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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AUY922 (NVP-AUY922)是高活性HSP90α和β抑制剂，IC50为13 nM和21 nM，对GRP94和 TRAP-1的活性较低。
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Geldanamycin是HSP90抑制剂，Kd为1.2 μM。
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VER-155008是Hsc70/Hsp70新型小分子抑制剂，对HCT116细胞GI50值为5uM。
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Elesclomol (STA-4783)是新型氧化应激诱导剂，能促肿瘤细胞凋亡。
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PU-H71是Hsp90抑制剂，IC50为50 nM。
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AUY922 (NVP-AUY922)是高活性HSP90α和β抑制剂，IC50为13 nM和21 nM，对GRP94和 TRAP-1的活性较低。
More
-
Geldanamycin是HSP90抑制剂，Kd为1.2 μM。
More
-
VER-155008是Hsc70/Hsp70新型小分子抑制剂，对HCT116细胞GI50值为5uM。
More
-
Elesclomol (STA-4783)是新型氧化应激诱导剂，能促肿瘤细胞凋亡。
More
-
PU-H71是Hsp90抑制剂，IC50为50 nM。
More
