BIX01294 (hydrochloride hydrate) is a selective inhibitor of G9a, a histone methyltransferase (HMT). It can also inhibit G9a-like protein (GLP), but is less effective. There are no known inhibitory effects on other HMTs. Also, BIX01294 has been used in combination with Bay-K8644 to facilitate generation of induced pluripotent stem cells from somatic cells in vitro.

≥98% by HPLC

BIX01294 inhibits G9a with an IC50 = 1.7 µM, and GLP with an IC50 = 38 µM.

Dissolve in water or other aqueous buffers. Solubility in water is ~20 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