A G9a histone methyltransferase inhibitor
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UNC0642

Item No. 14604

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)Epigenetic Chemical Probe Guide (PDF)
Technical Information
Formal Name
2-(4,4-difluoropiperidin-1-yl)-N-(1-isopropylpiperidin-4-yl)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-amine
CAS Number
1481677-78-4
Molecular Formula
C29H44F2N6O2
Formula Weight
546.7
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 20 mg/mlEthanol: 2 mg/ml
λmax
214, 250, 276, 343 nm
SMILES
COC1=CC2=C(NC3CCN(C(C)C)CC3)N=C(N4CCC(F)(F)CC4)N=C2C=C1OCCCN5CCCC5
InChi Code
InChI=1S/C29H44F2N6O2/c1-21(2)36-14-7-22(8-15-36)32-27-23-19-25(38-3)26(39-18-6-13-35-11-4-5-12-35)20-24(23)33-28(34-27)37-16-9-29(30,31)10-17-37/h19-22H,4-18H2,1-3H3,(H,32,33,34)
InChi Key
RNAMYOYQYRYFQY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $69

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    5 mg

    $198

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    10 mg

    $297

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    Cayman Chemical
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    Product Description

    UNC0642 is a selective inhibitor of G9a and GLP that competitively inhibits binding of H3K9 substrates with a Ki = 3.7 nM. It exhibits >2,000-fold selectivity over the lysine methyltransferase EZH2 and >20,000-fold selectivity over other methyltransferases.1 UNC0642 has been shown to reduce H3K9 dimethylation levels in MDA-MB-231 and PANC-1 cells with IC50 values of 110 and 40 nM, respectively.1 Furthermore, it displays improved pharmacokinetic properties relative to UNC0638 (Item No. 10734).1 See the Structural Genomics Consortium (SGC) website for more information.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Liu, F., Barsyte-Lovejoy, D., Li, F., et al. Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP. J. Med. Chem. 56(21), 8931-8942 (2013).