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    PS-1145
    PS-1145

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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 #: V0753
    CAS #: 431898-65-6Purity ≥98%

    Description: PS-1145 is a novel, potent and specific IKK (IκB kinase) inhibitor with IC50 of 88 NM and with anticancer activity. 

    References: J Biol Chem. 2002 May 10;277(19):16639-47.

    Related CAS: 1049743-58-9 (HCl)   431898-65-6 (free base) 

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    Molecular Weight (MW)322.75
    FormulaC17H11ClN4O
    CAS No.431898-65-6  (free base); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 64 mg/mL (198.3 mM)
    Water: <1 mg/mL
    Ethanol: 2 mg/mL warmed (6.2 mM)
    Other infoChemical Name: N-(6-chloro-9H-pyrido[3,4-b]indol-8-yl)nicotinamide
    InChi Key: JZRMBDHPALEPDM-UHFFFAOYSA-N
    InChi Code: InChI=1S/C17H11ClN4O/c18-11-6-13-12-3-5-20-9-15(12)21-16(13)14(7-11)22-17(23)10-2-1-4-19-8-10/h1-9,21H,(H,22,23)
    SMILES Code: O=C(C1=CC=CN=C1)NC2=CC(Cl)=CC3=C2NC4=C3C=CN=C4
    SynonymsPS 1145; PS1145; PS-1145; 


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    In Vitro

    In vitro activity: PS-1145 blocks TNFalpha-induced NF-kappaB activation through inhibition of IkappaBalpha phosphorylation, and blocks the protective effect of IL-6 against Dex-induced apotosis. PS-1145 also inhibits paracrine MM cell growth and IL-6 secretion in BMSCs triggered by MM cell adherence. In human primary CD4(+) T cells, PS-1145 abrogates cell proliferation and impairs the activation of NF-κB and AP-1 transcription factors by engagement of CD3 and CD28 coreceptor


    Kinase Assay: PS-1145 are dissolved in DMSO and stored at −20 °C until use. Ki value of PS-1145 against the IKK complex is determined by measuring Km , ATP against varying fixed concentration of the inhibitor. Briefly, partially purified IKK complex obtained from unstimulated HeLa S3 cells are pre-activated using the catalytic domain of MEKK1 expressed in sf9. Kinase activity is assessed using a biotinylated IκBα peptide (250 μM, RHDSGLDSMKD,Km ,peptide = 30 μM,K m , ATP = 10 μM) and phospho-[Ser32]-phosphoantibodies in an ELISA format with appropriate standard curve for quantification. For PS-1145 Ki measurement, the activated IKK complex is first preincubated in varying fixed concentration of the inhibitor (0.1–1 μM) at 25 °C for 1 h. Then apparentK m measurement for MgATP is performed at each discrete inhibitor concentration. 


    Cell Assay: The inhibitory effect of PS-1145 on MM growth is assessed by measuring MTT dye absorbance of the cells. Cells (MM.1S, U266, and RPMI8226 cell lines) from 48-h cultures are pulsed with 10 μL of 5 mg/ml MTT to each well for the last 4 h of 48-h cultures, followed by 100 μl of isopropanol containing 0.04N HCl. Absorbance is measured at 570 nm using a spectrophotometer.

    In VivoIn male Wistar rats with DMBA-induced skin tumor, PS-1145 (50 mg/kg, i.v.) enhances tumor cell apoptosis by up-regulating p53, activating caspases and down regulating NF-κB and VEGF factor, and thus induces the tumor progression.
    Animal modelMale Wistar rats with DMBA-induced skin tumor
    Formulation & DosageDissolved in 0.4 mg/mL in DMSO and diluted with 0.9% NaCl; 50 mg/kg; i.v. injection
    References

    J Biol Chem. 2002 May 10;277(19):16639-47; J Immunol. 2012 Mar 15;188(6):2545-55; Cell Biol Int. 2015 Nov;39(11):1317-28. 


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

     

    PS-1145

    PS-1145 blocks phosphorylation and degradation of IκBα triggered by TNFα. J Biol Chem. 2002 May 10;277(19):16639-47.
     

    PS-1145

    Effect of PS-1145 on DNA synthesis, cell cycle profile, and signaling cascades triggered by IL-6. J Biol Chem. 2002 May 10;277(19):16639-47.
     

    PS-1145

    Dex up-regulates IκBα protein and enhances the inhibitory effect of PS-1145 on NF-κB activation. J Biol Chem. 2002 May 10;277(19):16639-47.
     

    PS-1145

    PS-1145 inhibits growth and blocks the protective effect of IL-6 against Dex - and IMiD3-induced growth inhibition. J Biol Chem. 2002 May 10;277(19):16639-47.
     

    PS-1145

    PS-1145 inhibits TNFα-induced ICAM-1 expression and triggers TNFα-induced apoptosis in MM cells. J Biol Chem. 2002 May 10;277(19):16639-47.
     

    PS-1145

    PS-1145 inhibits paracrine MM cell growth and IL-6 secretion in BMSCs triggered by MM cell adherence. J Biol Chem. 2002 May 10;277(19):16639-47.


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