PJ34 hydrochloride

Name: PJ34 hydrochloride
Brand: MedChemExpress
SKU: HY-13688
Rating: 5.0 (26 reviews)

Cat. No.: HY-13688 Purity: 99.91%: FAQs
Data Sheet SDS COA Handling Instructions

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PJ34 hydrochloride is an inhibitor of PARP1/2 with IC₅₀ of 110 nM and 86 nM, respectively.

For research use only. We do not sell to patients.

PJ34 hydrochloride Chemical Structure

CAS No. : 344458-15-7

Size	Price	Stock	Quantity
5 mg	USD 37	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 180	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 288	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 26 publication(s) in Google Scholar

Other Forms of PJ34 hydrochloride:

PJ34 In-stock

25 Publications Citing Use of MCE PJ34 hydrochloride

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

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

PJ34 hydrochloride is an inhibitor of PARP1/2 with IC₅₀ of 110 nM and 86 nM, respectively.

IC₅₀ & Target^[1]

PARP

110 nM (IC₅₀)

PARP-2

86 nM (IC₅₀)

PARP-1

110 nM (IC₅₀)

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

331.80

Formula

C₁₇H₁₈ClN₃O₂

CAS No.

344458-15-7

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NC(C=C1C2=C3C=CC=C2)=CC=C1NC3=O)CN(C)C.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

H₂O : 50 mg/mL (150.69 mM; Need ultrasonic)

DMSO : 10 mg/mL (30.14 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent 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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1 mg/mL (3.01 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (3.01 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1 mg/mL (3.01 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.91%

Select Batch:

Data Sheet (283 KB) SDS (393 KB)

COA (252 KB) HNMR (187 KB) LCMS (92 KB)

Handling Instructions (2659 KB)

References

[1]. Iwashita A, et al. A novel and potent poly(ADP-ribose) polymerase-1 inhibitor, FR247304 (5-chloro-2-[3-(4-phenyl-3,6-dihydro-1(2H)-pyridinyl)propyl]-4(3H)-quinazolinone), attenuates neuronal damage in in vitro and in vivo models of cerebral ischemia. J Ph [Content Brief]

[2]. Haddad M, et al. Anti-inflammatory effects of PJ34, a poly(ADP-ribose) polymerase inhibitor, in transient focal cerebral ischemia in mice. Br J Pharmacol. 2006 Sep;149(1):23-30. [Content Brief]

[3]. Diani-Moore S, et al. NAD+ loss, a new player in AhR biology: prevention of thymus atrophy and hepatosteatosis by NAD+ repletion. Sci Rep. 2017 May 23;7(1):2268. [Content Brief]

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]	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]	Rats^[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	[1]. Iwashita A, et al. A novel and potent poly(ADP-ribose) polymerase-1 inhibitor, FR247304 (5-chloro-2-[3-(4-phenyl-3,6-dihydro-1(2H)-pyridinyl)propyl]-4(3H)-quinazolinone), attenuates neuronal damage in in vitro and in vivo models of cerebral ischemia. J Ph [Content Brief] [2]. Haddad M, et al. Anti-inflammatory effects of PJ34, a poly(ADP-ribose) polymerase inhibitor, in transient focal cerebral ischemia in mice. Br J Pharmacol. 2006 Sep;149(1):23-30. [Content Brief] [3]. Diani-Moore S, et al. NAD+ loss, a new player in AhR biology: prevention of thymus atrophy and hepatosteatosis by NAD+ repletion. Sci Rep. 2017 May 23;7(1):2268. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / H₂O	1 mM	3.0139 mL	15.0693 mL	30.1386 mL	75.3466 mL
	5 mM	0.6028 mL	3.0139 mL	6.0277 mL	15.0693 mL
	10 mM	0.3014 mL	1.5069 mL	3.0139 mL	7.5347 mL
	15 mM	0.2009 mL	1.0046 mL	2.0092 mL	5.0231 mL
	20 mM	0.1507 mL	0.7535 mL	1.5069 mL	3.7673 mL
	25 mM	0.1206 mL	0.6028 mL	1.2055 mL	3.0139 mL
	30 mM	0.1005 mL	0.5023 mL	1.0046 mL	2.5116 mL
H₂O	40 mM	0.0753 mL	0.3767 mL	0.7535 mL	1.8837 mL
	50 mM	0.0603 mL	0.3014 mL	0.6028 mL	1.5069 mL
	60 mM	0.0502 mL	0.2512 mL	0.5023 mL	1.2558 mL
	80 mM	0.0377 mL	0.1884 mL	0.3767 mL	0.9418 mL
	100 mM	0.0301 mL	0.1507 mL	0.3014 mL	0.7535 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.