1. Cell Cycle/DNA Damage
    Epigenetics
  2. PARP

PJ34 hydrochloride 

Cat. No.: HY-13688 Purity: 98.44%
Data Sheet SDS Handling Instructions

PJ34 hydrochloride is a potent specific inhibitor of PARPl/2 with IC50 of 110 nM and 86 nM, respectively.

For research use only. We do not sell to patients.
PJ34 hydrochloride Chemical Structure

PJ34 hydrochloride Chemical Structure

CAS No. : 344458-15-7

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $66 In-stock
10 mg $60 In-stock
50 mg $170 In-stock
100 mg $310 In-stock
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Other Forms of PJ34 hydrochloride:

    PJ34 hydrochloride purchased from MCE. Usage Cited in: Sci Rep. 2017 May 23;7(1):2268.

    The PARP inhibitor PJ34 prevents TCDD toxicities while increasing NAD+ levels. (a,b) Western blots on homogenates of liver and thymus glands from CE treated with TCDD or vehicle with or without PJ34.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    PJ34 hydrochloride is a potent specific inhibitor of PARPl/2 with IC50 of 110 nM and 86 nM, respectively.

    IC50 & Target

    IC50: 110 nM (PARP1), 86 nM (PARP2)[1]

    In Vitro

    PJ34 inhibits the PARP enzyme activity with an IC50 of 110±1.9 nM. To compare the neuroprotective properties of other PARP inhibitors in PC12 cells, PJ34 is evaluated using by LDH assay. PJ34 treatment also significantly and concentration dependently attenuates cell death at a concentration ranging from 10-7 to 10-5 M[1].

    In Vivo

    To compare the potency and efficacy with other PARP inhibitors, PJ34 is evaluated at the doses of 3.2 and 10 mg/kg, respectively. PJ34 at the dose of 3.2 mg/kg significantly reduces cortical damage by 33%; however, 10 mg/kg dosing shows reversed effect (17% reduction)[1]. PJ34 (25 mg/kg) reduces the levels of TNF-α mRNA in ischemic animals by 70% and these values in treated mice do not differ from that of sham or naive animals. Treatment of ischemic mice with PJ34 reduces the level of E-selectin mRNA by 81% and that of ICAM-1 mRNA by 54%, compared to vehicle-treated ischemic mice[2].

    References
    Preparing Stock Solutions
    Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
    1 mM 3.0139 mL 15.0693 mL 30.1386 mL
    5 mM 0.6028 mL 3.0139 mL 6.0277 mL
    10 mM 0.3014 mL 1.5069 mL 3.0139 mL
    Kinase Assay
    [1]

    To assess the PARP-1 or PARP-2 inhibitory activity of FR247304, 3-AB, and PJ34, PARP activity is evaluated with minor modifications. PARP enzyme assay is carried out in a final volume of 100 μL consisting of 50 mM Tris-HCl (pH 8.0), 25 mM MgCl2, 1 mM dithiothreitol, 10 μg activated salmon sperm DNA, 0.1 μCi of [adenylate-32P]NAD, 0.2 units of recombinant human PARP for PARP-1 assay or 0.1 units of recombinant mouse PARP-2 for PARP-2 assay, and various concentrations of FR261529 or 3-AB. The reaction mixture is incubated at room temperature (23°C) for 15 min, and the reaction is terminated by adding 200 μL of ice-cold 20% trichloroacetic acid (TCA) and incubated at 4°C for 10 min. The precipitate is transferred onto GF/B filter and washed three times with 10% TCA solution and 70% ethanol. After the filter is dried, the radioactivity is determined by liquid scintillation counting. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [1]

    PJ34 is dissolved in 100% DMSO at 10 mM and then diluted in DMEM without serum[1].

    PC12 cell cultured are grown in Dulbecco's modified Eagle's medium supplemented with 5% (v/v) fetal calf serum, 5% (v/v) horse serum, and a 1% (v/v) penicillin-streptomycin antibiotics mixture. Cells are grown in an atmosphere of 95% air and 5% CO2 at 37°C. For all experiment, cells are seeded at a density of 4×104 cells/well in 96-well culture plates and allowed to attach overnight. For assessment of cell viability, hydrogen peroxide-induced cytotoxicity is quantified by a standard measurement of LDH release with the use of the LDH assay kit. Briefly, 6 h after hydrogen peroxide exposure, 20 μL of medium of each well is collected, and the solution prepared from LDH assay kit is added. After incubation at room temperature for 30 min, the reaction is stopped by addition of 1 N HCl, and absorbance is measured at 450 nm using a microplate reader. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1][2]

    PJ34 is suspended with 0.5% methylcellulose (Rat)[1].
    PJ34 is dissolved in isotonic saline (NaCl, 0.9%) (Mice)[2].

    Rat[1]
    For transient focal ischemia, 9- to 10-week-old male Wistar rats (weighing 274-380 g) are used. FR247304, PJ34, or 3-AB, which is suspended with 0.5% methylcellulose, is administered at doses of 10 and 32 mg/kg for FR247304, 3.2 and 10 mg/kg for PJ34, or 32 and 100 mg/kg for 3-AB intraperitonially twice at 10 min before MCA occlusion and 10 min before recirculation. The administration volume is adjusted to 2 mL/kg.
    Mice[2]
    Male Swiss albino mice (27-32 g) are used. The PARP inhibitor, PJ34 (1.25, 12.5 or 25 mg/kg) is dissolved in isotonic saline (NaCl, 0.9%) and injected intraperitoneally, in a volume of 10 mL/kg, 15 min before ischemia and again 4 h after the onset of ischemia. Control ischemic mice and sham animals are given vehicle (saline). Naive animals are also included in the studies. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    331.8

    Formula

    C₁₇H₁₈ClN₃O₂

    CAS No.

    344458-15-7

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    PJ34 hydrochloride is prepared in 0.1 mL of distilled water[3].

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    References

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    Product Name:
    PJ34 hydrochloride
    Cat. No.:
    HY-13688
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