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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 public 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