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DS-437 | DS-437 : SAM competitive inhibitor of PRMT5, PRMT7
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (1 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
PRMT5
  • IC50:5900 nM
  • IC50:25000 nM
  • IC 50:1000 nM
PRMT7
  • IC50:6000 nM
  • IC50:37000 nM
  • IC 50:8000 nM
SAM competitive
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Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
DS-437 was inactive against a panel of 27 protein, RNA and DNA methyltransferases with residual acti ...

Potency
Cellular
In Vitro

PRMT5

Mode of Action: SAM competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/ml500467h

PRMT7

Mode of Action: SAM competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/ml500467h

Orthogonal Probes def

GSK591
EPZ015666

Chemical Information

Molecular Formula C15H23N7O4S
SMILEs CCNC(=O)NCCSC[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O
InChI InChI=1S/C15H23N7O4S/c1-2-17-15(25)18-3-4-27-5-8-10(23)11(24)14(26-8)22-7-21-9-12(16)19-6-20-13(9)22/h6-8,10-11,14,23-24H,2-5H2,1H3,(H2,16,19,20)(H2,17,18,25)/t8-,10-,11-,14-/m1/s1
Molecular weight 397.15 Da
AlogP -0.9199999999999986
HBond acceptors 11
HBond donors 6
Atoms 50

References

Publications

Cross References

Vendors

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Expert Reviews

by SERP
(on 18 Aug 2016)
Cellular Use Rating
(The reviewer did not leave any public comments)
by SERP
(on 3 Jan 2017)
Cellular Use Rating
This compound has not been used in animals. DS-437 exhibits an IC50 of 6 uM in vitro and is a dual inhibitor of PRMT5 and PRMT7. In the original publication, this compound is proposed as a chemical...
by SERP
(on 5 Jan 2017)
Cellular Use Rating
In Model Organisms
DS-437 is the only dual inhibitor for PRMT5 and PRMT7, and currently the only (documented) SAM-competitive inhibitor of PRMT5. Given the growing importance of both methyltransferases, especially with...
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