synuclein preformed fibrils, which act as seeds and recruit endogenous α-synuclein to aggregate.Synucleozid (0-1 μM; 24 hours) binds to the A bulge near the base of the IRE hairpin, reduced levels of α-synuclein in a dose-dependent manner with an IC50 of 500 nM, and inhibits α-synuclein protein expression in SH-SY5Y neuroblastoma cells.Synucleozid (100 nM-100 μM; 24 hours) binds to 2-AP-labeled and native IRE RNA with similar affinities. It decreases 2-AP emission with an EC50?value of 2.7 ± 0.4 μM, recovery of 2-AP emissions is observed as a function of unlabeled?SNCA?IRE RNA (RNA-0) concentration, affording a competitive?Kd?of 1.5 ± 0.3 μM.Synucleozid (0.25-1 μM; 24 hours) decreases α-synuclein and other proteins that have IREs in their mRNA’s UTR including APP, PrP, Ferritin and TfR as a dose-dependent mannner. All panels is completed in SH-SY5Y cells, except for PrP protein which is assessed in Neuro-2A cells.