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UNC3866 | UNC3866 : Antagonist of CBX7, CBX4
RATINGS:
Cellular Use: (3 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
CBX7
  • Kd:97 nM
  • IC 50:7.6 uM
CBX4
  • Kd:94 nM
  • IC 50:7.6 uM
Antagonist
30 uM

Selectivity

In Vitro Selectivity Assessment

Potency: KD - CBX2: 1.8 uM, CBX6: 0.610 uM, CBX8: 1.2 uM, CDY1: 6.3 uM, CDYL1b: 0.91 uM, CDYL2: 0.85 uM

Potency Assay Off-Target:
Isothermal titration calorimetry (ITC). We also profiled the compound on a microarray containing ...
Selectivity Assessment Description:
UNC3866 is selective over a broad range of chromatin-associated proteins (profiled versus 100+ Km ...
In Cell Selectivity Assessment

Potency:

Potency Assay Off-Target:
Assays to assess the cellular consequences of engaging the other non-PRC1 chromodomain targets (CDYs ...
Selectivity Assessment Description:
Assays to assess the cellular consequences of engaging the other non-PRC1 chromodomain targets (CDYs ...

Potency
Cellular
In Vitro

CBX7

Mode of Action: Antagonist

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/nchembio.2007

CBX4

Mode of Action: Antagonist

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/nchembio.2007

Negative Control Compounds

UNC4219

Chemical Information

Molecular Formula C43H66N6O8
SMILEs CCN(CC)CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(C(C)(C)C)cc1)C(=O)N[C@@H](CO)C(=O)OC
InChI InChI=1S/C43H66N6O8/c1-10-49(11-2)24-16-15-19-33(39(53)48-36(27-50)42(56)57-9)45-41(55)34(25-28(3)4)46-37(51)29(5)44-40(54)35(26-30-17-13-12-14-18-30)47-38(52)31-20-22-32(23-21-31)43(6,7)8/h12-14,17-18,20-23,28-29,33-36,50H,10-11,15-16,19,24-27H2,1-9H3,(H,44,54)(H,45,55)(H,46,51)(H,47,52)(H,48,53)/t29-,33-,34-,35-,36-/m0/s1
Molecular weight 794.49 Da
AlogP 3.0078
HBond acceptors 14
HBond donors 6
Atoms 123

References

Publications

Cross References

canSARChEMBLBindingDB

Vendors

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Expert Reviews

by SERP
(on 23 Oct 2016)
Cellular Use Rating
The probe UNC3866 has been well characterized for its interaction with the desired target CBX7 using ITC, a biotinylated analog, and co-crystal stuctures to provide strong evidence of interactions....
by SERP
(on 12 Jan 2017)
Cellular Use Rating
This probe is well-characterized and somewhat selective for CBX4 and CBX7 in biochemical assays, though it is only 6-fold less active against CBX6 and about 10-fold less active against CDYL1b and CDYL2....
by SERP
(on 21 Jan 2017)
Cellular Use Rating
UNC3866 is a first in class inhibitor for CBX7 and CBX4, as well as other related family members. It's highly potent in vitro and represents a great advancement in the CBX protein biology field. The...
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