SD70,HistoneDemethylaseJMJD2Inhibitor

SD70 is a potent, selective and cell-permeable inhibitor of histone demethylase JMJD2 (KDM4C), identified by phenotypic screening for inhibitors of ligand and genotoxic stress-induced translocations in prostate cancer cells. Through Chem-seq approach, SD70 was found to inhibit the androgen-dependent AR program and prostate cancer cell growth, acting, at least in part, by functionally inhibiting the Jumonji domain-containing demethylase KDM4C. SD70 inhibits AR target gene expression, inhibits prostate cancer cell growth in vitro and tumor growth in vivo. SD70 holds potential promise for ultimate use in prostate cancer therapy.

How to Use:

• In vitro: SD70 was used at 10 µM final concentration in various in vitro assays.
• In vivo: SD70 was administered by IP injection at 10 mg/kg once per day in xenografts model.

Reference:

1. 1.Jin C, et al. Chem-seq permits identification of genomic targets of drugs against androgen receptor regulation selected by functional phenotypic screens. (2014) Proc Natl Acad Sci USA. 111(25):9235-40.

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