产品号 #72042_C
表观遗传修饰剂；抑制 G9a 组蛋白甲基转移酶
总览
BIX01294 是一种非常特异的 G9a（IC₅₀ = 1.9 µM）和 G9a 样（GLP，IC₅₀ = 0.7 µM）组蛋白甲基转移酶抑制剂。这些甲基转移酶靶向组蛋白 3（H3K9）上的赖氨酸 9 位。BIX01294 通过占据组蛋白结合位点，阻止其与组蛋白相互作用，从而抑制 G9a 和 GLP（Chang et al., Kubicek et al.）。本产品以三盐酸盐水合物形式提供。
重编程
·无需使用 c-Myc 和 SOX2，即可增强小鼠胚胎成纤维细胞或胎儿神经祖细胞重编程为诱导性多能干细胞（Shi et al. 2008a, Shi et al. 2008b）。
细胞类型
多能干细胞
种属
人，小鼠，非人灵长类，其它细胞系，大鼠
应用
重编程
研究领域
干细胞生物学
CAS 编号
1808255-64-2
化学式
C₂₈H₃₈N₆O₂ · 3HCl [XH₂O]
纯度
≥98%
通路
表观遗传学
靶点
组蛋白甲基转移酶
Protocols and Documentation
Find supporting information and directions for use in the Product Information Sheet or explore additional protocols below.
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
Educational Materials (3)
Publications (4)
Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294. 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. 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. Cell stem cell 2008 JUN
Abstract
更多信息
| Species | Human, Mouse, Non-Human Primate, Other, Rat |
|---|---|
| Cas Number | 1808255-64-2 |
| Chemical Formula | C₂₈H₃₈N₆O₂ · 3HCl [XH₂O] |
| Purity | ≥ 98% |
| Target | Histone Methyltransferase |
| Pathway | Epigenetic |
相关产品
-
ReproRNA™-OKSGM一种非整合型、自我复制的 RNA 重编程载体，用于生成诱导多能干细胞
-
3-Deazaneplanocin A表观遗传修饰剂；抑制组蛋白 EZH2 赖氨酸甲基转移酶
-
RepSox（盐酸盐）激活素/BMP/TGF-β通路抑制剂；抑制ALK5
PRODUCTS ARE FOR RESEARCH USE ONLY AND NOT INTENDED FOR HUMAN OR ANIMAL DIAGNOSTIC OR THERAPEUTIC USES UNLESS OTHERWISE STATED. FOR ADDITIONAL INFORMATION ON QUALITY AT STEMCELL, REFER TO WWW.STEMCELL.COM/COMPLIANCE.
