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L-Moses | Antagonist of KAT2B, KAT2A
RATINGS:
Cellular Use: (6 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
KAT2B
  • Kd:48 nM
  • Ki:47 nM
  • Kd:126 nM
  • EC 50:256 nM
KAT2A
  • Kd:220 nM
  • Kd:550 nM
  • EC 50:256 nM
Antagonist
1-5 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
A selectivity thermal shift assay panel of 48 of the 61 expressed human Bromodomains was set up usin ...

Potency
Cellular
In Vitro

KAT2B

Mode of Action: Antagonist

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1002/anie.201610816

KAT2A

Mode of Action: Antagonist

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1002/anie.201610816

In Vivo Validations

Mouse
Dose: 10 mg/kg
Route of delivery: Oral
Plasma half life: 49 minutes
Systemic clearance: ND

DOI Reference: 10.1002/anie.201610816

Negative Control Compounds

D-Moses

Orthogonal Probes def

GSK4027

Chemical Information

Molecular Formula C21H25N6+
SMILEs Cc1[nH]nc2c3ccccc3c(N[C@@H](C)[C@H](c3ccccc3)N(C)C)n[n+]12
InChI InChI=1S/C21H24N6/c1-14(19(26(3)4)16-10-6-5-7-11-16)22-20-17-12-8-9-13-18(17)21-24-23-15(2)27(21)25-20/h5-14,19H,1-4H3,(H,22,25)/p+1/t14-,19+/m0/s1
Molecular weight 361.21 Da
AlogP 3.108320000000001
HBond acceptors 6
HBond donors 2
Atoms 52

References

Publications

Cross References

Vendors

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

Expert Reviews

by SERP
(on 19 Mar 2017 )
Cellular Use Rating
This is a good inhibitor developed against the PCAF bromodomain. Reasonably potent (Kd=100 nM by ITC) and selective against other BRDs by DSF. Although in this reviewer's opinion, this assay should...
by SERP
(on 27 Mar 2017 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
by SERP
(on 28 Mar 2017 )
Cellular Use Rating
This is a newly discovered probe molecule and as such there is not much data yet. The publication shows that the compound has good potency and selectivity, and the cellular target engagement assay shows...
by SERP
(on 10 Apr 2017 )
Cellular Use Rating
L-Moses is an ~200 nM inhibitor of the bromodomains present in PCAF and GCN5, which are 78% identical, but it does not inhibit/bind to other bromodomain-containing proteins. In cells, L-Moses displaced...
by SERP
(on 17 Apr 2017 )
Cellular Use Rating
The data in the primary publication are insufficient to meet the criteria for a high-quality chemical probe. Selectivity within the bromodomain family is only determined by DSF, rather than a more sensitive...
by SERP
(on 17 Apr 2017 )
Cellular Use Rating
The cellular activity for this probe is significantly weaker than for GSK4027, which currently represents the best probe for PCAF-Brd/GCN5 due to greater confidence in its selective on-target-mediated...
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