UNC0638

Cayman Chemical Item Number 10734

(CAS 1255580-76-7)

UNC0638 (CAS 1255580-76-7)

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Description

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

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%
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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CC(C)​N(CC1)​CCC1NC2=NC(C3CCCCC3)​=NC4=CC(OCCCN5CCCC5)​=C(OC)​C=C42
InCHI Code
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QOECJCJVIMVJGX-UHFFFAOYSA-N
InCHI Key
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QOECJCJVIMVJGX-UHFFFAOYSA-N

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UNC0638 is available in the following screening library:

Size Price Quantity Subtotal
1 mg $38.00 $0.00
5 mg $108.00 $0.00
10 mg $168.00 $0.00
50 mg $780.00 $0.00
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Cart Total $0.00

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Pricing updated 2014-04-24. Prices are subject to change without notice.

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