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MRK-740 | Inhibitor of PRDM9
RATINGS:
Cellular Use: (2 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
PRDM9
  • IC50:80 ± 16 nM
  • IC50:0.8 uM
Inhibitor
up to 3 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Enzyme Activity Assay
Selectivity Assessment Description:
Selectivity against 32 methyltransferases (MTs) were tested at 1 µM and 10 µM of compounds. PRDM9 wa ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
Eurofins Panlabs
Selectivity Assessment Description:
MRK-740 was profiled in a customized panel of 108 enzymes and receptors at Eurofins Panlabs Discover ...

Potency
Cellular
In Vitro

PRDM9

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

Negative Control Compounds

MRK-740-NC

Chemical Information

Molecular Formula C25H32N6O3
SMILEs COc1cc(OC)cc(-c2noc(N3CCN(C)C4(CCN(c5ccnc(C)c5)CC4)C3)n2)c1
InChI InChI=1S/C25H32N6O3/c1-18-13-20(5-8-26-18)30-9-6-25(7-10-30)17-31(12-11-29(25)2)24-27-23(28-34-24)19-14-21(32-3)16-22(15-19)33-4/h5,8,13-16H,6-7,9-12,17H2,1-4H3
Molecular weight 464.25 Da
AlogP 3.2482200000000017
HBond acceptors 9
HBond donors --
Atoms 66

References

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    Cross References

    Vendors

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    Expert Reviews

    by SERP
    (on 4 Nov 2020 )
    Cellular Use Rating
    MRK-740 is a probe that shows good biochemical target-based potency (80 nM), selectivity against other methyltransferases as well as against a customized panel of 108 enzymes and receptors at Eurofins...
    by SERP+
    (on 22 Mar 2023 )
    Cellular Use Rating
    MRK-740 is a highly selective probe without any significant off-targets in vitro or in cells with IC50 = 80 nM of cellular potency. We would recommend repeating the cytotoxicity assay in your relevant...

    Portal Comments

    ...

    (last updated: 7 Nov 2023)

    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