| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Poly(ADP-ribose) polymerase-1 (PARP-1). 1,5-Isoquinolinediol also inhibits NOS2 (inducible nitric oxide synthase) and PARS. PARP-1 is an enzyme involved in DNA repair and cellular responses to oxidative stress.
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| ln Vitro |
In stably integrated HSV tk gene mutation correction, 1,5-isoquinolinediol upregulates gene targeting absolute frequency by up to 8 times [1]. Strong PARP antagonist 1,5-isoquinolinediol lowers PARP cleavage in diabetic retinas. Retinal Muller cells' upregulation of cleaved PARP-1 expression caused by H2O2 is attenuated by 1,5-isoquinolinediol (500 μM H2O2; 24 hours). Retinal nitrated protein expression is upregulated in diabetes; however, 1,5-isoquinolinediol attenuates this effect. In the retina, diabetes-induced activation of NADPH oxidase is attenuated by 1,5-isoquinolinediol [2].
1,5-Isoquinolinediol inhibits PARP1 with an IC50 of 0.39 μM (reported range 0.18–1.00 μM across studies). By inhibiting PARP-1, the compound modulates DNA repair pathways and cellular responses to oxidant stress. It also inhibits NOS2, contributing to its neuroprotective effects. |
| ln Vivo |
1,5-Isoquinolinediol has been used in animal studies to investigate the role of PARP-1 in various disease models. Its neuroprotective properties have been demonstrated in models of nitric oxide-mediated neurotoxicity. The compound shows potential in models of oxidant stress-induced cell death.
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| Enzyme Assay |
Enzyme inhibition assays are performed using recombinant PARP-1 enzyme. 1,5-Isoquinolinediol is incubated with the enzyme and the substrate NAD⁺, and the inhibition of PARP-1 activity is measured. The IC50 value is determined from dose-response curves.
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| Cell Assay |
Cell-based assays are conducted using various cell lines to evaluate the compound's effects on DNA repair and cell death. Cells are treated with 1,5-Isoquinolinediol in the presence or absence of DNA-damaging agents or oxidative stress, and cell viability and PARP activity are assessed.
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| Animal Protocol |
In vivo studies are performed in animal models of neurodegenerative diseases, ischemia/reperfusion injury, or other conditions involving PARP-1 activation. 1,5-Isoquinolinediol is administered, and neuroprotective or cytoprotective effects are evaluated.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of 1,5-Isoquinolinediol have been characterized in preclinical studies. The compound is soluble in DMSO (20 mg/mL) and can be used in both in vitro and in vivo settings. Detailed PK parameters would require further investigation.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for 1,5-Isoquinolinediol are not extensively reported in the available literature. The compound is intended for research use only. Its use as a PARP inhibitor in various disease models suggests it is well-tolerated at research doses.
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| References | |
| Additional Infomation |
Isoquinoline-1,5-diol is an isoquinoline alcohol, a derivative of isoquinoline in which the hydrogen atoms at positions 1 and 5 are replaced by hydroxyl groups. It is an EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor.
1,5-Isoquinolinediol is a research tool for studying PARP-1 biology and evaluating the therapeutic potential of PARP inhibition in cancer, neurodegeneration, and inflammation. It has been identified as an anti-inflammatory, anticancer, and anti-aging agent. The compound is not approved for clinical use. |
| Molecular Formula |
C₉H₇NO₂
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|---|---|
| Molecular Weight |
161.16
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| Exact Mass |
161.047
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| CAS # |
5154-02-9
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| PubChem CID |
1340
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| Appearance |
Off-white to gray solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
501.1±30.0 °C at 760 mmHg
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| Melting Point |
270-275 °C
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| Flash Point |
256.8±24.6 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.743
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| LogP |
-0.17
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
12
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| Complexity |
225
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
LFUJIPVWTMGYDG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H7NO2/c11-8-3-1-2-7-6(8)4-5-10-9(7)12/h1-5,11H,(H,10,12)
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| Chemical Name |
5-hydroxy-2H-isoquinolin-1-one
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| Synonyms |
1,5 Isoquinolinediol 1,5 Isoquinolinediol
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~37.04 mg/mL (~229.83 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (12.91 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 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL 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: ≥ 2.08 mg/mL (12.91 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 20.8 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: ≥ 2.08 mg/mL (12.91 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 6.2050 mL | 31.0251 mL | 62.0501 mL | |
| 5 mM | 1.2410 mL | 6.2050 mL | 12.4100 mL | |
| 10 mM | 0.6205 mL | 3.1025 mL | 6.2050 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.
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