Chemical Probes logo
TACH101 | TACH101 : Inhibitor of KDM4 family members KDM4A, KDM4B, KDM4C, KDM4D
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
Download

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
KDM4A
  • IC50:80 nM
    KDM4B
    • IC50:58 nM
      KDM4C
      • Ki:38 nM
      • IC50:41 nM
      • IC50:0.4 nM
      • IC50:85 nM
      • IC50:10 - 370 nM
      KDM4D
      • IC50:50 nM
        Inhibitor
        up to 1 uM

        Selectivity

        In Vitro Selectivity Assessment
        Potency Assay Off-Target:
        The selectivity of TACH101 was assessed against KDM family members 2–7. TACH101 was observed to exhi ...
        Selectivity Assessment Description:
        Without preincubation, TACH101 inhibited KDM5 family members at potencies ranging from 0.14 to 0.40 ...
        In Cell Selectivity Assessment
        Potency Assay Off-Target:
        TACH101 antiproliferative activity was determined across a broad cancer cell line panel composed of ...
        In Cell Selectivity Assessment
        Potency Assay Off-Target:
        The antiproliferative activity of TACH101 was also tested in patient-derived cancer organoid models. ...

        Potency
        Cellular
        In Vitro

        KDM4A

        Mode of Action: Inhibitor

        Structure-Activity-Relationship data available? No

        DOI Reference: 10.1097/CAD.0000000000001514

        KDM4B

        Mode of Action: Inhibitor

        Structure-Activity-Relationship data available? Yes

        DOI Reference: 10.1097/CAD.0000000000001514

        KDM4C

        Mode of Action: Inhibitor

        Structure-Activity-Relationship data available? Yes

        DOI Reference: 10.1097/CAD.0000000000001514

        KDM4D

        Mode of Action: Inhibitor

        Structure-Activity-Relationship data available? No

        DOI Reference: 10.1097/CAD.0000000000001514

        Orthogonal Probes def

        QC6352

        Chemical Information

        Molecular Formula C26H29N3O3
        SMILEs CC(C)c1ccc(N(C)c2ccc3c(c2)OCC[C@H]3CNc2cnccc2C(=O)O)cc1
        InChI InChI=1S/C26H29N3O3/c1-17(2)18-4-6-20(7-5-18)29(3)21-8-9-22-19(11-13-32-25(22)14-21)15-28-24-16-27-12-10-23(24)26(30)31/h4-10,12,14,16-17,19,28H,11,13,15H2,1-3H3,(H,30,31)/t19-/m0/s1
        Molecular weight 431.22 Da
        AlogP 5.649300000000005
        HBond acceptors 6
        HBond donors 2
        Atoms 61

        References

        Publications

        Cross References

        Expert Reviews

        by SERP
        (on 7 May 2025 )
        Cellular Use Rating
        TACH101 is high-quality probe with selectivity for the KDM4 family of Jumonji (JMJ) demethylases. Both in vitro and cellular on-target effects are observed in the low nanomolar range. Cancer cell line...
        by SERP
        (on 13 May 2025 )
        Cellular Use Rating
        This is a pan-KDM4 inhibitor currently tested in clinical trials. In vitro, there seems only a small selectivity window to KDM5 inhibition. No unbiased data on cellular binding specificity e.g. by chemical...
        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