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TMX-2172 | TMX-2172 : Degrader (PROTAC) of CDK2, CDK5
RATINGS:
Cellular Use: (3 reviews)

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

Targets Biochemical/Biophysical Potency Cellular Potency
CDK2
  • IC50:6.5 nM
  • Dmax:~80%
CDK5
  • IC50:6.8 nM
    Degrader (PROTAC)
    250 nM

    Selectivity

    In Vitro Selectivity Assessment
    AURKA

    Gene ID: O14965

    Organism: Homo sapiens

    Family: Ser/Thr protein kinase family

    Potency: IC50 - 205 nM

    Potency Assay Off-Target:
    TMX-2172 was screened in KINOMEscan, which profiles more than 400 kinases.14 kinases exhibited >99 % ...

    Potency
    Cellular
    In Vitro

    CDK2

    Mode of Action: Degrader (PROTAC)

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1002/anie.202004087

    CDK5

    Mode of Action: Degrader (PROTAC)

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1002/anie.202004087

    Negative Control Compounds

    ZXH-7035
    Notes: ZXH-7035 was able to bind CDK2/5 with same affinity as TMX-2172 but it was not able to degrade the targets.

    Chemical Information

    Molecular Formula C41H45BrFN9O11S
    SMILEs Cc1cc(S(=O)(=O)NCCOCCOCCOCCOCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)ccc1Nc1ncc(Br)c(Nc2cccc(F)c2C(N)=O)n1
    InChI InChI=1S/C41H45BrFN9O11S/c1-24-22-25(8-9-29(24)49-41-46-23-27(42)37(51-41)48-31-7-3-5-28(43)35(31)36(44)54)64(58,59)47-13-15-61-17-19-63-21-20-62-18-16-60-14-12-45-30-6-2-4-26-34(30)40(57)52(39(26)56)32-10-11-33(53)50-38(32)55/h2-9,22-23,32,45,47H,10-21H2,1H3,(H2,44,54)(H,50,53,55)(H2,46,48,49,51)
    Molecular weight 969.21 Da
    AlogP 0.0
    HBond acceptors 20
    HBond donors 7
    Atoms 109

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    Expert Reviews

    by SERP
    (on 15 Jun 2024 )
    Cellular Use Rating
    TMX-2172 demonstrated potent degradation activity for CDK2 in some cell lines, but it also induced degradation of other proteins, such as CDK5 and AURKA. Additionally, the authors did not mention whether...
    by SERP
    (on 28 Aug 2024 )
    Cellular Use Rating
    While selectivity was shown for this probe in OVCAR8 cells (5 µM for 6 h) as well as Jurkat cells (10 µM for 6 h), more extensive cell profiling, including lines and time points, could have been performed...
    by SERP+
    (on 31 Oct 2024 )
    Cellular Use Rating
    Including additional time points after treatment would be beneficial.
    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