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Chemical Structure| 344458-15-7 Chemical Structure| 344458-15-7

Structure of PJ34 HCl
CAS No.: 344458-15-7

Chemical Structure| 344458-15-7

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

Synonyms: PJ-34 (hydrochloride); PJ34 hydrochloride

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Product Details of PJ34 HCl

CAS No. :344458-15-7
Formula : C17H18ClN3O2
M.W : 331.80
SMILES Code : O=C(NC(C=C1C2=C3C=CC=C2)=CC=C1NC3=O)CN(C)C.[H]Cl
Synonyms :
PJ-34 (hydrochloride); PJ34 hydrochloride
MDL No. :MFCD16618379
InChI Key :RURAZZMDMNRXMI-UHFFFAOYSA-N
Pubchem ID :16760621

Safety of PJ34 HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of PJ34 HCl

epigenetics
DNA

Isoform Comparison

Biological Activity

Target
  • PARP

    PARP, EC50:20 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
PE/CA PJ34 1 μM or 10 μM 2 h before and 24 h after RT To evaluate the effect of AZD5363 on the radiosensitivity of tumor cells, results showed that AZD5363 did not enhance the radiosensitivity of any of the 15 cell lines investigated. PMC5709765
endothelial progenitor cells (EPCs) 2 μM 6 hours PJ34 treatment preserved intracellular NAD+levels by inhibiting PARP1 activation and decreasing PAR synthesis, thereby increasing SIRT1 activity and improving the function of aging EPCs. PMC6107962
Human bronchial epithelial cells (BEAS-2B) 10 μM 24 hours PJ34 significantly reduced SiNPs-induced production of cytokines and chemokines, as well as cell death, indicating that PARP activation plays a critical role in SiNPs-induced inflaμMation and cytotoxicity. PMC7281956

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice FaDu and PE/CA PJ34 tumor models Oral 2 mg/kg Twice a week, until death or sacrifice (max 52 weeks) To evaluate the effect of AZD5363 in combination with radiotherapy on tumor control, results showed that AZD5363 significantly improved tumor control when administered as an adjuvant after radiotherapy. PMC5709765
C57BL/6 mice Pulmonary inflammation model Intraperitoneal injection Bicalutamide: 10 mg/kg/day; Docetaxel: 8 mg/kg/week; Doxorubicin: 2.5 mg/kg/week Once a week for 15 days PJ34 significantly alleviated SiNPs-induced pulmonary inflammation and lung injury, indicating that PARP plays a critical role in SiNPs-induced inflammation. PMC7281956
Mice Wilson's disease model Intraperitoneal injection 50 mg/kg Twice daily for 7 days Inhibition of hepatic inflammation improved cognitive and locomotor performance in R778L mice PMC11437830
Mice COVID-19 pneumonia model Intraperitoneal injection 10 mg/kg/d Once daily for 7 days PJ34 alleviates pneumonia by preventing the N protein-induced downregulation of Dicer, XPO5, SRSF3, and hnRNPA3 PMC11322655

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.01mL

0.60mL

0.30mL

15.07mL

3.01mL

1.51mL

30.14mL

6.03mL

3.01mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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