NQDI-1
Based on 6 publication(s) in Google Scholar
NQDI-1 inhibits apoptosis signal-regulating kinase 1 (ASK1) with a Ki of 500 nM and an IC50 of 3 μM.
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- Pureza: 98.11%
- No. CAS: 175026-96-7
- Fòrmula: C19H13NO4
- Peso molecular:319.31
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
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- Referencias
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Publications Citing Use of MedChemExpress (MCE) NQDI-1
More- Cell Death Discov. 2018 Apr 27:4:47. [Abstract]
- J Agric Food Chem. 2024 Apr 10;72(14):7832-7844. [Abstract]
- Ecotoxicol Environ Saf. 2021 Apr 15:213:112066. [Abstract]
- Toxicol Appl Pharmacol. 2018 Nov 15:359:34-46. [Abstract]
- Endocrine. 2020 Apr;68(1):103-115. [Abstract]
- Biochem Biophys Res Commun. 2019 Nov 26;520(1):211-217. [Abstract]
Ver todos los productos específicos de isoformas MAP3K
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Actividad biológica
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ASK1 500 nM (Ki) |
ASK1 3 μM (IC50) |
The selectivity of NQDI-1 is evaluated in vitro on four serine/threonine protein kinases (protein kinase CK2 (CK2), c-Jun N-terminal kinase 3 (JNK3), Rho-associated protein kinase 1 (Rock1), and Aurora A) and three tyrosine protein kinases (FGFR1, hHGFR, and endothelial TEK tyrosine kinase (Tie2)). The results show that NQDI-1 is a selective inhibitor of ASK1. The activity of FGFR1 protein kinase is inhibited by NQDI-1 (residual activity of 44%). NQDI-1 inhibits ASK1 with a Ki of 500 nM. Inhibition of ASK1 by NQDI-1 is competitive with respect to the phosphodonor substrate ATP[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 175026-96-7
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Appearance Solid
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Peso molecular 319.31
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Fòrmula C19H13NO4
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Color Yellow to orange
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SMILES
O=C(C1=C2C3=C(NC1=O)C=CC=C3C(C4=C2C=CC=C4)=O)OCC
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (6)
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Journal Impact Factor
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Most Recent
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Cell Death Discov
Dual function of peroxiredoxin I in lipopolysaccharide-induced osteoblast apoptosis via reactive oxygen species and the apoptosis signal-regulating kinase 1 signaling pathway. [Abstract]2018 Apr 27:4:47. PMID: 29707240 -
J Agric Food Chem
Lycopene Alleviates Endoplasmic Reticulum Stress in Steatohepatitis through Inhibition of the ASK1-JNK Signaling Pathway. [Abstract]2024 Apr 10;72(14):7832-7844. PMID: 38544357 -
Ecotoxicol Environ Saf
Microcystin-LR induces ovarian injury and apoptosis in mice via activating apoptosis signal-regulating kinase 1-mediated P38/JNK pathway. [Abstract]2021 Apr 15:213:112066. PMID: 33610944 -
Toxicol Appl Pharmacol
Berberine modulates ASK1 signaling mediated through TLR4/TRAF2 via upregulation of miR-23a. [Abstract]2018 Nov 15:359:34-46. PMID: 30240693 -
Endocrine
Inhibition of thioredoxin 2 by intracellular methylglyoxal accumulation leads to mitochondrial dysfunction and apoptosis in INS-1 cells. [Abstract]2020 Apr;68(1):103-115. PMID: 31939094 -
Biochem Biophys Res Commun
NQDI-1 protects against acinar cell necrosis in three experimental mouse models of acute pancreatitis. [Abstract]2019 Nov 26;520(1):211-217. PMID: 31587872
Solvente y solubilidad
