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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.

  • XL888 EY0672

    XL888一种ATP竞争性的HSP90抑制剂，IC50为24 nM。XL888 作用于NCI-N87细胞，诱导HER2退化，IC50为56 nM。XL888 抑制过量表达HER2的NCI-N87, 过量表达HER2的BT-474，过量表达HER2的MDA-MB-453, MET突变的MKN45, B-Raf突变的Colo-205, B-Raf突变的SK-MEL-28, EGFR突变的HN5, EGFR突变的NCI-H1975, 及K-Ras突变的A549细胞增殖，IC50分别为21.8, 0.1, 16.0, 45.5, 11.6, 0.3, 5.5, 0.7, 和 4.3 nM。XL888作用于Vemurafenib敏感的和抗Vemurafenib的黑色素瘤细胞系及具有内在耐药性的黑色素瘤细胞系，导致细胞生长降低，这种作用存在剂量依赖性，IC50 约为0.1 μM。

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  • SNX-2112 EY0517

    SNX-2112选择性结合到HSP90α和HSP90β的ATP结合袋中，Ka分别为30 nM和30 nM，比17-AAG更有效。

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  • BIIB021 EY0509

    BIIB021是口服活性的HSP90抑制剂，Ki和EC50分别为1.7 nM和38 nM。

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  • Onalespib EY0339

    AT13387是一种有效的，选择性Hsp90抑制剂，作用于A375细胞，IC50为18 nM，具有较长时间的抗肿瘤活性。

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  • Nelfinavir Mesylate EY0327

    Nelfinavir Mesylate 是口服的人HIV-1蛋白酶抑制剂，Ki为2nM。

    More

  • XL888 EY0672

    XL888一种ATP竞争性的HSP90抑制剂，IC50为24 nM。XL888 作用于NCI-N87细胞，诱导HER2退化，IC50为56 nM。XL888 抑制过量表达HER2的NCI-N87, 过量表达HER2的BT-474，过量表达HER2的MDA-MB-453, MET突变的MKN45, B-Raf突变的Colo-205, B-Raf突变的SK-MEL-28, EGFR突变的HN5, EGFR突变的NCI-H1975, 及K-Ras突变的A549细胞增殖，IC50分别为21.8, 0.1, 16.0, 45.5, 11.6, 0.3, 5.5, 0.7, 和 4.3 nM。XL888作用于Vemurafenib敏感的和抗Vemurafenib的黑色素瘤细胞系及具有内在耐药性的黑色素瘤细胞系，导致细胞生长降低，这种作用存在剂量依赖性，IC50 约为0.1 μM。

    More

  • SNX-2112 EY0517

    SNX-2112选择性结合到HSP90α和HSP90β的ATP结合袋中，Ka分别为30 nM和30 nM，比17-AAG更有效。

    More

  • BIIB021 EY0509

    BIIB021是口服活性的HSP90抑制剂，Ki和EC50分别为1.7 nM和38 nM。

    More

  • Onalespib EY0339

    AT13387是一种有效的，选择性Hsp90抑制剂，作用于A375细胞，IC50为18 nM，具有较长时间的抗肿瘤活性。

    More

  • Nelfinavir Mesylate EY0327

    Nelfinavir Mesylate 是口服的人HIV-1蛋白酶抑制剂，Ki为2nM。

    More
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