BIX01294 (hydrochloride hydrate)

Cayman Chemical Item Number 13124

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The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferase (HMTase) G9a can mono- or dimethylate lysine 9 on histone 3 (H3), contributing to early embryogenesis, genomic imprinting, and lymphocyte development.1,2,3 BIX01294 (hydrochloride hydrate) is a selective inhibitor of G9a HMTase (IC50 = 1.7 μM).4 It less effectively inhibits the HMTase G9a-like protein (GLP; IC50 = 38 μM) and has no effect on other known HMTases.4 BIX01294 has been used in combination with the calcium channel activator BayK8644 to facilitate the generation of induced pluripotent stem cells from somatic cells in vitro.5

1. Tachibana, M., Sugimoto, K., Nozaki, M., et al. G9a histone methyltransferase plays a dominant role in euchromatic histone H3 lysine 9 methylation and is essential for early embryogenesis. Genes Dev 16 1779-1791 (2002).

2. Wagschal, A., Sutherland, H.G., Woodfine, K., et al. G9a histone methyltransferase contributes to imprinting in the mouse placenta. Mol Cell Biol 28(3) 1104-1113 (2008).

3. Thomas, L.R., Miyashita, H., Cobb, R.M., et al. Functional analysis of histone methyltransferase G9a in B and T lymphocytes. J Immunol 181 485-493 (2008).

4. Kubicek, S., O'Sullivan, R.J., August, E.M., et al. Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase. Mol Cell 25 473-481 (2007).

5. Shi, Y., Desponts, C., Do, J.T., et al. Induction of pluripotent stem cells from mouse embryonic fibroblasts by Oct4 and Klf4 with small-molecule compounds. Cell Stem Cell 3(5) 568-574 (2008).

Formal Name 2-​(hexahydro-​4-​methyl-​1H-​1,​4-​diazepin-​1-​yl)-​6,​7-​dimethoxy-​N-​[1-​(phenylmethyl)-​4-​piperidinyl]-​4-​quinazolinamine,​ trihydrochloride,​ hydrate
Molecular Formula C28H38N6O2 • 3HCl [XH2O]
Formula Weight 600.0
Formulation A crystalline solid
Purity ≥98%
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
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Size Price Quantity Subtotal
1 mg $23.00 $0.00
5 mg $92.00 $0.00
10 mg $138.00 $0.00
50 mg $460.00 $0.00
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Cart Total $0.00

Pricing updated 2015-07-29. Prices are subject to change without notice.

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Warning This product is not for human or veterinary use.

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Cayman Chemical Company regularly evaluates our shipping methods to ensure product stability is maintained and our corporate environmental impact is minimized. Products selected for review are evaluated and shipping methods are certified by our Scientists. While occasionally our method of shipping a product may change, rest assured the shipping conditions on all Cayman Chemical products have been reviewed and validated.

Upon receipt, it is important to check the storage requirements of your products and place them at the appropriate temperature. Products shipped without ice may require frozen storage for long term stability.

Cayman Chemical was formed over thirty years ago by demonstrating the value of naturally growing gorgonian corals as a renewable, economically viable source of prostaglandins. Today we operate our business knowing that we owe our start to the renewable resources our environment had provided. As Cayman Chemical continues to grow we consistently evaluate our business processes to ensure we are operating at the highest environmental standards.

Cayman Chemical

1180 East Ellsworth Road

Ann Arbor, Michigan 48108 USA


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