Daminozide

A dimethylamino substituted succinamate that, in addition to its well known use as a plant growth regulator, also acts as an inhibitor against histone lysine demthylases KDM2A, LSD1 (KDM7A; KIAA1718), and PHF8 (IC₅₀ = 1.5, 2.1, and 0.55 µM, respectively), but not KDM3A, KDM4E, KDM5C, KDM6B, or three hydroxylases (IC₅₀ >100 µM). Substrate-competition and/or active site Iron chelating likely accounts for the inhibitory activity against the FAD-dependent LSD1, while 2-oxoglutarate (2-OG) competition (K_i = 1.97 µM) appears as the major mode of action against KDM2A.

A dimethylamino substituted succinamic acid compound that, in addition to its well known use as a plant growth regulator, also acts as an inhibitor against histone lysine demthylases KDM2A, LSD1 (KDM7A; KIAA1718), and PHF8 (IC₅₀ = 1.5, 2.1, and 0.55 µM, respectively), but not KDM3A, KDM4E, KDM5C, KDM6B, (IC₅₀ >100 µM) or three hydroxylases (FIH, PHD2, and BBOX1; IC₅₀ >100 µM). Although kinetic studies indicate 2-oxoglutarate (2-OG) competition (K_i = 1.97 µM) as the major mode of action against KDM2A, substrate-competition and/or active site Iron chelation more likely accounts for the compound′s inhibitory activity against the FAD-dependent LSD1.

Packaged under inert gas

Toxicity: Harmful & Carcinogenic / Teratogenic (E)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Rose, N.R., et al. 2012. J. Med. Chem.55, 6639.

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