KDM5-C70,JARID1HistoneDemethylasesInhibitor

Biological Activity:

KDM5-C70 is an ethyl ester derivative of KDM5-C49, which is a potent and selective inhibitor of Jumonji AT-Rich Interactive Domain 1 (JARID1) histone demethylases. The highly polar carboxylate group of KDM5-C49 restricts its cellular permeability; therefore KDM5-C70 was developed as a pro-drug, masking the polarity of the acid group of the KDM5-C49, for cellular assays and in vivo use. KDM5-C70 increases H3K4me3 levels in myeloma cells. Treatment of MCF7 and MDA-MB-231 breast cancer cells with KDM5-C70 significantly increased global levels of H3K4me3 while having little impact on H3K4me2/me1 or modifications regulated by other histone lysine demethylases.

How to Use:

In vitro: KDM5-C70 was used at 1-10 µM in vitro and cellular assays.
In vivo: possible use for in vivo study (IP dosing 15-50 mg/kg, bid)

Reference:

• 1. Marc Labelle, et al. Inhibitors of Histone Demethylases. (2014). PCT WO 2014053491
• 2. Johansson C, et al. Structural analysis of human KDM5B guides histone demethylase inhibitor development. (2016) Nat Chem Biol. 12(7):539-45. 
• 3. Horton JR, et al. Structural Basis for KDM5A Histone Lysine Demethylase Inhibition by Diverse Compounds. (2016) Cell Chem Biol. 23(7):769-81. 

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