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LP99 | Antagonist of BRD9, BRD7
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
BRD9
  • Kd:99 nM
  • IC 50:3300 nM
BRD7
  • Kd:909 nM
  • IC 50:3700 nM
Antagonist
up to 10 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Differential scanning fluorimetry assay
Selectivity Assessment Description:
LP99 was active only against BRD7 and BRD9 out of 48 human bromodomains.

Potency
Cellular
In Vitro

BRD9

Mode of Action: Antagonist

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1002/anie.201501394

BRD7

Mode of Action: Antagonist

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1002/anie.201501394

Negative Control Compounds

2S,3R-enantiomer

Orthogonal Probes def

VZ185

Chemical Information

Molecular Formula C26H30ClN3O4S
SMILEs Cc1cc(=O)n(C)c2cc(N3C(=O)CC[C@H](NS(=O)(=O)CC(C)C)[C@H]3c3ccc(Cl)cc3)ccc12
InChI InChI=1S/C26H30ClN3O4S/c1-16(2)15-35(33,34)28-22-11-12-24(31)30(26(22)18-5-7-19(27)8-6-18)20-9-10-21-17(3)13-25(32)29(4)23(21)14-20/h5-10,13-14,16,22,26,28H,11-12,15H2,1-4H3/t22-,26+/m0/s1
Molecular weight 515.16 Da
AlogP 0.0
HBond acceptors 7
HBond donors 1
Atoms 65

References

Publications

Cross References

canSARChEMBLBindingDBPDBPubMedPubMed

Vendors

Note: This is not an exhaustive list and does not indicate endorsement by the portal.

Expert Reviews

by SERP
(on 10 Aug 2016 )
Cellular Use Rating
LP99 is the first published selective inhibitor of BRD9 and BRD7 (ITC Kd BRD9 = 99 nM vs. ITC Kd BRD7 = 909 nM). It is selective against a panel of 48 bromodomains, with only BRD9 and BRD7 showing significant...
by SERP
(on 8 Sept 2016 )
Cellular Use Rating
LP99 is a selective inhibitor of BRD9 (KD = 99 nM) and BRD7 (KD = 909 nM) with good selectivity against a panel of 48 bromodomains at 10 uM and with cellular activity in the low uM range. The availability...
by SERP
(on 5 Apr 2017 )
Cellular Use Rating
The chemical probe LP99 was the first in its class, and this was an important achievement. The Structural Genomics Consortium (SGC) has setup a list of criteria for chemical probes. Two of these are...
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