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MIV-6R | MIV-6R : Menin-MLL PPI inhibitor of KMT2A
RATINGS:
Cellular Use: (3 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
KMT2A
  • KD:85 nM
  • GI50:1.1 uM
PPI
up to 10 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Not available

Potency
Cellular
In Vitro

KMT2A

Mode of Action: PPI

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/jm401868d

Negative Control Compounds

MIC-nc

Chemical Information

Molecular Formula C27H35N3O
SMILEs N#Cc1ccc(OCCCN2CCC([C@@](N)(c3ccccc3)C3CCCC3)CC2)cc1
InChI InChI=1S/C27H35N3O/c28-21-22-11-13-26(14-12-22)31-20-6-17-30-18-15-25(16-19-30)27(29,24-9-4-5-10-24)23-7-2-1-3-8-23/h1-3,7-8,11-14,24-25H,4-6,9-10,15-20,29H2/t27-/m1/s1
Molecular weight 417.28 Da
AlogP 0.0
HBond acceptors 4
HBond donors 2
Atoms 66

References

Publications

Cross References

canSARChEMBLBindingDBPDB

Vendors

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Expert Reviews

by SERP
(on 11 Sept 2016 )
Cellular Use Rating
In Model Organisms
This compound has nice SAR and structure-based probe design. More testing for off-target activities is needed for MIV-6R, which should encompass cell-based and biochemical assays.
by SERP
(on 20 Jan 2017 )
Cellular Use Rating
( The reviewer did not leave any comments )
by SERP
(on 18 Apr 2018 )
Cellular Use Rating
MIV-6R is a Menein-MLL PPI inhibitor with good in vitro activity. Compound inhibited cell proliferation and induced hematopoietic differentiation in MLL Leukemia cells. It also reduces the expression...
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