| Molecular Weight: | 336.43 |
| Formula: | C17H28N4O3 |
| Purity: | ≥98% |
| CAS#: | n/a |
| Solubility: | DMSO up to 100 mM |
| Chemical Name: | ethyl 2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-oxoethyl)amino)methyl)isonicotinate |
| Storage: | Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year. |
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.
