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    LDC000067 (LDC067)
    LDC000067 (LDC067)

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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 #: V1544
    CAS #: 1073485-20-7Purity ≥98%

    Description: LDC000067 (also called LDC-000067; LDC-067) is a novel, potent, highly selective and ATP-competitive inhibitor of cyclin-dependent kinase (CDK9) with potential antineoplastic activity. It inhibits CDK9 with an IC50 of 44 nM. CDK9 is an important and excellent therapeutic target for anticancer drugs but currently available inhibitors show low specificity and/or narrow therapeutic windows. LDC000067 exhibited selectivity for CDK9 over other CDKs in the range of 55-fold (vs. CDK2) to over 230-fold (vs. CDK6 and CDK7). LDC067 also inhibited transcription in a dose-dependent and ATP-competitive manner. In whole cells, LDC000067 induced the tumor suppressor protein p53 activation and apoptosis. LDC000067 also selectively reduced short-lived mRNAs, including those that encode regulators of apoptosis and proliferation such as MYC and MCL1.

    References: Br J Pharmacol. 2014 Jan;171(1):55-68

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    Molecular Weight (MW)370.43 
    FormulaC18H18N4O3S 
    CAS No.1073485-20-7 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 74 mg/mL (199.8 mM) 
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    SMILESCN1N=CC(C2=NN3C(C=C2)=NN=C3SC4=CC=C5N=CC=CC5=C4)=C1
    SynonymsLDC067; LDC000067; LDC-000067; LDC-067; LDC 067; LDC 000067


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    In Vitro

    In vitro activity: LDC000067 reduces Ser2-P, induces p53 activation and leads to apoptosis in mESCs. In addition, LDC067 also dose-dependently inhibits P-TEFb-dependent de novo RNA synthesis of cellular genes.


    Kinase Assay: Kinase inhibition by LDC000067 was measured in a radio metric assay, which directly measured kinase catalytic activity towards a specific substrate. Briefly, 10 μM LDC000067 or DMSO as solvent control, were added to base reaction buffer (10 mM MgCl2, 1 mM EDTA, 20 mM HEPES pH 7.5, 2 mM DTT, 0.02 mg·mL-1 BSA, 0.1 mM Na3VO4, 0.02% Brij35, 1% DMSO), containing cofactors and substrates, which were required by the individual kinase. 10 μCi of [γ-33P]-APP (10mCi·mL-1, 3000Ci·mmol-1, Perkin Elmer) was added to the reaction mixture. And such kinase reaction incubated for 120min at room temperature. Reactions were found on P81 ion exchange paper, and filters generally washed in 0.75% phosphoric acid before radiometric quantification. Each protein kinase was measured in duplicate, and its catalytic activity expressed as residual kinase activity, which shows the percentage of average substrate phophorylation in contrast with the solvent control reaction.


    Cell Assay: LDC000067 inhibits CDK9 with an IC50 value of 44(10 nM, and its selectivity for CDK9 over other CDKs is in the range of 55-fold to over 230-fold, especially higher selectivity in an ATP-competitive kinase binding assay. Besides, effects of LDC000067 in whole cells contain induction of the tumour suppressor protein p53 and apoptosis. Moreover, gene expression profiling of cells treated with LDC000067 demonstrate selective reduction of short-lived mRNAs, which encode regulators of proliferation and apoptosis, such as MCL1 and MYC.

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    References Br J Pharmacol. 2014 Jan;171(1):55-68. 


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

    LDC000067

    Inhibition of in vitro transcription by LDC067.  2014 Jan;171(1):55-68.

     

    LDC000067

    Microarray analysis of THP1 cells treated with LDC067.  2014 Jan;171(1):55-68.

     

    LDC000067

    Increase of RNAPII pausing at MYC in the presence of LDC067.


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