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A-196 | A-196 : Inhibitor of KMT5B, KMT5C
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
KMT5B
  • IC 50:25 nM
  • EC 50:740 nM (activating H4K20me1); 262 nM (inhibiting H4K20me2); 370 nM (inhibiting H4K20me3)
KMT5C
  • IC 50:144 nM
  • EC 50:740 nM (activating H4K20me1); 262 nM (inhibiting H4K20me2); 370 nM (inhibiting H4K20me3)
Inhibitor
500-1000 nM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50

Potency Assay Off-Target:
Scintillation proximity assay. No activity was detected in assays with 29 methyltransferases at 1 or ...
Selectivity Assessment Description:
125 non-family targets including kinases, GPCRs, ion channels, and transporters (via Cerep and th ...

Potency
Cellular
In Vitro

KMT5B

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/nchembio.2282

KMT5C

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/nchembio.2282

Negative Control Compounds

A-197
SGC2043
SMILES: CN(C1CCCC1)C2=NN=C(C3=CC=NC=C3)C4=C2C=C(C(=C4)Cl)Cl

Chemical Information

Molecular Formula C18H16Cl2N4
SMILEs Clc1cc2c(NC3CCCC3)nnc(-c3ccncc3)c2cc1Cl
InChI InChI=1S/C18H16Cl2N4/c19-15-9-13-14(10-16(15)20)18(22-12-3-1-2-4-12)24-23-17(13)11-5-7-21-8-6-11/h5-10,12H,1-4H2,(H,22,24)
Molecular weight 358.08 Da
AlogP 5.353100000000003
HBond acceptors 4
HBond donors 1
Atoms 40

References

Publications

Cross References

canSARChEMBLBindingDBPDB

Vendors

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Expert Reviews

by SERP
(on 15 Mar 2017 )
Cellular Use Rating
( The reviewer did not leave any comments )
by SERP
(on 21 Mar 2017 )
Cellular Use Rating
( The reviewer did not leave any comments )
by SERP
(on 30 Mar 2017 )
Cellular Use Rating
In Model Organisms
This probe represents the best in class for SUV420H1 and H2 - hitting the enzymes at 25 and 144 nM, respectively, with selectivity data against a wide panel of related epigenetic and other targets....
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