JG-98 is an allosteric Hsp70 inhibitor, displays high active against the breast cancer cell lines MDA-MB-231 and MCF-7 (EC50s: 0.4/0.7 μM).

HSP70(MCF-7):0.7 μM, HSP70 (MDA-MB-231):0.4μM

JG-98对MDA-MB-231细胞具有0.4 ± 0.03 μM的活性，并对MCF7细胞具有0.7 ± 0.2 μM的EC50值。在MDA-MB-231细胞中，JG-98的处理激活了凋亡介质（caspase-3和PARP）。JG-98对MDA-MB-231和MCF7细胞的处理显著影响了自噬流[1]。JG-98具有抗增殖活性（EC50值在0.3至4 μmol/L之间），覆盖了来自多个起源的癌细胞系。JG-98破坏了FoxM1并解除了对下游效应物，包括p21和p27的抑制[2]。

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]。

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].

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].