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.
体外研究
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.
Active against all of the lines tested, and the EC50s were variable (between ~0.3 μM and 4 μM). Normal MEFs and OPM1 and OPM2 were relatively less sensitive.
Western Blot Analysis
Cell Line:
MDA-MB-231 cells
Concentration:
10 μM
Incubation Time:
48 hours
Result:
Incudes apoptotic mediators cleavage of caspase 3 and PARP.
体内研究
JG-98 (3 mg/kg; i.p.; on days 0, 2, and 4) suppresses tumor growth in xenograft models bearing MCF7 and HeLa cells.
Animal Model:
6-week-old NCR mice (xenografts of MCF7 and HeLa cells)
Dosage:
3 mg/kg
Administration:
Intraperitoneal injection; on days 0, 2, and 4
Result:
Limited tumor growth, but somewhat less effectively.
分子式
C24H21Cl2N3Os3
分子量
534.54
CAS号
1456551-16-8
运输条件
Room temperature in continental US; may vary elsewhere.