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R1-ICR-5 | R1-ICR-5 : Degrader (PROTAC) of RIPK1
RATINGS:
Cellular Use: (1 reviews)

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

Targets Biochemical/Biophysical Potency Cellular Potency
RIPK1
    • Dmax:~100%
    • DC50: about 50 nM
    • DC50:50 nM
    • Dmax:101
    Degrader (PROTAC)
    Effective in most cells at 100nM.
    up to 1 µM

    Selectivity

    In Cell Selectivity Assessment
    Potency Assay Off-Target:
    In cell selectivity was confirmed via Western Blot: R1-ICR-5 was unable to depleape RIPK2, RIPK3, BR ...

    Potency
    Cellular
    In Vitro

    RIPK1

    Mode of Action: Degrader (PROTAC)

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1016/j.immuni.2024.04.025

    Negative Control Compounds

    canSAR7437536
    Notes: R1-ICR-5S does not bind VHL and fail to deplete RIPK1.

    Chemical Information

    Molecular Formula C54H70N8O7S2
    SMILEs Cc1ncc(-c2ccc3nc(NC(=O)CCCCCCCCCCC(=O)N[C@H](C(=O)N4C[C@H](O)C[C@H]4C(=O)NCc4ccc(-c5scnc5C)cc4)C(C)(C)C)sc3c2)cc1NC(=O)OC1CCCCC1
    InChI InChI=1S/C54H70N8O7S2/c1-34-43(59-53(68)69-41-17-13-12-14-18-41)27-39(31-55-34)38-25-26-42-45(28-38)71-52(58-42)61-47(65)20-16-11-9-7-6-8-10-15-19-46(64)60-49(54(3,4)5)51(67)62-32-40(63)29-44(62)50(66)56-30-36-21-23-37(24-22-36)48-35(2)57-33-70-48/h21-28,31,33,40-41,44,49,63H,6-20,29-30,32H2,1-5H3,(H,56,66)(H,59,68)(H,60,64)(H,58,61,65)/t40-,44+,49-/m1/s1
    Molecular weight 1006.48 Da
    AlogP 10.628439999999996
    HBond acceptors 15
    HBond donors 5
    Atoms 141

    References

    Publications

    Cross References

    Expert Reviews

    by SERP+
    (on 31 Oct 2024 )
    Cellular Use Rating
    ( The reviewer did not leave any comments )
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