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A-484954

CAS No. : 142557-61-7

MCE 站：A-484954

产品活性：A-484954 是真核延长因子 2 (eEF2) 的高度选择性抑制剂，其 IC₅₀ 值为 280 nM。

研究领域：Neuronal Signaling  |  Autophagy

作用靶点：CaMK  |  Autophagy

In Vitro: A-484954 is a highly selective eEF2K inhibitor with an IC₅₀ value of 280 nM against eEF2K in the enzymatic assay and little activity against a wide panel of serine/threonine and tyrosine kinases. In enzymatic assay, the IC₅₀ value of A-484954 is increased as the concentration of ATP increased but unaffected by increasing concentrations of calmodulin.

In Vivo: A484954 causes relaxation in E (+) and E (-) aorta or mesenteric artery precontracted with NA. Pretreatment with L-NAME but not indomethacin or cimetidine partially inhibits the A484954-induced relaxation in mesenteric artery. Long-term A-484954 treatment inhibits MCT-induced increases PA pressure. It is revealed that A-484954 inhibits MCT-induced PA hypertrophy and fibrosis but not impairment of endothelium-dependent and -independent relaxation. Furthermore, A-484954 inhibits MCT-induced NADPH oxidase-1 expression and ROS generation as well as matrix metalloproteinase-2 activation.

相关产品：Kinase Inhibitor Library  |  Neuronal Signaling Compound Library  |  Anti-Cancer Compound Library  |  Bioactive Compound Library Plus  |  Autophagy Compound Library  |  KN-93  |  STO-609  |  KN-62  |  NH125  |  CaMKII-IN-1  |  K-252a  |  KN-92 hydrochloride  |  MLCK inhibitor peptide 18  |  Autocamtide-2-related inhibitory peptide TFA  |  Calmidazolium chloride  |  DDD107498 succinate  |  Rimacalib  |  Syntide 2 TFA  |  Autocamtide 2  |  A-3 hydrochloride  |  Lavendustin C  |  Autocamtide 2, amide  |  Calmodulin-Dependent Protein Kinase II (290-309)  |  Metofenazate

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