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SGC0946 | Inhibitor of DOT1L
RATINGS:
Cellular Use: (4 reviews)

In Model Organisms: (0 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
DOT1L
  • Kd:0.06 nM
  • IC50:0.3 nM
  • IC50:8.8 nM
100 nM - 5 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Inactive against 12 protein methyltransferases and DNMT1
Selectivity Assessment Description:
No notable activity against 29 receptors from the Ricerca selectivity panel

Potency
Cellular
In Vitro

DOT1L

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1038/ncomms2281

Negative Control Compounds

SGC0649

Chemical Information

Molecular Formula C28H40BrN7O4
SMILEs CC(C)N(CCCNC(=O)Nc1ccc(C(C)(C)C)cc1)C[C@H]1O[C@@H](n2cc(Br)c3c(N)ncnc32)[C@H](O)[C@@H]1O
InChI InChI=1S/C28H40BrN7O4/c1-16(2)35(12-6-11-31-27(39)34-18-9-7-17(8-10-18)28(3,4)5)14-20-22(37)23(38)26(40-20)36-13-19(29)21-24(30)32-15-33-25(21)36/h7-10,13,15-16,20,22-23,26,37-38H,6,11-12,14H2,1-5H3,(H2,30,32,33)(H2,31,34,39)/t20-,22-,23-,26-/m1/s1
Molecular weight 617.23 Da
AlogP 3.614900000000002
HBond acceptors 11
HBond donors 6
Atoms 80

Vendors

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Expert Reviews

by SERP
(on 17 May 2016)
Cellular Use Rating
The inactive control SGC-0649 should only be used but at relatively low concentrations as it still retains some DOT1L activity (IC50 = 390 nM).
by SERP
(on 6 Jun 2016)
Cellular Use Rating
SGC0649 is now available as a control compound. It is the 4-t-butylphenylamide as opposed to the urea in SGC0946
by SERP
(on 10 Jun 2016)
Cellular Use Rating
This compound shows single digit nanomolar potency in cellular assays measuring reduction of H3K79me2. Downstream effects appear to require a higher concentration (1 - 5 micromolar). While concerns...
by SERP
(on 20 Jun 2016)
Cellular Use Rating
...
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