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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 public comments)
by SERP
(on 21 Mar 2017)
Cellular Use Rating
(The reviewer did not leave any public 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