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    LDC4297
    LDC4297

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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 #: V2731
    CAS #: 1453834-21-3Purity ≥98%

    Description: LDC4297 is a novel and potent CDK7 (Cyclin-dependent protein kinase 7) inhibitor with IC50 of 0.13±0.06 nM for CDK7 and IC50s between 10 nM and 10,000 nM for all other analyzed CDKs. Cyclin-dependent protein kinase 7 (CDK7) plays crucial regulatory roles in cell cycle and transcription, both connected with the replication of many viruses. The affinity of LDC4297 for CDK7 proves to be extremely high. The replication of HCMV in cultured primary human fibroblasts (HFFs) is inhibited by LDC4297 in a concentration-dependent manner with a 50% effective concentration (EC50) value of 24.5 ± 1.3 nM. Notably, CDK7 inhibition by LDC4297 is not associated with general cytotoxicity at submicromolar concentrations. Summarized, the CDK7 inhibitor LDC4297 is a promising candidate for further antiviral drug development, possibly offering new options for a comprehensive approach to antiviral therapy.

    References: Antimicrob Agents Chemother. 2015 Apr;59(4):2062-71.


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    Molecular Weight (MW)432.52
    FormulaC23H28N8O
    CAS No.1453834-21-3
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 86 mg/mL (198.8 mM)
    Water: <1 mg/mL 
    Ethanol: 86 mg/mL (198.8 mM)
    SMILESCC(C)C(C=NN12)=C1N=C(OC3CNCCC3)N=C2NCC4=CC=CC=C4N5N=CC=C5
    SynonymsLDC044297; LCD-044297; LCD 044297; LDC4297; LDC-4297; LDC 4297 


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    In Vitro

    In vitro activity: LDC4297 inhibits CDK7 in vitro in the nano-picomolar range. The affinity of LDC4297 for CDK7 proves to be extremely high. The replication of HCMV in cultured primary human fibroblasts (HFFs) is inhibited by LDC4297 in a concentration-dependent manner with a 50% effective concentration (EC50) value of 24.5 ± 1.3 nM. Notably, CDK7 inhibition by LDC4297 is not associated with general cytotoxicity at submicromolar concentrations. In contrast, LDC4297 induces cytotoxicity in a set of tumor cell lines, i.e., already at extremely low, nanomolar concentrations in specific cases. Anti-HCMV activity of LDC4297 is exerted through a multifaceted mode of action that involves an interference with virus-induced Rb phosphorylation.


    Kinase Assay: LDC4297 is a novel and potent CDK7 (Cyclin-dependent protein kinase 7) inhibitor with IC50 of 0.13±0.06 nM for CDK7 and IC50s between 10 nM and 10,000 nM for all other analyzed CDKs. Cyclin-dependent protein kinase 7 (CDK7) plays crucial regulatory roles in cell cycle and transcription, both connected with the replication of many viruses. The affinity of LDC4297 for CDK7 proves to be extremely high. The replication of HCMV in cultured primary human fibroblasts (HFFs) is inhibited by LDC4297 in a concentration-dependent manner with a 50% effective concentration (EC50) value of 24.5 ± 1.3 nM. Notably, CDK7 inhibition by LDC4297 is not associated with general cytotoxicity at submicromolar concentrations. Summarized, the CDK7 inhibitor LDC4297 is a promising candidate for further antiviral drug development, possibly offering new options for a comprehensive approach to antiviral therapy.


    Cell Assay: A trypan blue exclusion assay is performed with cultured cells seeded in 24-well plates and incubated with increasing concentrations of antiviral compounds (range, 0.1 to 50 μM) for the durations indicated. Cell staining is achieved with 0.1% trypan blue for 10 min at room temperature before the percentage of viable cells is determined by microscopic counting.

    In VivoThe PK analyses of LDC4297 performed thus far have also been highly promising. An analysis of the PK parameters in CD1 mice reveals positive characteristics after oral administration, as demonstrated for a single-dose treatment (100 mg/kg of LDC4297. The half-life (t1/2z) is determined to be 1.6 h, and a time (Tmax) to a mean peak plasma concentration of 1,297.6 ng/ml is reached 0.5 h after administration, with a continued presence of LDC4297 plasma levels for at least 8 h and a bioavailability of 97.7%.
    Animal modelCD-1 mice
    Formulation & Dosage100 mg/kg; p.o.
    ReferencesAntimicrob Agents Chemother. 2015 Apr;59(4):2062-71.


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

    LDC4297

    Chemical structure and selectivity profile of LDC4297.



    LDC4297

    Inhibitory effect of LDC4297 on individual stages of viral gene expression. Antimicrob Agents Chemother. 2015 Apr;59(4):2062-71. 
     

    LDC4297

    Inhibitory activity of LDC4297 regarding HCMV replication and cell proliferation. Antimicrob Agents Chemother. 2015 Apr;59(4):2062-71. 
     

    LDC4297

    LDC4297 exerts differential impact on the expression levels of several cellular and viral proteins.



    LDC4297

    In vitro kinase activity of pUL97 is not inhibited by LDC4297. Antimicrob Agents Chemother. 2015 Apr;59(4):2062-71. 


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