Biological Activity:

NSC636819 is a cell permeable and selective novel active-site KDM4A/KDM4B inhibitor with IC50 ~6.4 μM for KDM4A and 9.3 μM for KDM4B. It inhibits histone demethylase activity on H3K9me3 and induces apoptosis in LNCaP prostate cancer cells in vitro. It also negatively regulates androgen-responsive genes. The overexpression of KDM4A/KDM4B in prostate cancer and their association with androgen receptor suggest that KDM4A/KDM4B are potential progression factors for prostate cancer.

How to Use:

In vitro: NSC636819 was used at 10 µM final concentration in vitro and in cellular assays.
In vivo: n/a

Reference:

• 1. Chu CH, et al. KDM4B as a target for prostate cancer: structural analysis and selective inhibition by a novel inhibitor. (2014) J Med Chem. 57(14):5975-85.