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 0.55uM, respectively), but not KDM3A, KDM4E, KDM5C, KDM6B, or three hydroxylases (IC50 >100uM). 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 (Ki = 1.97uM) appears as the major mode of action against KDM2A.
Formula:C6H12N2O3
Solubility:H2O
Molar Mass:160.2
Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.