DMSO : 10 mg/mL (31.32 mM; Need ultrasonic and warming; 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 0.71 mg/mL (2.22 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 0.71 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.1 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 0.71 mg/mL (2.22 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 0.71 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.1 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
Enzyme activity of human protein kinases ASK1, Aurora A, ROCK1, HGFR, FGFR1, Tie2, JNK3, and CK2 is determined using in vitro kinase assay (γ-32P-ATP method). Each reaction mixture contains 6 μL of buffer solution (25 mM MOPS, pH 7.2, 2.5 mM EGTA, 2.5 mM EDTA, 0.5 mM DTT, 0.25 mg/mL BSA, 20 mM β-glycerophosphate), 3 μL of substrate solution (MBP, Long S6 kinase substrate peptide, KKKSPGEYVNIEFG, IGF-IRtide (12-527), TK substrate 2, JNK3tide, or RRRDDDSDDD for each kinase, respectively) (5.0 μg/μL), 0.3 μL of enzyme (protein kinase catalytic subunit, 0.1 μg/μL≈32 mU/μL), and 10.25 μL of H2O. The reaction mixture (total volume of 19 μL) is quickly added to 1.5 mL tubes at room temperature. The stock solutions of inhibitors (e.g., NQDI-1) are prepared in DMSO, and the concentration of inhibitor is 1 mM. The concentration of DMSO in the reaction does not exceed 3%. Then 1 μL of inhibitor solution in DMSO is added to each tube and mixed by pipetting. ATP solution is prepared separately. For each sample 0.05 mCi γ-[P32]ATP is taken (specific activity of 100 μCi/μM). The total concentration of labeled and unlabeled ATP is 100 μM. The reaction is started with addition of ATP solution (150 μM ATP, 30 mM MgCl2, 15 mM MOPS, pH 7.2). The time of reaction is 20 min at 30°C. The reaction is stopped by adding 20 μL of 0.5 M orthophosphoric acid. Then the reaction mixture is loaded on the 20 mm filter disks of the cellulose phosphate paper. Filters are washed three times with 0.075 M orthophosphoric acid at room temperature and dried. For detection of products, dried filters are counted by Tri-Carb 2800-TR liquid scintillation analyzer. Then 1 μL of DMSO is added to the reaction volume instead of the inhibitor stock solution for a positive control[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rats[2]
A total of 12 female Sprague-Dawley rats with litters of mixed gender pups are used. The mothers are housed at 25°C under a 12-h light/dark cycle, with ad libitum access to food and water, until the pups are 7-days-old. The HI model is established. The pups are anesthetized with 2.5% halothane and are intracerebroventricularly infused with DMSO or 250 nmol NQDI-1, dissolved in DMSO into the right cerebral hemisphere 30 min prior to HI using a 30-gauge needle with a 5 μL Hamilton syringe (infusion rate, 1 μL/min).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (287 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Volynets GP, et al. Identification of 3H-naphtho[1,2,3-de]quinoline-2,7-diones as inhibitors of apoptosis signal-regulating kinase 1 (ASK1). J Med Chem. 2011 Apr 28;54(8):2680-6. [Content Brief]
[2]. Hao H, et al. NQDI-1, an inhibitor of ASK1 attenuates acute perinatal hypoxic-ischemic cerebral injury by modulating cell death. Mol Med Rep. 2016 Jun;13(6):4585-92. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1318 mL | 15.6588 mL | 31.3175 mL | 78.2938 mL |
| 5 mM | 0.6264 mL | 3.1318 mL | 6.2635 mL | 15.6588 mL | |
| 10 mM | 0.3132 mL | 1.5659 mL | 3.1318 mL | 7.8294 mL | |
| 15 mM | 0.2088 mL | 1.0439 mL | 2.0878 mL | 5.2196 mL | |
| 20 mM | 0.1566 mL | 0.7829 mL | 1.5659 mL | 3.9147 mL | |
| 25 mM | 0.1253 mL | 0.6264 mL | 1.2527 mL | 3.1318 mL | |
| 30 mM | 0.1044 mL | 0.5220 mL | 1.0439 mL | 2.6098 mL |
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