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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 (PS1145) is a novel, potent and specific IKK (IκB kinase) inhibitor with anticancer activity. It inhibits IKK with an IC50 of 88 NM. PS 1145 exhibits excellent in vivo antitumor efficacy in rats bearing DMBA-induced skin tumors.

    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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