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    HTH-01-015
    HTH-01-015

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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 #: V0250
    CAS #: 1613724-42-7Purity ≥98%

    Description: HTH-01-015 is a novel, potent and selective inhibitor of NUAK1( (NUAK family SnF1-like kinase-1) which can serve as useful chemical probes to delineate the biological roles of the NUAK kinases. It inhibits NUAK1 with an IC50 of ~100 nM, and exhibits >100-fold higher selectivity for NUAK1 over NUAK2 (IC50 of >10 μM). The NUAK1 and NUAK2 are members of the AMPK (AMP-activated protein kinase) family of protein kinases that are activated by the LKB1 (liver kinase B1) tumour suppressor kinase. 

    References: Biochem J. 2014 Jan 1;457(1):215-25; Biochem J. 2014 Jul 15;461(2):233-45.

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    Molecular Weight (MW)

    468.55

    Formula

    C26H28N8O

    CAS No.

    1613724-42-7

    Storage

    -20℃ for 3 years in powder form

    -80℃ for 2 years in solvent

    Solubility (In vitro)

    DMSO: 58 mg/mL (123.8 mM)

    Water: <1 mg/mL

    Ethanol: 30 mg/mL (64.0 mM)

    SMILES Code

     CC1=C(N(C)C(C2=CC(C=CC=C3)=C3C=C2N4C)=O)C4=NC(NC5=CN(N=C5)C6CCNCC6)=N1

    Synonyms

     HTH-01015; HTH01015; HTH 01015; HTH-01-015; HTH01-015; HTH 01-015


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    In Vitro

    In vitro activity: In HEK-293 cells express NUAK1 as well as NUAK2, HTH-01-015 suppresses NUAK1-mediated MYPT1 phosphorylation. HTH-01-015 suppresses cell migration In NUAK1+/+ MEFs, and inhibit U2OS cell invasion. Moreover, HTH-01-015 inhibits cell proliferation in both cell lines. HTH-01-015 inhibitors markedly restricted cells from entering into mitosis in U2OS cells.

     

    Kinase Assay: In vitro activities of purified GST–NUAK1 and GST–NUAK1[A195T] are measured using Cerenkov counting of incorporation of radioactive 32P from [γ-32P]ATP into Sakamototide substrate peptide. Reactions are carried out in a 50 μL reaction volume for 30 min at 30°C and reactions are terminated by spotting 40 μL of the reaction mix on to P81 paper and immediately immersing in 50 mM orthophosphoric acid. Samples are washed three times in 50 mM orthophosphoric acid followed by a single acetone rinse and air drying. The kinase-mediated incorporation of [γ-32P]ATP into Sakamototide is quantified by Cerenkov counting. One unit of activity is defined as that which catalyses the incorporation of 1 nmol of [32P]phosphate into the substrate over 1 h.

     

    Cell Assay: Cell proliferation assays are carried out colorimetrically in 96-well plates using the CellTiter 96® AQueous Non-Radioactive Cell Proliferation Assay kit following the manufacturer's protocol. Initially, 2000 cells per well are seeded for U2OS cells and 3000 cells per well are seeded for MEFs. The proliferation assays are carried out over 5 days in the presence or absence of 10 μM HTH-01-015.

    In Vivo

    Short-term treatment of normal Sprague Dawley rats with A-769662 decreases liver malonyl CoA levels and the respiratory exchange ratio, VCO2/VO2, indicating an increased rate of whole-body fatty acid oxidation. Treatment of ob/ob mice with 30 mg/kg b.i.d. A-769662 decreases hepatic expression of PEPCK, G6Pase, and FAS, lowers plasma glucose by 40%, reduced body weight gain and significantly decreases both plasma and liver triglyceride levels.

    Animal model

    NA

    Formulation & Dosage

    NA

    References

    Biochem J. 2014 Jan 1;457(1):215-25; Biochem J. 2014 Jul 15;461(2):233-45.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    HTH-01-015

    HTH-01-015, a specific NUAK1 inhibitor.  2014 Jan 1;457(1):215-25.

    HTH-01-015

    HTH-01-015 and WZ4003 inhibit MYPT1 Ser445  phosphorylation in vivo.  2014 Jan 1;457(1):215-25. 

    HTH-01-015

    NUAK1 inhibition suppresses cell migration.  2014 Jan 1;457(1):215-25.

    HTH-01-015

    NUAK1 inhibition suppresses cell proliferation.  2014 Jan 1;457(1):215-25.

    HTH-01-015

    NUAK1 inhibition suppresses invasion potential.  2014 Jan 1;457(1):215-25.

    HTH-01-015

    NUAK1 degradation is required for controlled mitotic progression.  2014 Jul 15;461(2):233-45. 


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