JG-98
产品说明书
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同义名 : | - |
| CAS号 : | 1456551-16-8 | |
| 货号 : | A625683 | |
| 分子式 : | C24H21Cl2N3OS3 | |
| 纯度 : | 97% | |
| 分子量 : | 534.54 | |
| MDL号 : | MFCD32067914 | |
| 存储条件： |
Pure form Inert atmosphere, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
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| 描述 | Heat shock protein 70 (Hsp70) is an ATP-dependent molecular chaperone that plays essential roles in protein homeostasis. These chaperones bind and stabilize a wide array of proteins, including many kinases and transcription factors involved in pro-survival signaling. Accordingly, high levels of Hsp70s are associated with immortalized cells and poor prognosis in multiple types of cancer, including breast cancer, endometrial cancer, and cervical cancer. JG-98, an allosteric Hsp70 inhibitor, has antiproliferative activity against cancer cell lines through its ability to inhibit members of the Hsp70 family of molecular chaperones. JG-98 exhibited activity against the breast cancer cell lines MDA-MB-231 and MCF-7 with EC50 values of 0.4 ± 0.03 and 0.7 ± 0.2 μM, respectively. After MDA-MB-231 cells were treated with JG-98 for 48 h, both apoptotic mediators (caspase-3 and PARP) were activated, suggesting that JG-98 triggers apoptosis. Treatment of both MDA-MB-231 and MCF7 cells with JG-98 strongly affected autophagic flux, as indicated by an increase in p62 oligomerization and a reduction in p62 monomer[1]. JG-98 strongly inhibited the interactions between Hsp70 and Bag3, with an IC50 value of 1.6 ± 0.3 μM. JG-98 was a good inhibitor of the Hsp70-Bag1 and Hsp70-Bag2 complexes, with IC50 values of 0.6 ± 0.1 and 1.2 ± 0.1 μM, respectively. Hsp70 was immunoprecipitated from HeLa cells in the presence of JG-98 (50 μM) to test if JG-98 could disrupt the Hsp70-Bag3 interaction in cells. JG-98 reduced the Hsp70-Bag3 interaction by ~ 60%. JG-98 (3 mg/kg) suppressed tumor growth in a HeLa xenograft model[2]. | ||
| 作用机制 | JG-98 bound to a conserved, allosteric site on Hsp70 (residues I142, F148, D222, T223, and H224)[1]. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.87mL 0.37mL 0.19mL |
9.35mL 1.87mL 0.94mL |
18.71mL 3.74mL 1.87mL |
| 参考文献 |
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