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SK2188 | SK2188 : Degrader (PROTAC) of AURKA
RATINGS:
Cellular Use: (2 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
AURKA
    • DC50:3.9 nM
    • IC50:31.9 nM
    Degrader (PROTAC)
    up to 500 nM

    Selectivity

    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    SK2188 was assessed against a panel of 468 kinases via a discoverX KINOMEscan @ 100 and 1000 nM.
    Selectivity Assessment Description:
    At 1000 nM, besides AURKA (0.3% control), SK2188 only binds 15 other kinases with a value < 35% cont ...
    In Cell Selectivity Assessment
    Potency Assay Off-Target:
    Mass spectrometry-based shotgun proteome profiling was used to assess the degradation in cellular en ...
    Selectivity Assessment Description:
    From a total of 7175 detected proteins, AURKA was the most significantly downregulated at both 100 n ...

    Potency
    Cellular
    In Vitro

    AURKA

    Mode of Action: Degrader (PROTAC)

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1016/j.ejmech.2022.115033

    Negative Control Compounds

    SK3288
    Notes: The inactive degrader analogue SK3288 displayed no degradation and very weak antiproliferative effects.
    SMILES: O=C(NCCOCCOCCOCCNC([C@@]1(CC[C@H](CC1)Oc2c(F)c(Cl)ccc2)Cc3nc(Nc4sccn4)ccc3)=O)COc5c(C(N(C6=O)C7CCC(N(C)C7=O)=O)=O)c6ccc5

    Orthogonal Probes def

    MK-5108

    Chemical Information

    Molecular Formula C45H49ClFN7O11S
    SMILEs O=C(COc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O)NCCOCCOCCOCCNC(=O)[C@]1(Cc2cccc(Nc3nccs3)n2)CC[C@@H](Oc2cccc(Cl)c2F)CC1
    InChI InChI=1S/C45H49ClFN7O11S/c46-31-6-3-8-34(39(31)47)65-29-12-14-45(15-13-29,26-28-4-1-9-35(51-28)52-44-50-18-25-66-44)43(60)49-17-20-62-22-24-63-23-21-61-19-16-48-37(56)27-64-33-7-2-5-30-38(33)42(59)54(41(30)58)32-10-11-36(55)53-40(32)57/h1-9,18,25,29,32H,10-17,19-24,26-27H2,(H,48,56)(H,49,60)(H,50,51,52)(H,53,55,57)/t29-,32?,45-
    Molecular weight 949.29 Da
    AlogP 4.3871000000000056
    HBond acceptors 18
    HBond donors 4
    Atoms 115

    References

    Publications

    Cross References

    canSARChEMBL

    Expert Reviews

    by SERP
    (on 5 Jan 2026 )
    Cellular Use Rating
    This is a high quality AURKA degrader tool compound that compares well to other, orthogonal, AURKA degraders that used alisertib based AURKA ligands.
    by SERP+
    (on 6 Feb 2026 )
    Cellular Use Rating
    This compound is a highly selective AURKA degrader that is a useful probe up to 500 nM. It shows on-target engagement and will be a useful probe when used with its control compounds.
    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