Chemical Probes logo
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
Vendors
Download

Probe Summary

More...

Targets Biochemical/Biophysical Potency Cellular Potency
PTPN2
  • IC50:1.8 nM
  • EC50:176 nM
  • IC50:64 nM
PTPN1
  • IC50:2.5 nM
    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 1.2053
    HBond acceptors 7
    HBond donors 3
    Atoms 50

    Vendors

    Note: This is not an exhaustive list and does not indicate endorsement by the Portal.

    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...
    If you would like to explore AI-generated evaluations, you may wish to visit the page for this compound on our collaborator website
    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