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    ML167 (CID 44968231)
    ML167 (CID 44968231)

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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 #: V1545
    CAS #: 1285702-20-6Purity ≥98%

    Description: ML167 (also called CID-44968231; NCGC-00188654; ML-167; CID 44968231; NCGC00188654) is a novel, ATP-competitive and highly selective Cdc2-like kinase 4 (Clk4) inhibitor with potential anticancer activity. It inhibits Clk4 with an IC50 of 136 nM, and shows >10-fold selectivity for closely related kinases such as Clk1-3 and Dyrk1A/1B.  

    References: Rosenthal A S, Tanega C, Shen M, et al. An inhibitor of the Cdc2-like kinase 4 (Clk4). 2011.

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    Molecular Weight (MW)335.36 
    FormulaC19H17N3O3 
    CAS No.1285702-20-6
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 67 mg/mL (199.8 mM) 
    Water: <1 mg/mL
    Ethanol: 13 mg/mL (38.8 mM) 
    SMILESOCC1=CC=C(C2=CC3=C(NCC4=CC=C(C)O4)N=CN=C3C=C2)O1
    SynonymsCID 44968231; NCGC00188654; ML167; CID44968231; NCGC 00188654; ML-167; CID-44968231; NCGC-00188654; ML 167


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    In Vitro

    In vitro activity: ML167 (also known as CID 44968231) is a highly selective Cdc2-like kinase 4 (Clk4) inhibitor with IC50 of 136 nM, >10-fold selectivity for closely related kinases Clk1-3 and Dyrk1A/1B. ML167 is found as the first fully selective inhibitor of Clk4 but not other related kinases including Clk1, Clk2 and Clk3 and Dyrk1A/1B. It is 10-fold more potent against Clk4 over other kinases. The treatment of ML167 on Caco-2 cells proves that ML167 is highly cell-permeable. Besides that, ML167 is also found to be an ATP-competitive inhibitor.  


    Kinase Assay: All compounds were screened using a qHTS approach, where compounds are assayed using at least seven concentrations to generate concentration-response curves for every compounds. The methodology for creating a concentration-titration series between successive copies of library plates for the purpose of large-scale titration-based screening has been described. Briefly, qHTS uses an inter-plate dilution method where the first plate contains the highest concentration of a set of compounds in DMSO, while subsequent plates contain the same compounds in the same well locations, but at successive lower concentrations. Using the protocol outlined above, we calculated a plate throughput of 18 plates/hr, or approximately 7 samples/sec, on the Kalypsys robotic system, which means that a 7 point CRC was obtained every second on the robotic system.


    Cell Assay: ML167, as a probe of Clk4, shows high cell permeability in a Caco-2 assay.

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    ReferencesRosenthal A S, Tanega C, Shen M, et al. An inhibitor of the Cdc2-like kinase 4 (Clk4). 2011. 


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

    ML167

    LCMS traces of NCGC00188654/CID 44968231/ML167 in PBS buffer, pH 7.4 at 23°C at 0 hours and 48 hours. 

     

    ML167

    Structure of NCGC00188654/CID 44968231/ML167 and dose response curve for in-house Clk4 assay.  An inhibitor of the Cdc2-like kinase 4 (Clk4).

     

    ML167

    A. Inhibitory dose response of 2 in the presence of three different ATP concentrations [1μM (filled circles), 50μM (empty circles), 100μM (empty squares)]. B. Inhibitory dose response of 2 in the presence of three different peptide. An inhibitor of the Cdc2-like kinase 4 (Clk4).


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