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    GNE-495
    GNE-495

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V4550
    CAS #: 1449277-10-4Purity ≥98%

    Description: GNE-495 is a novel, potent and selective MAP4K4 (mitogen-activated protein kinase kinase kinase kinase 4) inhibitor with an IC50 of 3.7 nM. Diverse biological roles for mitogen-activated protein kinase kinase kinase kinase 4 (MAP4K4) have necessitated the identification of potent inhibitors in order to study its function in various disease contexts. In particular, compounds that can be used to carry out such studies in vivo would be critical for elucidating the potential for therapeutic intervention. A structure-based design effort coupled with property-guided optimization directed at minimizing the ability of the inhibitors to cross into the CNS led to an advanced compound 13 (GNE-495) that showed excellent potency and good PK and was used to demonstrate in vivo efficacy in a retinal angiogenesis model recapitulating effects that were observed in the inducible Map4k4 knockout mice.

    References 2015 Jun 29;6(8):913-8. 


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    GNE-495

    Name: GNE-495
    CAS#: 1449277-10-4
    Chemical Formula: C22H20FN5O2
    Exact Mass: 405.1601
    Molecular Weight: 405.43
    Elemental Analysis: C, 65.18; H, 4.97; F, 4.69; N, 17.27; O, 7.89
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Technical InformationSynonym: GNE-495; GNE 495; GNE495.
    IUPAC/Chemical Name: 8-amino-N-(1-(cyclopropanecarbonyl)azetidin-3-yl)-2-(3-fluorophenyl)-1,7-naphthyridine-5-carboxamide
    InChi Key: FYXCIBJXJYBWPX-UHFFFAOYSA-N
    InChi Code: InChI=1S/C22H20FN5O2/c23-14-3-1-2-13(8-14)18-7-6-16-17(9-25-20(24)19(16)27-18)21(29)26-15-10-28(11-15)22(30)12-4-5-12/h1-3,6-9,12,15H,4-5,10-11H2,(H2,24,25)(H,26,29)
    SMILES Code: O=C(C1=C2C=CC(C3=CC=CC(F)=C3)=NC2=C(N)N=C1)NC4CN(C(C5CC5)=O)C4


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    GNE-495


    (A) Profile of pyridopyrimidine MAP4K4 inhibitor 1; (B) X-ray structure of 1 in MAP4K4 (PDB: 4OBP).  2015 Jun 29;6(8):913-8.

     GNE-495


    X-ray structure of 13 bound to MAP4K4 at 2.89 Å (PDB: 4ZK5).  2015 Jun 29;6(8):913-8.

     GNE-495


    (A) Representative images of Isolectin-B4 (vascular marker) stained flat-mounted retinas at postnatal day 6 (P6) from mice treated with vehicle or 100 mg/kg GNE-495 daily from P1–P5.  2015 Jun 29;6(8):913-8.


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