A PRMT6 inhibitor
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EPZ020411

Item No. 19160

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N1,N2-dimethyl-N1-[[3-[4-[[trans-3-[2-(tetrahydro-2H-pyran-4-yl)ethoxy]cyclobutyl]oxy]phenyl]-1H-pyrazol-4-yl]methyl]-1,2-ethanediamine
CAS Number
1700663-41-7
Molecular Formula
C25H38N4O3
Formula Weight
442.6
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 5 mg/mlEthanol: 1 mg/mlPBS (pH 7.2): 0.3 mg/ml
λmax
250 nm
SMILES
CN(CCNC)CC1=CNN=C1C(C=C2)=CC=C2O[C@H](C3)C[C@@H]3OCCC4CCOCC4
InChi Code
InChI=1S/C25H38N4O3/c1-26-10-11-29(2)18-21-17-27-28-25(21)20-3-5-22(6-4-20)32-24-15-23(16-24)31-14-9-19-7-12-30-13-8-19/h3-6,17,19,23-24,26H,7-16,18H2,1-2H3,(H,27,28)/t23-,24-
InChi Key
QMDKVNSQXPVCRD-RQNOJGIXSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $52

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    5 mg

    $227

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    10 mg

    $396

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    25 mg

    $867

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    Product Description

    EPZ020411 is an inhibitor of protein arginine methyltranferase 6 (PRMT6; IC50 = 10 nM) that less potently targets PRMT1 and PRMT8 (IC50s = 119 and 223 nM, respectively).1 It dose-dependently decreases methylation of the PRMT6 substrate H3R2 in A375 cells transiently expressing PRMT6 (IC50 = 0.637 µM).1 EPZ020411 shows a moderate clearance rate in rats following intravenous bolus administration, and, following 5 mg/kg subcutaneous dosing, has an unbound blood concentration exceeding the PRMT6 biochemical IC50 value for more than 12 hours.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Mitchell, L.H., Drew, A.E., Ribich, S.A., et al. Aryl pyrazoles as potent inhibitors of arginine methyltransferases: Identification of the first PRMT6 tool compound. ACS Med. Chem. Lett. 6(6), 655-659 (2015).