化合物JG-98 T5350

Product Introduction
Bioactivity


英文名: JG-98

描述: JG-98 是一种热休克蛋白 70 (Hsp70)变构抑制剂，可与 Hsp70 上的保守位点紧密结合，打断 Hsp70-Bag3 相互作用。它影响癌细胞和肿瘤相关巨噬细胞，具有抗癌活性。

细胞实验: Cell viability was determined using an MTT colorimetric assay with the following modifications. Briefly, cells (5 x 10^3 ) were plated into 96-well assay plates in 0.1 ml media and allowed to attach overnight. Cells were then treated with compound at various concentrations in 0.2 mL media. After the 72-hour incubation period, cells were washed in PBS (3 x 100 μL), and 10 μL MTT reagent was added with 100 μL fresh media. Cells were then incubated for 4 hr in a humidified chamber at 37 oC with 5% CO2. Insoluble formazan crystals were solubilized by addition of 0.1 mL detergent solution (4 hr at room temp., dark). Resulting colored solutions were then quantified at an absorbance of 570 nm [1].

动物实验: Briefly, one million MCF7 or HeLa cells in Matrigel were subcutaneously injected bilaterally into 6 week old NCR mice. Once tumors were established, JG-98 (3 mg/kg; n=5) or vehicle control (1:1 PBS: DMSO; n=5) was introduced interperitoneally on days 2, 4 and 6. Tumor growth (10 tumors/5 mice) was measured by caliper every other day [2].

体外活性: JG-98 had a potency of 0.4 ± 0.03 μM against MDA-MB-231 cells and an EC50 value of 0.7 ± 0.2 μM for MCF7 cells. In MDA-MB-231 cells, the treatment of JG-98 activated apoptotic mediators (caspase-3 and PARP). Treatment of both MDA-MB-231 and MCF7 cells with JG-98 strongly affected autophagic flux [1]. JG-98 has antiproliferative activity (EC50 values between 0.3 and 4 μmol/L) across cancer cell lines from multiple origins. JG-98 destabilized FoxM1 and relieved suppression of downstream effectors, including p21 and p27 [2].

体内活性: JG-98（3 mg/kg）在HeLa异种移植模型中抑制了肿瘤生长，尽管效果较弱[2]。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 5 mg/mL (9.35 mM)


关键字: HSP | Apoptosis | JG-98 | inhibit | Heat shock proteins | Inhibitor

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