纯度:98% by TLC;NMR (Conforms)
分子式:C27H45IN2
分子量:524.56
溶剂:DMSO (>25 mg/ml) Ethanol (>25 mg/ml)
性状:Off-white solid
存储:-20°C
Activity (short version):Eukaryotic elongation factor 2 (eEF-2) kinase inhibitor
Function / Pharmacology:NH125 was originally discovered as an antibacterial agent active against various Gram-positive and -negative bacteria via inhibition of histidine protein kinase.1 It was also found to be a potent inhibitor of eukaryotic elongation factor 2 (eEF-2) kinase (IC50 = 60 nM) with efficacy against a broad spectrum of human cancer cell lines.2 Other studies have linked the anticancer effects of NH125 to induction of eEF2 phosphorylation.3,4 NH125 has also been shown to engage the EIF2a-ATF4-CHOP axis resulting in induction of DR5 expression.5 Treatment of glioma stem cells with NH125 resulted in a sustained decrease in tumor volume via activation of integrated stress response (ISR) and GADD45 pathways.5