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SIAIS630121 | SIAIS630121 : Degrader (PROTAC) of NAMPT
RATINGS:
Cellular Use: (1 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
NAMPT
    • DC50:3.9 nM
    • IC50:8.5 and 4.7 nM
    Degrader (PROTAC)
    up to 10 nM

    Selectivity

    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    To assess selectivity of 630121, a mass spectrometry-based quantitative proteomics analysis in the H ...

    Potency
    Cellular
    In Vitro

    NAMPT

    Mode of Action: Degrader (PROTAC)

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1016/j.chembiol.2022.10.007

    In Vivo Validations

    Rat
    Dose: 2 mg/Kg
    Route of delivery: Intravenous
    Area Under the Curve:: 452.49 h × ng/mL

    DOI Reference: 10.1016/j.chembiol.2022.10.007

    Dose: 10 mg/Kg
    Route of delivery: Oral
    Bioavailability: 23.2%

    DOI Reference: 10.1016/j.chembiol.2022.10.007

    Negative Control Compounds

    canSAR7437544
    Notes: SIAIS630121-NC contains methylated CRBN ligand and is unable to degrade NAMPT in cell.

    Chemical Information

    Molecular Formula C49H59N7O5
    SMILEs O=C(/C=C/c1cccnc1)NCCCCC1CCN(C(=O)c2ccc(N3CCN(CCCCCCC#Cc4cccc5c4CN(C4CCC(=O)NC4=O)C5=O)CC3)cc2)CC1
    InChI InChI=1S/C49H59N7O5/c57-45(22-16-38-12-10-26-50-35-38)51-27-7-6-11-37-24-29-55(30-25-37)48(60)40-17-19-41(20-18-40)54-33-31-53(32-34-54)28-8-4-2-1-3-5-13-39-14-9-15-42-43(39)36-56(49(42)61)44-21-23-46(58)52-47(44)59/h9-10,12,14-20,22,26,35,37,44H,1-4,6-8,11,21,23-25,27-34,36H2,(H,51,57)(H,52,58,59)/b22-16+
    Molecular weight 825.46 Da
    AlogP 5.8189000000000055
    HBond acceptors 12
    HBond donors 2
    Atoms 120

    Expert Reviews

    by SERP+
    (on 6 Feb 2026 )
    Cellular Use Rating
    We would recommend 630121 for studies of NAMPT degradation/inhibition. The probe demonstrates degradation of NAMPT with consequent inhibition of NAMPT NAD+ synthase activity. The probe results in cytotoxicity...
    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