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    PD 151746
    PD 151746

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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 #: V0704
    CAS #: 179461-52-0Purity ≥98%

    Description: PD 151746 (PD-151746) is a novel, potent, selective, and cell-permeable calpain inhibitor with important biological activity. It inhibits calpain with a Ki of 0.26 μM for μ-Calpain, and has about 20-fold higher selectivity for u-calpain (Ki = 0.26 ± 0.03 μM) over m-calpain (Ki = 5.33 ± 0.77 μM). PD151746 significantly inhibited NMDA-induced α-spectrin breakdown product (SBDP) of 145 kDa and completely inhibited the fragmentation of calmodulin-dependent protein kinase II-α (CaMPK-IIα) and nitric oxide synthase (nNOS), which were cleaved by calpain. The μ-calpain inhibitor PD 151746 decreases oxLDL-induced cytotoxicity.

    References: Proc Natl Acad Sci U S A. 1996 Jun 25;93(13):6687-92; Biochem J. 2003 Sep 1;374(Pt 2):403-11.


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    Molecular Weight (MW)237.25
    FormulaC11H8FNO2S
    CAS No.179461-52-0
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 47 mg/mL (198.1 mM)
    Water: <1 mg/mL
    Ethanol: 47 mg/mL (198.1 mM)
    Other infoChemical Name: 3-(5-Fluoro-3-indolyl)-2-mercapto-2-propenoic Acid
    InChi Key: HWMQHECFXSVZGN-KMKOMSMNSA-N
    InChi Code: InChI=1S/C11H8FNO2S/c12-7-1-2-9-8(4-7)6(5-13-9)3-10(16)11(14)15/h1-5,13,16H,(H,14,15)/b10-3-
    SMILES Code: O=C(O)/C(S)=C/C1=CNC2=C1C=C(F)C=C2 
    SynonymsPD 151746; PD151746; PD-151746; 


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    In Vitro

    In vitro activity: In SY5Y cells, PD151746 effectively attenuates the SLLVY-AMC hydrolysis induced by maitotoxin. In HMEC-1 cells, PD 151746 decreases cytotoxicity induced by oxidized low-density lipoprotein (oxLDL).


    Kinase Assay: PD151746 is a calpain inhibitor, shows a 20-fold selectivity for u-calpain (Ki = 0.26 ± 0.03 μM) over m-calpain (Ki = 5.33 ± 0.77 μM). 


    Cell Assay: In cerebellar granule cells, PD151746 inhibited serum/potassium (S/K) withdrawal induced apoptosis by 29% through inhibition of calpain. Also, PD151746 inhibited the increase of MEF2 phosphorylation and cdk5/p25 formation and inhibited caspase-3 activity. In human hepatoma G2 cells, PD151746 significantly reduced insulin-stimulated glycogen synthesis and increased the amount of protein tyrosine phosphatase-ε (PTPε), which suggested that calpain played an important role in regulation of insulin-stimulated glycogen synthesis. In HEK-293 cells expressing human formyl peptide receptor (hFPR) or hFPR-like 1 (hFPRL1), PD151746 increased cytoplasmic free Ca2+ ([Ca2+]I).

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    ReferencesProc Natl Acad Sci U S A. 1996 Jun 25;93(13):6687-92; Br J Pharmacol. 2005 Aug;145(8):1103-11; Biochem J. 2003 Sep 1;374(Pt 2):403-11.


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

    PD 151746
    Analysis of calpain and caspase-3 activities in 12 h S/K withdrawal in CGNs in the absence or presence of PD150606 (40 μM), PD151746 (40 μM) and z.VAD.fmk (100 μM). Br J Pharmacol. 2005 Aug;145(8):1103-11.
    PD 151746
    Antineurotoxic effect of PD150606, PD151746 and PD145305 on S/K withdrawal in CGNs.  Br J Pharmacol. 2005 Aug;145(8):1103-11.
    PD 151746
    Antiapoptotic effect of PD150606, PD151746 and PD145305 on S/K withdrawal-induced changes in the percentage of cells rated as apoptotic by means of flow cytometric (hypodiploid cells, open bars) or morphological analysis (gray bars). Br J Pharmacol.2005 Aug;145(8):1103-11.


     

    PD 151746
    (a) Western blot analysis of cdk5, p35/p25 and p-MEF2. (b) Immunostaining against cdk5 and MEF2 of CGNs after 12 h S/K withdrawal in the absence or presence of 40 μM PD150606. Br J Pharmacol. 2005 Aug;145(8):1103-11.
    scanned image of page 6690
    Proc Natl Acad Sci U S A. 1996 Jun 25; 93(13): 6687–6692.

     


    scanned image of page 6691
    Proc Natl Acad Sci U S A. 1996 Jun 25; 93(13): 6687–6692.


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