UNC0224 is a potent and selective inhibitor of G9a, a histone methyltransferase (HMT). It also inhibits GLP, a closely-related H3K9 HMT, but is more than 1,000-fold selective against SET7/9 and SET8.

≥98% by HPLC

UNC0224 inhibits G9a with an IC50 value of 15 nM. It has been shown to inhibit GLP with assay-dependent IC50 values of 20-58 nM.

Soluble in DMSO, DMF and ethanol, purged with an inert gas. Solubility in DMSO and DMF is approximately 2 mg/ml, and solubility in ethanol is ~15 mg/ml.

A crystalline solid.

Store at or below –20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.

1. Tachibana, M., et al., Genes Dev. 2002; 16:1779-1791.
2. Wagschal, A., et al., Mol. Cell. Biol. 2008; 28(3):1104-1113.
3. Thomas, L.R., et al., J. Immunol. 2008; 181:485-493.

Methyltransferase

Inhibitor