MRK-990 | MRK-990 : Inhibitor of PRMT9, PRMT5
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (0 reviews)
In Vivo
Vendors

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
PRMT9
  • IC50:10 nM
  • IC50:145 nM
PRMT5
  • IC50:30 nM
  • IC50:519 nM
Inhibitor
up to 10 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Selectivity was assessed against 8 PRMTs at 1 and 10uM: PRMT7 and PMRT4 remaining activity of 20 and ...

Potency
Cellular
In Vitro

PRMT9

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

Other Reference: Peer reviewed at SGC

PRMT5

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

Other Reference: Peer reviewed at SGC

Negative Control Compounds

canSAR7437541
Notes: MRK-990-NC is a closely related negative control with IC50 > 10 micromolar.

Chemical Information

Molecular Formula C26H38N6O3S
SMILEs Cc1cn([C@@H]2O[C@H](CSCCCCNCc3cccnc3C(C)(C)C)[C@@H](O)[C@H]2O)c2ncnc(N)c12
InChI InChI=1S/C26H38N6O3S/c1-16-13-32(24-19(16)23(27)30-15-31-24)25-21(34)20(33)18(35-25)14-36-11-6-5-9-28-12-17-8-7-10-29-22(17)26(2,3)4/h7-8,10,13,15,18,20-21,25,28,33-34H,5-6,9,11-12,14H2,1-4H3,(H2,27,30,31)/t18-,20-,21-,25-/m1/s1
Molecular weight 514.27 Da
AlogP 2.936820000000001
HBond acceptors 9
HBond donors 5
Atoms 74

Expert Reviews


(on 7 Jun 2023 )
Cellular Use Rating
There are many tool compounds available to explore PRMT5 biology that modulate its activity selectively through a number of different binding modes. The value of MRK-990 comes from its PRMT9 cellular activity...
(on 23 Sept 2024 )
Cellular Use Rating
( The reviewer did not leave any comments )
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