BIX01294

Epigenetic modifier; Inhibits G9a histone methyltransferase

BIX01294

Epigenetic modifier; Inhibits G9a histone methyltransferase

From: 70 USD
Catalog #
72042_C
Epigenetic modifier; Inhibits G9a histone methyltransferase

Overview

BIX01294 is a very specific inhibitor of the G9a (IC₅₀ = 1.9 µM) and G9a-like (GLP, IC₅₀ = 0.7 µM) histone methyltransferases. These methyltransferases target the lysine 9 position on histone 3 (H3K9). BIX01294 inhibits G9a and GLP by occupying the histone binding site, preventing interaction with histones (Chang et al., Kubicek et al.). This product is supplied as the trihydrochloride hydrate form of the molecule.

REPROGRAMMING
· Enhances reprogramming of mouse embryonic fibroblasts or fetal neural progenitor cells to induced pluripotent stem cells without using c-Myc and SOX2 (Shi et al. 2008a, Shi et al. 2008b).
Alternative Names
Not applicable
Cell Type
Pluripotent Stem Cells
Species
Human, Mouse, Rat, Non-Human Primate, Other
Application
Reprogramming
Area of Interest
Stem Cell Biology
CAS Number
1808255-64-2
Chemical Formula
C₂₈H₃₈N₆O₂ · 3HCl [XH₂O]
Molecular Weight
600.0 g/mol (anhydrous basis)
Purity
≥ 98%
Pathway
Epigenetic
Target
Histone Methyltransferase

Protocols and Documentation

Find supporting information and directions for use in the Product Information Sheet or explore additional protocols below.

Document Type
Product Name
Catalog #
Lot #
Language
Catalog #
72042, 72044
Lot #
All
Language
English
Catalog #
72042, 72044
Lot #
All
Language
English
Document Type
Safety Data Sheet
Catalog #
72042, 72044
Lot #
All
Language
English

Applications

This product is designed for use in the following research area(s) as part of the highlighted workflow stage(s). Explore these workflows to learn more about the other products we offer to support each research area.

Resources and Publications

Publications (4)

Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294. Chang Y et al. Nature structural & molecular biology 2009 MAR

Abstract

Histone lysine methylation is an important epigenetic mark that regulates gene expression and chromatin organization. G9a and G9a-like protein (GLP) are euchromatin-associated methyltransferases that repress transcription by methylating histone H3 Lys9. BIX-01294 was originally identified as a G9a inhibitor during a chemical library screen of small molecules and has previously been used in the generation of induced pluripotent stem cells. Here we present the crystal structure of the catalytic SET domain of GLP in complex with BIX-01294 and S-adenosyl-L-homocysteine. The inhibitor is bound in the substrate peptide groove at the location where the histone H3 residues N-terminal to the target lysine lie in the previously solved structure of the complex with histone peptide. The inhibitor resembles the bound conformation of histone H3 Lys4 to Arg8, and is positioned in place by residues specific for G9a and GLP through specific interactions.
Induction of pluripotent stem cells from mouse embryonic fibroblasts by Oct4 and Klf4 with small-molecule compounds. Shi Y et al. Cell stem cell 2008 NOV

Abstract

Somatic cells can be induced into pluripotent stem cells (iPSCs) with a combination of four transcription factors, Oct4/Sox2/Klf4/c-Myc or Oct4/Sox2/Nanog/LIN28. This provides an enabling platform to obtain patient-specific cells for various therapeutic and research applications. However, several problems remain for this approach to be therapeutically relevant due to drawbacks associated with efficiency and viral genome integration. Recently, it was shown that neural progenitor cells (NPCs) transduced with Oct4/Klf4 can be reprogrammed into iPSCs. However, NPCs express Sox2 endogenously, possibly facilitating reprogramming in the absence of exogenous Sox2. In this study, we identified a small-molecule combination, BIX-01294 and BayK8644, that enables reprogramming of Oct4/Klf4-transduced mouse embryonic fibroblasts, which do not endogenously express the factors essential for reprogramming. This study demonstrates that small molecules identified through a phenotypic screen can compensate for viral transduction of critical factors, such as Sox2, and improve reprogramming efficiency.
A combined chemical and genetic approach for the generation of induced pluripotent stem cells. Shi Y et al. Cell stem cell 2008 JUN

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