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KMI169 | KMI169 : Inhibitor of N6AMT1
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
N6AMT1
  • Kd:25 nM
  • ΔTm:12.5 K
  • IC50:50 nM
  • ΔTm:9.8 K
  • ΔTm:8.3 K
  • GI50:150 nM
  • INH:1 µM
  • INH:1 µM
  • INH:1 µM
Inhibitor
2 µM
1 µM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Selectivity of 1.5 uM KMI169 was assessed against the full panel of SET-domain and Rossmann-fold met ...
In Cell Selectivity Assessment
Selectivity Assessment Description:
No effect on symmetric dimethyl arginine in PC-3M cells, indicating no inhibition of PRMT5. No effec ...

Potency
Cellular
In Vitro

N6AMT1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/s41467-023-44243-6

Negative Control Compounds

CANSAR4199061
Notes: Control compound didn't show any biochemical activity or cellular.

Chemical Information

Molecular Formula C31H31Cl2N7O2
SMILEs Nc1nc(Cl)nc2c1c(-c1nn(Cc3ccccc3)cc1Cl)cn2[C@@H]1C[C@H](c2cccc(CN3CCC3)c2)[C@@H](O)[C@H]1O
InChI InChI=1S/C31H31Cl2N7O2/c32-23-17-39(15-18-6-2-1-3-7-18)37-26(23)22-16-40(30-25(22)29(34)35-31(33)36-30)24-13-21(27(41)28(24)42)20-9-4-8-19(12-20)14-38-10-5-11-38/h1-4,6-9,12,16-17,21,24,27-28,41-42H,5,10-11,13-15H2,(H2,34,35,36)/t21-,24-,27-,28+/m1/s1
Molecular weight 603.19 Da
AlogP 0.0
HBond acceptors 9
HBond donors 4
Atoms 73

References

Publications

Cross References

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Vendors

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Expert Reviews

by SERP
(on 13 Feb 2024 )
Cellular Use Rating
KMI169 and its control compound KMI169 Ctrl were well characterized in vitro in terms of potency, target engagement, and selectivity. Their cellular activities were demonstrated with multiple sets of GI50...
by SERP
(on 20 Feb 2024 )
Cellular Use Rating
( The reviewer did not leave any comments )
by SERP
(on 5 Mar 2024 )
Cellular Use Rating
KMI169 is a well characterised probe with data from biophysical, biochemical and cellular assays which together with the inactive control compound provide valuable tools to enable exploration of KMT9 biology....
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