| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| Other Sizes |
|
Purity: ≥98%
PJ34 HCl, the hydrochloride of PJ34, is a novel, potent and selective inhibitor of poly(ADP-ribose) polymerase (PARP) with potential anticancer and neuro-protective activities. In a cell-free assay, it inhibits PARP with an EC50 value of 20 nM. In a variety of tumor types, PJ34 has neuro-protective properties and can strengthen the effects of chemotherapy.
| Targets |
PARP ( IC50 = 110 nM ); PARP-2 ( IC50 = 86 nM ); PARP-1 ( IC50 = 110 nM )
|
|
|---|---|---|
| ln Vitro |
|
|
| ln Vivo |
|
|
| Enzyme Assay |
Minor modifications are made to PARP activity in order to evaluate the inhibitory activity of PARP-1 or PARP-2 of FR247304, 3-AB, and PJ34. The PARP enzyme assay is performed in a final volume of 100 μL with the following contents: 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 mouse PARP-2 for the PARP-2 assay, 0.1 units of recombinant human PARP for the PARP-1 assay, and different concentrations of FR261529 or 3-AB. The reaction is stopped by adding 200 μL of ice-cold 20% trichloroacetic acid (TCA) and incubating at 4°C for 10 minutes.The reaction mixture is then incubated at room temperature (23°C) for 15 minutes. Following three rounds of washing with 70% ethanol and 10% TCA solution, the precipitate is moved to a GF/B filter. Liquid scintillation counting determines the radioactivity after the filter has dried.
|
|
| Cell Assay |
PC12 cell cultures are maintained in Dulbecco's modified Eagle's medium, which is supplemented with 1% (v/v) of penicillin-streptomycin antibiotic mixture, 5% (v/v) of horse serum, and 5% (v/v) of fetal calf serum. At 37°C, cells are grown in an environment consisting of 95% air and 5% CO2. In every experiment, 96-well culture plates are seeded with 4×104 cells/well and left overnight for the cells to attach. Hydrogen peroxide-induced cytotoxicity is measured using an LDH assay kit to measure LDH release as a standard method of assessing cell viability. In summary, 20 μL of the medium from each well is collected 6 hours after the hydrogen peroxide exposure, and the LDH assay kit solution is added. The reaction is halted by adding 1 N HCl after 30 minutes of room temperature incubation, and absorbance is measured at 450 nm using a microplate reader.
|
|
| Animal Protocol |
|
|
| References |
|
|
| Additional Infomation |
PJ34 hydrochloride is a hydrochloride salt prepared from equimolar amounts of PJ34 and hydrochloric acid. It has a role as an angiogenesis inhibitor, an anti-inflammatory agent, an antiatherosclerotic agent, an antineoplastic agent, an apoptosis inducer, a cardioprotective agent, an EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor and a neuroprotective agent. It contains a PJ34(1+).
|
| Molecular Formula |
C17H17N3O2.HCL
|
|
|---|---|---|
| Molecular Weight |
331.8
|
|
| Exact Mass |
331.11
|
|
| Elemental Analysis |
C, 61.54; H, 5.47; Cl, 10.68; N, 12.66; O, 9.64
|
|
| CAS # |
344458-15-7
|
|
| Related CAS # |
|
|
| PubChem CID |
16760621
|
|
| Appearance |
Light yellow to yellow solid powder
|
|
| Boiling Point |
539.1ºC at 760 mmHg
|
|
| Flash Point |
279.9ºC
|
|
| LogP |
3.114
|
|
| Hydrogen Bond Donor Count |
3
|
|
| Hydrogen Bond Acceptor Count |
3
|
|
| Rotatable Bond Count |
3
|
|
| Heavy Atom Count |
23
|
|
| Complexity |
438
|
|
| Defined Atom Stereocenter Count |
0
|
|
| SMILES |
Cl[H].O=C1C2=C([H])C([H])=C([H])C([H])=C2C2C([H])=C(C([H])=C([H])C=2N1[H])N([H])C(C([H])([H])N(C([H])([H])[H])C([H])([H])[H])=O
|
|
| InChi Key |
RURAZZMDMNRXMI-UHFFFAOYSA-N
|
|
| InChi Code |
InChI=1S/C17H17N3O2.ClH/c1-20(2)10-16(21)18-11-7-8-15-14(9-11)12-5-3-4-6-13(12)17(22)19-15;/h3-9H,10H2,1-2H3,(H,18,21)(H,19,22);1H
|
|
| Chemical Name |
2-(dimethylamino)-N-(6-oxo-5H-phenanthridin-2-yl)acetamide;hydrochloride
|
|
| Synonyms |
PJ-34 hydrochloride; PJ-34 HCl; PJ-34; PJ34; PJ 34
|
|
| HS Tariff Code |
2934.99.9001
|
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
|
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (3.01 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1 mg/mL (3.01 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1 mg/mL (3.01 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 30% PEG400+0.5% Tween80+5% propylene glycol: 14 mg/mL |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
