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CAS No.: 1456551-16-8

JG-98 Catalog No. CSN22600

Synonyms: JG98

JG-98, an allosteric heat shock protein 70 (Hsp70) inhibitor which shows anti-cancer activities affecting both cancer cells and tumor-associated macrophages.

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400-920-2911

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技术信息

生物活性

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].
参考文献

[1] Li X, Srinivasan SR, Connarn J, et al. Analogs of the Allosteric Heat Shock Protein 70 (Hsp70) Inhibitor, MKT-077, as Anti-Cancer Agents. ACS Med Chem Lett. 2013;4(11):1042-1047.
[2] Li X, Colvin T, Rauch JN, et al. Validation of the Hsp70-Bag3 protein-protein interaction as a potential therapeutic target in cancer. Mol Cancer Ther. 2015;14(3):642-648.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.8708 mL
- 9.3538 mL
- 18.7075 mL
- 5 mM
- 0.3742 mL
- 1.8708 mL
- 3.7415 mL
- 10 mM
- 0.1871 mL
- 0.9354 mL
- 1.8708 mL

技术信息

CAS号

1456551-16-8

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H21Cl2N3OS3

运输

蓝冰

分子量

534.54

别名

JG98

溶解度

DMSO	8.0 mg/mL (15.0 mM)
Water	Insoluble
Ethanol	Insoluble

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