A potent inhibitor of G9a histone methyltransferase
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UNC0224

Item No. 13631

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
7-[3-(dimethylamino)propoxy]-2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6-methoxy-N-(1-methyl-4-piperidinyl)-4-quinazolinamine
CAS Number
1197196-48-7
Molecular Formula
C26H43N7O2
Formula Weight
485.7
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 2.5 mg/mlDMSO: 2 mg/mlEthanol: 15 mg/mlPBS (pH 7.2): 2.5 mg/ml
λmax
251, 346 nm
SMILES
COC1=CC2=C(NC3CCN(C)CC3)N=C(N4CCN(C)CCC4)N=C2C=C1OCCCN(C)C
InChi Code
InChI=1S/C26H43N7O2/c1-30(2)10-7-17-35-24-19-22-21(18-23(24)34-5)25(27-20-8-13-32(4)14-9-20)29-26(28-22)33-12-6-11-31(3)15-16-33/h18-20H,6-17H2,1-5H3,(H,27,28,29)
InChi Key
XIVUGRBSBIXXJE-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

    $129

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    10 mg

    $231

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    50 mg

    $1,030

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    Product 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 UNC0224 is a potent and selective G9a HMTase inhibitor, exhibiting an IC50 value of 15 nM.4 Isothermal titration calorimetry revealed UNC0224 binds to G9a with a Kd value of 29 nM. UNC0224 also inhibits GLP, a closely-related H3K9 HMTase, with assay-dependent IC50 values of 20-58 nM, but is more than 1,000-fold selective against SET7/9 (a H3K4 HMTase) and SET8 (a H4K20 HMTase).4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    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(14), 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(1), 485-493 (2008).

    4. Liu, F., Chen, X., Allali-Hassani, A., et al. Discovery of a 2,4-diamino-7-aminoalkoxyquinazoline as a potent and selective inhibitor of histone lysine methyltransferase G9a. J. Med. Chem. 52(24), 7950-7953 (2009).