An inhibitor of G9a/GLP methyltransferases
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UNC0646

Item No. 11085

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(1-cyclohexyl-4-piperidinyl)-2-[hexahydro-4-(1-methylethyl)-1H-1,4-diazepin-1-yl]-6-methoxy-7-[3-(1-piperidinyl)propoxy]-4-quinazolinamine
CAS Number
1320288-17-2
Molecular Formula
C36H59N7O2
Formula Weight
621.9
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 5 mg/mlEthanol: 30 mg/mlEthanol:PBS(pH 7.2) (1:1): 0.5 mg/ml
λmax
213, 250, 348 nm
SMILES
CC(C)N(CCC1)CCN1C2=NC(C=C(OCCCN3CCCCC3)C(OC)=C4)=C4C(NC(CC5)CCN5C6CCCCC6)=N2
InChi Code
InChI=1S/C36H59N7O2/c1-28(2)41-19-10-20-43(24-23-41)36-38-32-27-34(45-25-11-18-40-16-8-5-9-17-40)33(44-3)26-31(32)35(39-36)37-29-14-21-42(22-15-29)30-12-6-4-7-13-30/h26-30H,4-25H2,1-3H3,(H,37,38,39)
InChi Key
OUKWLRHRXOPODD-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $53

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    5 mg

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    10 mg

    $231

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    50 mg

    $1,030

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    Product Description

    G9a and G9a-like protein (GLP) are euchromatic histone-lysine methyltransferases (EHMT2 and EHMT1, respectively) that can heterodimerize with each other to methylate several proteins in addition to histone H3. UNC0646 is a potent and selective inhibitor of G9a and GLP activities in vitro (IC50s = 6 and 15 nM, respectively) and G9a/GLP-mediated dimethylation of histone 3 on lysine 9 in MDA-MB-231 cells (IC50 = 26 nM).1 It is highly selective for G9a/GLP over several other protein lysine and arginine methyltransferases.1 UNC0646 potently inhibits G9a/GLP activity in a variety of cancer cell lines as well as in the human fetal lung IMR-90 line.1 This compound selectively targets the corepressor function of G9a without affecting its ability to act as a coactivator with glucocorticoid receptor.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Liu, F., Barsyte-Lovejoy, D., Allali-Hassani, A., et al. Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. J. Med. Chem. 54(17), 6139-6150 (2011).

    2. Bittencourt, D., Wu, D.Y., Jeong, K.W., et al. G9a functions as a molecular scaffold for assembly of transcriptional coactivators on a subset of glucocorticoid receptor target genes. Proc. Natl. Acad. Sci. USA 109(48), 19673-19678 (2012).