A selective SET8 inhibitor
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UNC0379

Item No. 16400

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6,7-dimethoxy-2-(1-pyrrolidinyl)-N-[5-(1-pyrrolidinyl)pentyl]-4-quinazolinamine
CAS Number
1620401-82-2
Molecular Formula
C23H35N5O2
Formula Weight
413.6
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 10 mg/ml
λmax
210, 249, 345 nm
SMILES
COC1=C(OC)C=C(N=C(N2CCCC2)N=C3NCCCCCN4CCCC4)C3=C1
InChi Code
InChI=1S/C23H35N5O2/c1-29-20-16-18-19(17-21(20)30-2)25-23(28-14-8-9-15-28)26-22(18)24-10-4-3-5-11-27-12-6-7-13-27/h16-17H,3-15H2,1-2H3,(H,24,25,26)
InChi Key
WEXCGGWTIDNVNT-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $61

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    10 mg

    $104

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    25 mg

    $242

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    Product Description

    UNC0379 is a substrate-competitive inhibitor of the lysine methyltransferase SET8 (IC50 = 7.3 µM; Kd = 18.3 µM).1 It is selective for SET8 over 15 other methyltransferases, including G9a and GLP (IC50s = >100 µM).1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ma, A., Yu, W., Li, F., et al. Discovery of a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8. J. Med. Chem. (2014).