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UNC6934 | UNC6934 : Antagonist of NSD2 PWWP domain
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
NSD2 (Other variant:N-terminal domain)
  • Kd:91 ± 8 nM
  • IC50:104 ± 13 nM
  • IC50:78 ± 29 nM
  • EC50:1230 ± 250 nM
Antagonist
up to 5 µM for longer incubation times as no cytotoxicity has been observed up to this concentration; up to 12.5 µM, which is 10-fold the cellular IC50 in U2OS cells
up to 10 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
UNC6934 is selective for NSD2-PWWP1 over 15 other human PWWP domains (assessed by differential scann ...

Potency
Cellular
In Vitro

NSD2 (Other variant:N-terminal domain)

Mode of Action: Antagonist

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/s41589-021-00898-0

Negative Control Compounds

UNC7145
Notes: Cpd 4 Kd > 20000 nM
SMILES: O=C1COc2c(N1)ccc(C(N(C(C)C)Cc3ccc(C(Nc4ncncc4)=O)cc3)=O)c2

Chemical Information

Molecular Formula C24H21N5O4
SMILEs O=C1COc2cc(C(=O)N(Cc3ccc(C(=O)Nc4ccncn4)cc3)C3CC3)ccc2N1
InChI InChI=1S/C24H21N5O4/c30-22-13-33-20-11-17(5-8-19(20)27-22)24(32)29(18-6-7-18)12-15-1-3-16(4-2-15)23(31)28-21-9-10-25-14-26-21/h1-5,8-11,14,18H,6-7,12-13H2,(H,27,30)(H,25,26,28,31)
Molecular weight 443.16 Da
AlogP 2.864600000000001
HBond acceptors 9
HBond donors 2
Atoms 54

Expert Reviews

by SERP
(on 13 Jan 2023 )
Cellular Use Rating
UNC6934 is a well-characterized selective probe for Nuclear receptor-binding SET domain containing 2 (NSD2-PWWP1). NSD2 is the responsible for the dimethylation of lysine 36 of histone 3 and is overexpressed...
by SERP
(on 22 Jan 2023 )
Cellular Use Rating
UNC7142 offers a helpful probe to investigate the mechanisms and phenotypes of NSD2 inhibition in the cellular context. When used in parallel with the reported and closely related inactive control, the...
by SERP
(on 30 Jan 2023 )
Cellular Use Rating
This probe, as well as its control compound, has been rigorously assessed with orthogonal biochemical and cellular methods as the blocker of the PWWP domain of NDS2 in terms of target engagement and potential...
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