5-Hydroxyisoquinoline
Based on 1 Customer Validation
5-Hydroxyisoquinoline is a SARM1 inhibitor, IC50 = 2.6 μM, with axon-protective activity. 5-Hydroxyisoquinoline binds to and inhibits the NADase catalytic activity of the SARM1 protein TIR domain, reducing SARM1-mediated NAD+ depletion and cADPR production. 5-Hydroxyisoquinoline can be used in research on SARM1-related diseases; it can also serve as an intermediate for research related to organic synthesis.
For research use only. We do not sell to patients.
- Purity : 98.0%
- CAS No.: 2439-04-5
- Formula: C9H7NO
- Molecular Weight:145.16
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
Description
In Vitro
5-Hydroxyisoquinoline (compound 3) inhibits recombinant human SARM1 SAM-TIR NADase activity with an IC50 of 2.6 µM in a cell-free SAM-TIR NADase assay[1].
5-Hydroxyisoquinoline dose-dependently reduces axonal fragmentation in cultured DRG neurons from mice with transection injury, and its protective activity is weaker than that of DSRM-3716 (HY-W021879)[1].
5-Hydroxyisoquinoline (compound 1) can be used as a precursor to react and obtain a series of 5-hydroxyisoquinolinium bromides 7-11[2].
5-Hydroxyisoquinoline is a key aromatic ring-fused structural fragment in the κ opioid receptor agonist GR86014[3].
Synthesis of iso-QP[5] using 5-Hydroxyisoquinoline as a precursor aromatic hydrocarbon derivative[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2439-04-5
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Appearance Solid
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Molecular Weight 145.16
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Formula C9H7NO
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Color Light yellow to brown
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SMILES
C1=CC=C(C2=CC=NC=C12)O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 5 mg/mL (34.44 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)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Hughes RO, et al. Small Molecule SARM1 Inhibitors Recapitulate the SARM1 Phenotype and Allow Recovery of a Metastable Pool of Axons Fated to Degenerate. Cell reports. 2021 Jan 05;34(1):108588. [Content Brief]
[2]. Soukup O, et al. Synthesis, antimicrobial evaluation and molecular modeling of 5-hydroxyisoquinolinium salt series; the effect of the hydroxyl moiety. Bioorganic & medicinal chemistry. 2016 Feb 15;24(4):841-8. [Content Brief]
[5]. He M, et al. Synthesis and Anti-Toxoplasma Activity In vitro of Arctigenin Derivatives. Letters in Drug Design & Discovery. 2024 Dec;21(19):4949-61. [Content Brief]
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 6.8889 mL | 34.4447 mL | 68.8895 mL | 172.2237 mL |
| 5 mM | 1.3778 mL | 6.8889 mL | 13.7779 mL | 34.4447 mL | |
| 10 mM | 0.6889 mL | 3.4445 mL | 6.8889 mL | 17.2224 mL | |
| 15 mM | 0.4593 mL | 2.2963 mL | 4.5926 mL | 11.4816 mL | |
| 20 mM | 0.3444 mL | 1.7222 mL | 3.4445 mL | 8.6112 mL | |
| 25 mM | 0.2756 mL | 1.3778 mL | 2.7556 mL | 6.8889 mL | |
| 30 mM | 0.2296 mL | 1.1482 mL | 2.2963 mL | 5.7408 mL |
Keywords
- 5-Hydroxyisoquinoline
- 2439-04-5
- Toll-like Receptor (TLR)
- Drug Intermediate
- NADase-mediated NAD+ hydrolysis
- SARM1 inhibitor
- apoptosis
- apoptosis-related gene expression
- breast cancer
- breast cancer cells
- cell-free SAM-TIR NADase assay
- proliferation
- recombinant human SARM1 SAM-TIR NADase
- κ-opioid receptor activator
- Inhibitor
- inhibitor
- inhibit