|Solubility:||DMSO up to 100 mM|
|Chemical Name:||N-(1-benzylpiperidin-4-yl)-6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine trihydrochloride|
|Storage:||Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.|
BIX-01294 is a potent and selective G9a and GLP histone lysine methyltransferase inhibitor with an IC50 ~0.7 μM and 1.7 μM respectively. It has no activity at other histone methyltransferases. BIX-01294 modulates H3K9me2 levels in mammalian cells and potentiates induction of pluripotent stem cells from somatic cells in vitro. It could reactivate expression of HIV-1 from latently infected cells such as ACH-2 and OM10.1, suggesting the involvement of histone H3 lysine 9 (H3K9) methyltransferase G9a in the maintenance of HIV-1 latency. It can also inhibit malaria parasite histone methyltransferases, resulting in rapid and irreversible parasite death.
How to Use:
In vitro: BIX-01294 was used at 10 µM in vitro and cellular assays.
In vivo: n/a
- Kubicek S, et al. Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase. (2007) Mol Cell. 25(3):473-81.
- Shi Y, et al. Induction of pluripotent stem cells from mouse embryonic fibroblasts by Oct4 and Klf4 with small-molecule compounds. (2008) Cell Stem Cell. 3(5):568-74.
- Chang Y, et al. Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294. (2009) Nat Struct Mol Biol. 16(3):312-7.
- Imai K, et al. Involvement of histone H3 lysine 9 (H3K9) methyltransferase G9a in the maintenance of HIV-1 latency and its reactivation by BIX01294. (2010) J Biol Chem. 285(22):16538-45.
- Malmquist NA, et al. Small-molecule histone methyltransferase inhibitors display rapid antimalarial activity against all blood stage forms in Plasmodium falciparum. (2012) Proc Natl Acad Sci USA. 109(41):16708-13.
- Kim Y, et al. BIX-01294 induces autophagy-associated cell death via EHMT2/G9a dysfunction and intracellular reactive oxygen species production. (2013) Autophagy. 9(12):2126-39.
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