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EPZ020411 | Inhibitor of PRMT6
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
PRMT6
  • IC50:0.010 uM
  • IC50:0.0637 uM
Inhibitor
40 nM - 1 uM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - PRMT8 0.223 uM, PRMT1 0.119 uM

Potency Assay Off-Target:
Same as on-target assay. The probe was also >100-fold selective against other methyltransferases, in ...
Selectivity Assessment Description:
Unknown
In Cell Selectivity Assessment
Potency Assay Off-Target:
The probe was 10-fold selective for PRMT6 > PRMT1 by comparing methylation of PRMT6-specific substra ...
Selectivity Assessment Description:
Unknown

Potency
Cellular
In Vitro

PRMT6

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

In Vivo Validations

male Sprague-Dawley rats
Dose: 5 mg/mL
Route of delivery: Subcutaneous
Plasma half life: 9.19 h

Reference: --

Chemical Information

Molecular Formula C25H38N4O3
SMILEs CNCCN(C)Cc1c[nH]nc1-c1ccc(O[C@H]2C[C@H](OCCC3CCOCC3)C2)cc1
InChI 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-
Molecular weight 442.29 Da
AlogP 0.0
HBond acceptors 7
HBond donors 2
Atoms 70

References

Publications

    Cross References

    canSARChEMBLBindingDBPDB

    Vendors

    Note: This is not an exhaustive list and does not indicate endorsement by the portal.

    Expert Reviews

    by SERP
    (on 30 May 2016 )
    Cellular Use Rating
    In Model Organisms
    EPZ020411 is not greatly selective for PRMT6 over PRMT1 or PRMT8 in vitro. PRMT6 is the only PRMT known to methylate the H3R2 position, and EPZ020411 can be used as a probe to assess the functionality...
    by SERP
    (on 6 Jun 2016 )
    Cellular Use Rating
    In Model Organisms
    Selectivity over some other isoforms of arginine methyltransferase is limited 10 - 20 fold. No data is available on CNS exposure of EPZ02041.
    by SERP
    (on 15 Jun 2017 )
    Cellular Use Rating
    In Model Organisms
    EPZ020411 is a potent inhibitor of PRMT6 in biochemical (IC50 = 10 nM) and cellular (IC50 = 600 nM) assays EPZ020411 is selective against the related enzymes PRMT3, PRMT4, PRMT5, and PRMT7 in a biochemical...
    Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria