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(R)-SKBG-1 | (R)-SKBG-1 : Covalent Inhibitor of NONO
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
NONO
    • IC50:3100 nM
    • IC50:5500 nM
    • EC50:630 nM
    • Activity:20 µM
    up to 20 uM

    Selectivity

    In Cell Selectivity Assessment
    Potency Assay Off-Target:
    Identification of the protein target(s) of the active compound by chemical proteomics. 22Rv1 cells w ...

    Potency
    Cellular
    In Vitro

    NONO

    Mode of Action: Covalent Inhibitor

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1038/s41589-023-01270-0

    Negative Control Compounds

    (S)-SKBG-1N
    PubChem ID: https://pubchem.ncbi.nlm.nih.gov/compound/166637068

    Chemical Information

    Molecular Formula C22H26ClN3O6S
    SMILEs COc1ccc(CNC(=O)[C@H]2CN(C(=O)CCl)CCN2S(=O)(=O)c2ccc(OC)cc2)cc1
    InChI InChI=1S/C22H26ClN3O6S/c1-31-17-5-3-16(4-6-17)14-24-22(28)20-15-25(21(27)13-23)11-12-26(20)33(29,30)19-9-7-18(32-2)8-10-19/h3-10,20H,11-15H2,1-2H3,(H,24,28)/t20-/m1/s1
    Molecular weight 495.12 Da
    AlogP 1.4605
    HBond acceptors 9
    HBond donors 1
    Atoms 59

    Vendors

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    Expert Reviews

    by SERP
    (on 31 Jul 2023)
    Cellular Use Rating
    (R)-SKBG-1 fails to meet criteria (doi.org/10.1021/acs.jmedchem.3c00550) for covalent probes regarding potency (> 1 µM), negative control compound (activity difference between (R)-SKBG-1 and (S)-SKBG-1N...
    by SERP
    (on 9 Aug 2023)
    Cellular Use Rating
    This probe is a recently-developed covalent modulator of NONO function. Chemoproteomics studies demonstrate that the probe shows high selectivity across the proteome, and use of the NONO C145S resistance...
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