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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C17H17N3O2.HCl |
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分子量 | 331.8 | CAS No. | 344458-15-7 | |
Solubility (25°C)* | 体外 | DMSO | 66 mg/mL (198.91 mM) | |
Water | 66 mg/mL (198.91 mM) | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | PJ34 HCl is the hydrochloride salt of PJ34, which is a PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1/2. |
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in vitro | PJ34 is a potent, phenanthridinone PARS inhibitor, which is approximately 10,000 times more potent than the prototypical PARS inhibitor 3-aminobenzamide. PJ34 inhibited peroxynitrite-induced cell necrosis with EC50 of 20 nM. PJ34 provides cardioprotection by decreasing myocardial infarct size and enhancing postischemic regional and global functional recovery. [1] |
in vivo | PJ34 suppresses the development of clinical signs of EAE in MBP-immunized PLSJL mice. PJ34 exerted therapeutic effects at the onset of EAE that are associated with reduced CNS inflammation and the maintenance of neurovascular integrity. PJ34 partially inhibits the expression of TNF-α and ICAM-1 in the Spinal Cord Tissues of MBP-Immunized Mice.[2] PJ34 provides significant, dose-dependent, anti-inflammatory effects in a variety of local inflammation models. PJ34 dose-dependently suppresses neutrophil infiltration and nitric oxide (but not KC and IL-1β) production in peritonitis. In a model of systemic endotoxemia, PJ34 pretreatment significantly reduces plasma levels of TNF-α, IL-1β and nitrite/nitrate (breakdown products of nitric oxide) production. PJ34 treatment (oral gavage) induces a significant suppression of the inflammatory response in dextran sulfate colitis, multiple low dose streptozotocin diabetes and cyclophosphamide-accelerated autoimmune diabetes in the non-obese diabetic mice, and reduces the degree of mononuclear cell infiltration into the iris in an endotoxin-induced uveitis model. [3] |
特徴 | Water-soluble PARP1/2 inhibitor with >10,000-fold potentcy vs. 3-aminobenzamide (prototypical PARP inhibitor). Potential uses in cardiovascular diseases (stroke, cerebral ischemia, & myocardial ischemia). |
動物実験 | 動物モデル | Female PLSJL mice |
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投薬量 | 10 mg/kg b.wt. twice daily | |
投与方法 | orally |
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Data from [Data independently produced by , , PLoS One, 2014, doi:10.1371/journal.pone.0114583]
Data from [Data independently produced by , , Brain Res, 2016, 1644:32-8]
Data from [Data independently produced by , , Brain Res, 2016, 1644:32-8.]
Targetable lesions and proteomes predict therapy sensitivity through disease evolution in pediatric acute lymphoblastic leukemia [ Nat Commun, 2023, 14(1):7161] | PubMed: 37989729 |
Regulation of Rad52-dependent replication fork recovery through serine ADP-ribosylation of PolD3 [ Nat Commun, 2023, 14(1):4310] | PubMed: 37463936 |
PARP inhibitor shuts down the global translation of thyroid cancer through promoting Pol II binding to DIMT1 pause [ Int J Biol Sci, 2023, 19(12):3970-3986] | PubMed: 37564214 |
Nuclear DJ-1 Regulates DNA Damage Repair via the Regulation of PARP1 Activity [ Int J Mol Sci, 2023, 24(10)8651] | PubMed: 37239999 |
PARP14 is a novel target in STAT6 mutant follicular lymphoma [ Leukemia, 2022, 36(9):2281-2292] | PubMed: 35851155 |
PARP14 is a novel target in STAT6 mutant follicular lymphoma [ Leukemia, 2022, 36(9):2281-2292] | PubMed: 35851155 |
The lactate-NAD+ axis activates cancer-associated fibroblasts by downregulating p62 [ Cell Rep, 2022, 39(6):110792] | PubMed: 35545049 |
Parthanatos participates in glutamate-mediated HT22 cell injury and hippocampal neuronal death in kainic acid-induced status epilepticus rats [ CNS Neurosci Ther, 2022, 28(12):2032-2043] | PubMed: 35909335 |
Poly (ADP-ribose) polymerase 1-mediated defective mitophagy contributes to painful diabetic neuropathy in the db/db model [ J Neurochem, 2022, 10.1111/jnc.15606] | PubMed: 35263449 |
SPINDOC binds PARP1 to facilitate PARylation [ Nat Commun, 2021, 12(1):6362] | PubMed: 34737271 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。