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    CID-2011756
    CID-2011756

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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 #: V0452
    CAS #: 638156-11-3Purity ≥98%

    Description: CID-2011756, discovered from an HTS-high throughput screening campaign, is a cell-permeable, ATP-competitive and specific inhibitor of PKD (protein kinase D) with potential anticancer activity. It inhibits PKD2/3/1 with IC50 values of 0.6, 0.7 and 3.2 μM, respectively. PKD is a novel family of serine/threonine kinases regulated by diacylglycerol, which is involved in multiple cellular processes and various pathological conditions. CID-2011756 inhibits phorbol ester-induced endogenous PKD1 activation in LNCaP prostate cancer cells in a concentration-dependent manner. 

    References:  2011;6(10):e25134

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    Molecular Weight (MW) 396.87 
    Formula C22H21ClN2O3                 
    CAS No. 638156-11-3
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 10 mM 
    Water: <1 mg/mL
    Ethanol: N/A
    SMILES CodeO=C(C1=CC=C(C2=CC=CC(Cl)=C2)O1)NC3=CC=C(CN4CCOCC4)C=C3
    Synonyms

    CID 2011756; CID-2011756; CID2011756.

    Chemical Name: 5-(3-chlorophenyl)-N-(4-(morpholinomethyl)phenyl)furan-2-carboxamide

    InChi Key: XQJWTJLJEYIUDZ-UHFFFAOYSA-N

    InChi Code: InChI=1S/C22H21ClN2O3/c23-18-3-1-2-17(14-18)20-8-9-21(28-20)22(26)24-19-6-4-16(5-7-19)15-25-10-12-27-13-11-25/h1-9,14H,10-13,15H2,(H,24,26)

    SMILES Code: O=C(C1=CC=C(C2=CC=CC(Cl)=C2)O1)NC3=CC=C(CN4CCOCC4)C=C3 


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    In Vitro

    In vitro activity: CID-2011756, discovered from a high throughput screening campaign, is a potent, cell-active, ATP competitive and specific inhibitor of PKD (protein kinase D) with IC50 values of 0.6, 0.7 and 3.2 μM for PKD2, PKD3 and PKD1 respectively. It inhibits phorbol ester-induced endogenous PKD1 activation in LNCaP prostate cancer cells in a concentration-dependent manner. PKD is a novel family of serine/threonine kinases regulated by diacylglycerol, which is involved in multiple cellular processes and various pathological conditions. The limited number of cell-active, selective inhibitors has historically restricted biochemical and pharmacological studies of PKD.


    Kinase Assay: CID 2011756 has pan-PKD inhibitory effects (PKD2 IC50 = 0.6±0.1 uM; PKD3 IC50 = 0.7±0.2 uM) with similar, albeit not identical, potencies which may be expected for an ATP competitive inhibitor. CID 2011756 was the most potent of the inhibitors with a cellular EC50 of 10±0.7 uM (n = 3), an EC50 value comparable to that of our previously described benzoxoloazepinolone.


    Cell Assay:  It inhibits phorbol ester-induced endogenous PKD1 activation in LNCaP prostate cancer cells in a concentration-dependent manner. 

    In Vivo
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    Formulation & Dosage
    References  2011;6(10):e25134.


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

    CID-2011756


    Select, novel PKD1 SMI display inhibition of cellular PKD1 phosphorylation at Ser916.  2011;6(10):e25134.

     CID-2011756


    Docking simulations of select cellular active PKD1 small molecule inhibitors in a conserved PKA catalytic core.  2011;6(10):e25134.

     CID-2011756


    Confirmed novel PKD1 inhibitors display competitive activity with respect to ATP.  2011;6(10):e25134.


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