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dCDK9-202 | dCDK9-202 : Degrader (PROTAC) of CDK9
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
CDK9
    • DC50:3.5 ± 0.7 nM
    • IC50:8.5 ± 0.2 nM
    Degrader (PROTAC)
    10 nM, up to 25 nM

    Selectivity

    In Cell Selectivity Assessment
    Potency Assay Off-Target:
    dCDK9-202 was evaluated for its target selectivity in the TC-71 cell line. Among CDKs, compound dCDK ...
    In Cell Selectivity Assessment
    Potency Assay Off-Target:
    dCDK9-202 was highly potent and effective in the inhibition of multiple cancer cell lines and achiev ...

    Potency
    Cellular
    In Vitro

    CDK9

    Mode of Action: Degrader (PROTAC)

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/acs.jmedchem.5c01111

    In Vivo Validations

    Mouse
    Dose: 2 mg/Kg
    Route of delivery: Intravenous
    Plasma half life: 0.3 h
    Systemic clearance: 312 mL/min/Kg
    Cmax: 280 ng/mL
    Area Under the Curve:: 116 h*ng/mL
    Volume of Distribution at Steady-State: 7.1 L/Kg

    DOI Reference: 10.1021/acs.jmedchem.5c01111

    Negative Control Compounds

    dCDK9-202Me
    Notes: dCDK9-202Me was not able to degrade CDK9 with a Dmax of only 5% and IC50 >1000 nM in cell growth inhibition assay

    Chemical Information

    Molecular Formula C40H49N7O7S2
    SMILEs CC(C)(C)c1cnc(CSc2cnc(NC(=O)C3CCN(C(=O)CCCCCCCN4Cc5cc6c(cc5C4)C(=O)N(C4CCC(=O)NC4=O)C6=O)CC3)s2)o1
    InChI InChI=1S/C40H49N7O7S2/c1-40(2,3)30-19-41-32(54-30)23-55-34-20-42-39(56-34)44-35(50)24-12-15-46(16-13-24)33(49)9-7-5-4-6-8-14-45-21-25-17-27-28(18-26(25)22-45)38(53)47(37(27)52)29-10-11-31(48)43-36(29)51/h17-20,24,29H,4-16,21-23H2,1-3H3,(H,42,44,50)(H,43,48,51)
    Molecular weight 803.31 Da
    AlogP 5.655600000000006
    HBond acceptors 14
    HBond donors 2
    Atoms 105

    References

    Publications

    Cross References

    Expert Reviews

    by SERP
    (on 25 Nov 2025)
    Cellular Use Rating
    In Model Organisms
    dCDK9-202 is a potent CDK9 degrader, CRBN and proteasome dependent. In comparison with the earlier degrader THAL-SNS-032 (based on the same inhibitor), the authors report improved cellular potency and...
    by SERP
    (on 27 Nov 2025)
    Cellular Use Rating
    In Model Organisms
    (The reviewer did not leave any public comments)
    by SERP
    (on 6 Feb 2026)
    Cellular Use Rating
    In Model Organisms
    This is a potent and selective CDK9 degrader and currently the best probe available. Data suggests that there is selectivity to CDK9 over other CDKs, but a full proteomics assessment is not provided....
    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