Cayman Chemical Item Number 10734

(CAS 1255580-76-7)

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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 UNC0638 is a potent G9a HMTase inhibitor, exhibiting an IC50 value of <15 nM in vitro. UNC0638 also inhibits GLP, a closely-related H3K9 HMTase, with an IC50 value of 19 nM, but is more than 10,000-fold selective against SET7/9 (a H3K4 HMTase), SET8 (a H4K20 HMTase), PRMT3, and SUV39H2. UNC0638 inhibits H3K9 dimethylation in MDA-MB231 cells with an IC50 value of 81 nM and demonstrates favorable separation of functional and toxic effects.4 See the Structural Genomics Consortium (SGC) website for more information.

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. unlisted. G9a/GLP selective methyltransferase chemical probe, UNC0638. (2010).

Formal Name 2-​cyclohexyl-​6-​methoxy-​N-​[1-​(1-​methylethyl)-​4-​piperidinyl]-​7-​[3-​(1-​pyrrolidinyl)propoxy]-​4-​quinazolinamine
CAS Number 1255580-76-7
Molecular Formula C30H47N5O2
Formula Weight 509.7
Formulation A crystalline solid
Purity ≥98%
λmax 216, 245, 320, 333 nm
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
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UNC0638 is available in the following screening library:

Size Price Quantity Subtotal
1 mg $38.00 $0.00
5 mg $95.00 $0.00
10 mg $171.00 $0.00
50 mg $770.00 $0.00
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Cart Total $0.00

Pricing updated 2015-07-31. Prices are subject to change without notice.

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Ann Arbor, Michigan 48108 USA


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