JG-98, an allosteric heat shock protein 70 (Hsp70) inhibitor, which binds tightly to a conserved site on Hsp70 and disrupts the Hsp70-Bag3 interaction. JG-98 shows anti-cancer activities affecting both cancer cells and tumor-associated macrophages.
性状
Solid
IC50 & Target[1][2]
Heat shock protein 70
体外研究(In Vitro)
JG-98 (30 nM-30 μM; 72 hours) has antiproliferative activity across a range of cell lines with the EC50s between ~0.3 and 4 μM.JG-98 (10 μM; 48 hours) activates apoptotic mediators (cleavage of caspase-3 and PARP) in MDA-MB-231 cells.JG-98 destabilizes FoxM1 and relieves suppression of downstream effectors, including p21 and p27. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Proliferat
体内研究(In Vivo)
JG-98 (3 mg/kg; i.p.; on days 0, 2, and 4) suppresses tumor growth in xenograft models bearing MCF7 and HeLa cells. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: 6-week-old NCR mice
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Li X, et al. Analogs of the Allosteric Heat Shock Protein 70 (Hsp70) Inhibitor, MKT-077, as Anti-Cancer Agents. ACS Med Chem Lett. 2013 Nov 14;4(11).[2]. Li X, et al. Validation of the Hsp70-Bag3 protein-protein interaction as a potential therapeutic target in cancer. Mol Cancer Ther. 2015 Mar;14(3):642-8.
溶解度数据
In Vitro: DMSO : 5 mg/mL (9.35 mM; Need ultrasonic)配制储备液