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YCT-529 | YCT-529 : Antagonist of RARA
RATINGS:
Cellular Use: (0 reviews)

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

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Targets Biochemical/Biophysical Potency Cellular Potency
RARA
    • IC50:1.2 nM
    Antagonist
    up to 100 nM

    Selectivity

    In Cell Selectivity Assessment
    Potency Assay Off-Target:
    Selectivity over target family: RARB and RARG have respectively IC50 >430 nM and 370 nM

    Potency
    Cellular
    In Vitro

    RARA

    Mode of Action: Antagonist

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/acs.jmedchem.5c03051

    In Vivo Validations

    Mouse
    Dose: 10 mg/Kg
    Route of delivery: Oral
    Plasma half life:  6.1 h
    Cmax: 907 ng/ml or 2 µM
    Tmax: 0.5 h
    Area Under the Curve:: 7,713 h*ng/mL

    DOI Reference: 10.1038/s43856-025-00752-7

    Chemical Information

    Molecular Formula C29H25NO3
    SMILEs Cc1ccc(C2=CC(C)(C)Oc3ccc(-c4ccc(-c5ccc(C(=O)O)cc5)[nH]4)cc32)cc1
    InChI InChI=1S/C29H25NO3/c1-18-4-6-19(7-5-18)24-17-29(2,3)33-27-15-12-22(16-23(24)27)26-14-13-25(30-26)20-8-10-21(11-9-20)28(31)32/h4-17,30H,1-3H3,(H,31,32)
    Molecular weight 435.18 Da
    AlogP 6.9580200000000065
    HBond acceptors 4
    HBond donors 2
    Atoms 58

    Expert Reviews

    No SERP comments found for YCT-529

    Probe YCT-529 is in the process of SERP review.

    Please continue to check back for new reviews and commentary.