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ABBV-CLS-484 | ABBV-CLS-484 : Competitive, reversible of PTPN2, PTPN1
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
PTPN2
  • IC50:1.8 nM
  • EC50:176 nM
  • IC50:64 nM
PTPN1
  • IC50:2.5 nM
    Competitive, reversible
    up to 1 uM

    Selectivity

    In Vitro Selectivity Assessment
    PTPN9

    Gene ID: P43378

    Organism: Homo sapiens

    Family: protein-tyrosine phosphatase family

    Potency: IC50 - 15 nM

    Potency Assay Off-Target:
    In a biochemical phosphatase screen, AC484 demonstrated high selectivity for PTPN2/N1, with 6–8-fold ...
    In Cell Selectivity Assessment

    Potency
    Cellular
    In Vitro

    PTPN2

    Mode of Action: Competitive, reversible

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1038/s41586-023-06575-7

    PTPN1

    Mode of Action: Competitive, reversible

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1038/s41586-023-06575-7

    In Vivo Validations

    Mouse
    Dose: 1, 10 mg/Kg
    Route of delivery: Intravenous, Oral
    Plasma half life: 2 h PO
    Systemic clearance: 1.7 L/h/Kg
    Fb : 99.14%
    Target engagement assay: Unbound mouse brain/plasma ratio (12h) 0.86

    DOI Reference: 10.1038/s41586-023-06575-7

    Chemical Information

    Molecular Formula C17H24FN3O4S
    SMILEs CC(C)CCN[C@@H]1CCc2cc(O)c(N3CC(=O)NS3(=O)=O)c(F)c2C1
    InChI InChI=1S/C17H24FN3O4S/c1-10(2)5-6-19-12-4-3-11-7-14(22)17(16(18)13(11)8-12)21-9-15(23)20-26(21,24)25/h7,10,12,19,22H,3-6,8-9H2,1-2H3,(H,20,23)/t12-/m1/s1
    Molecular weight 385.15 Da
    AlogP 0.0
    HBond acceptors 7
    HBond donors 3
    Atoms 50

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    Expert Reviews

    by SERP
    (on 3 Jan 2024 )
    Cellular Use Rating
    In Model Organisms
    A concentration of 1 uM seems sufficient to achieve full response in cells using multiple readouts. Of note, no data regarding cellular toxicity at that concentration have been shown. If used in whole...
    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