HSP
HSPs are a family of proteins that are produced by cells in response to exposure to stressful conditions. Many members of this group perform chaperone function by stabilizing new proteins to ensure correct folding or by helping to refold proteins that were damaged by the cell stress. This increase in expression is transcriptionally regulated. The dramatic upregulation of the heat shock proteins is a key part of the heat shock response and is induced primarily by heat shock factor (HSF). Heat-shock proteins are named according to their molecular weight. For example, Hsp60, Hsp70 and Hsp90 (the most widely studied HSPs) refer to families of heat shock proteins on the order of 60, 70, and 90 kilodaltons in size, respectively. The small 8-kilodalton protein ubiquitin, which marks proteins for degradation, also has features of a heat shock protein. Heat Shock Factor 1 (HSF1) is a transcription factor that is involved in the general maintenance and upregulation of Hsp70 protein expression. HSF1 inhibition by a potent RNA aptamer attenuates mitogenic (MAPK) signaling and induces cancer cell apoptosis.
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KNK437 是一种泛-HSP 抑制剂，其抑制诱导型HSPs，包括 HSP105，HSP72，和 HSP40的合成。
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NMS-E973 是一种强效的选择性的Hsp90抑制剂，其结合于Hsp90的 DC50 小于10 nM , 对一系列52种其他不同蛋白激酶没有抑制活性。
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NVP-HSP990是Hsp90抑制剂，对Hsp90α的IC50值为13nM，抗癌增殖活性。
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VER-50589能高效抑制Hsp90，IC50为21 nM。
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CH5138303 是一种口服有效的Hsp90抑制剂，其Kd为 0.48 nM。
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KNK437 是一种泛-HSP 抑制剂，其抑制诱导型HSPs，包括 HSP105，HSP72，和 HSP40的合成。
More
-
NMS-E973 是一种强效的选择性的Hsp90抑制剂，其结合于Hsp90的 DC50 小于10 nM , 对一系列52种其他不同蛋白激酶没有抑制活性。
More
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NVP-HSP990是Hsp90抑制剂，对Hsp90α的IC50值为13nM，抗癌增殖活性。
More
-
VER-50589能高效抑制Hsp90，IC50为21 nM。
More
-
CH5138303 是一种口服有效的Hsp90抑制剂，其Kd为 0.48 nM。
More
