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SGC-CAMKK2-1 | SGC-CAMKK2-1 : Inhibitor of CAMKK1, CAMKK2
RATINGS:
Cellular Use: (3 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
CAMKK1
  • Activity:12 Percent of Control
    CAMKK2
    • IC50:30 nM
    • IC50:1603 nM
    Inhibitor
    up to 5 uM

    Selectivity

    In Vitro Selectivity Assessment
    Selectivity Assessment Description:
    SGC-CAMKK2-1 was profiled in the KINOMEscan assay against 403 wild-type kinases at 1 uM. Only two ki ...

    Potency
    Cellular
    In Vitro

    CAMKK1

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.3390/cells12020287

    CAMKK2

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.3390/cells12020287

    Negative Control Compounds

    CANSAR3550556
    Notes: SGC-CAMKK2-1N is a suitable structurally similar negative control. It has an IC50 = 27 µM on purified CAMKK2, and cellular potency > 10,000 µM.

    Orthogonal Probes def

    STO609

    Chemical Information

    Molecular Formula C26H23NO3
    SMILEs Cc1cccc(-c2cnc3occ(-c4ccc(C(=O)O)c(C5CCCC5)c4)c3c2)c1
    InChI InChI=1S/C26H23NO3/c1-16-5-4-8-18(11-16)20-13-23-24(15-30-25(23)27-14-20)19-9-10-21(26(28)29)22(12-19)17-6-2-3-7-17/h4-5,8-15,17H,2-3,6-7H2,1H3,(H,28,29)
    Molecular weight 397.17 Da
    AlogP 0.0
    HBond acceptors 4
    HBond donors 1
    Atoms 53
    PAINS * Yes

    * This is an automated alert only, and may not necessarily indicate an issue with this probe. ( Learn more about PAINS )

    Expert Reviews

    by SERP
    (on 22 Apr 2022 )
    Cellular Use Rating
    This exact compound is not detailed in the reference. The detailed compound is the phenyl ring on the 5-position of the azabenzofuran system. This particular compound has the 3-methylphenyl. More detailed...
    by SERP
    (on 22 Apr 2022 )
    Cellular Use Rating
    The kinome selectivity profile of this probe is exceptional. The inactive analogue is also of high quality and it is well worth using in parallel with the probe to obtain conclusive results. The lipophilic...
    by SERP+
    (on 23 May 2024 )
    Cellular Use Rating
    This is a potent and selective compound for CAMKK2 . However, the cellular potency is slightly above the suggested 1 µM threshold and effect of the compound on cellular viability would have been nice to...
    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