A G9a and GLP inhibitor
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UNC0321

Item No. 41100

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
7-[2-[2-(dimethylamino)ethoxy]ethoxy]-2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6-methoxy-N-(1-methyl-4-piperidinyl)-4-quinazolinamine
CAS Number
1238673-32-9
Molecular Formula
C27H45N7O3
Formula Weight
515.7
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Slightly Soluble: 0.1-1 mg/mlEthanol: Sparingly Soluble: 1-10 mg/mlPBS (pH 7.2): Sparingly Soluble: 1-10 mg/ml
SMILES
COC1=CC2=C(NC3CCN(C)CC3)N=C(N=C2C=C1OCCOCCN(C)C)N4CCCN(C)CC4
InChi Code
InChI=1S/C27H45N7O3/c1-31(2)15-16-36-17-18-37-25-20-23-22(19-24(25)35-5)26(28-21-7-11-33(4)12-8-21)30-27(29-23)34-10-6-9-32(3)13-14-34/h19-21H,6-18H2,1-5H3,(H,28,29,30)
InChi Key
AULLUGALUBVBDD-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    5 mg

    $109

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    10 mg

    $196

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    25 mg

    $382

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    50 mg

    $600

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    Product Description

    UNC0321 is an inhibitor of the histone methyltransferases G9a and G9a-like protein (GLP; IC50s = 9 and 15 nM, respectively).1 It is selective for G9a and GLP over SET domain-containing protein 7 (SET7), SET8, protein arginine methyltransferase 3 (PRMT3), and jumonji domain-containing 2E (JMJD2E; IC50s = >10,000 nM for all). UNC0321 decreases the levels of dimethylated lysine 9 on histone H3 (H3K9me2) in MDA-MB-231 cells (IC50 = 11 µM) without inducing cytotoxicity (EC50 = >40 µM).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Liu, F., Chen, X., Allali-Hassani, A., et al. Protein lysine methyltransferase G9a inhibitors: Design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines. J. Med. Chem. 53(15), 5844-5857 (2010).

    2. 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).