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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

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Targets Biochemical/Biophysical Potency Cellular Potency
PRMT6
  • IC50:10 nM
  • IC50:63.7 nM
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

DOI Reference: 10.1021/acsmedchemlett.5b00071

In Vivo Validations

Rat
Dose: 5 mg/mL
Route of delivery: Subcutaneous
Plasma half life: 9.19 h
Cmax: 844 ng/mL
Tmax: 0.444 h
Area Under the Curve:: 2775 h·ng/mL
Bioavailability: 65.6%

DOI Reference: 10.1021/acsmedchemlett.5b00071

Dose: 1 mg/Kg
Route of delivery: Intravenous
Plasma half life: 8.54 h
Systemic clearance: 19.7 mL/min/kg
Area Under the Curve:: 846 h·ng/mL
Volume of Distribution at Steady-State: 11.1 L/Kg

DOI Reference: 10.1021/acsmedchemlett.5b00071

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 3.471000000000002
HBond acceptors 7
HBond donors 2
Atoms 70

References

Publications

Cross References

ChEMBL BindingDB PDB canSAR

Vendors

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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...
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