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一般描述
7-Desacetoxy-6,7-dehydrogedunin (7DG) is structurally similar to HSP90 (heat shock protein 90) inhibitor, also known as gedunin.
生化/生理作用
7-Desacetoxy-6,7-dehydrogedunin (7DG) is a selective inhibitor of protein kinase R (PKR).
7-Desacetoxy-6,7-dehydrogedunin (7DG) is a selective inhibitor of protein kinase R (PKR). 7DG appears to directly interact with the C-terminal half of PKR, and unlike C16, does not bind the ATP catalytic pocket. 7-Desacetoxy-6,7-dehydrogedunin completely protected macrophages from anthrax lethal toxin (LT)-induced pyroptotic cell death, a model for inflammasome-mediated caspase-1 activation, with an (IC50) of 5 μM, showing a role for PKR in pyroptosis.
特点和优势
This compound is featured on the Caspases page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
警示用语:
Warning
危险声明
危险分类
Acute Tox. 4 Oral
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Nature chemical biology, 9(6), 398-405 (2013-04-23)
Formation of the inflammasome, a scaffolding complex that activates caspase-1, is important in numerous diseases. Pyroptotic cell death induced by anthrax lethal toxin (LT) is a model for inflammasome-mediated caspase-1 activation. We discovered 7-desacetoxy-6,7-dehydrogedunin (7DG) in a phenotypic screen as
商品
Agents reported to activate cellular caspases include chemotherapeutic drugs, TNF receptor agonists, and other enzymes. Inhibitors of apoptosis were the first identified endogenous caspase inhibitors.
据报道可激活细胞半胱天冬酶的试剂包括化疗药物、TNF 受体激动剂和其他酶。细胞凋亡抑制剂是第一个确定的内源性半胱天冬酶抑制剂。
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