NK-252
Based on 24 publication(s) in Google Scholar
NK-252 is a potential Nrf2 activator, which exhibits a great Nrf2-activating potential.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.74%
- No. CAS: 1414963-82-8
- Fòrmula: C13H11N5O3
- Peso molecular:285.26
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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
- Pureza y Documentación
- Referencias
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Publications Citing Use of MedChemExpress (MCE) NK-252
More- Nature. 2025 Jan;637(8045):461-469. [Abstract]
- Cell Metab. 2023 Oct 3;35(10):1688-1703.e10. [Abstract]
- Cell Death Dis. 2020 Jul 30;11(7):607. [Abstract]
- Phytomedicine. 2024 Jun:128:155401. [Abstract]
- Int J Biol Macromol. 2025 Jan 20:140133. [Abstract]
- Clin Transl Med. 2024 Apr;14(4):e1661. [Abstract]
- Ecotoxicol Environ Saf. 2024 Nov 5:287:117266. [Abstract]
- Biochem Pharmacol. 2025 Jan 31:116790. [Abstract]
- Biochem Pharmacol. 2024 Jul 28:116456. [Abstract]
- Inflamm Res. 2024 Nov;73(11):1981-1994. [Abstract]
- Drug Des Devel Ther. 2026 Jun 26:20:564608. [Abstract]
- Int Immunopharmacol. 2026 Jul 1:180:116703. [Abstract]
- Int J Mol Sci. 2026 Mar 13;27(6):2646. [Abstract]
- Int J Mol Sci. 2024 Sep 5;25(17):9612. [Abstract]
- Chem Biol Interact. 2023 Oct 27:110788. [Abstract]
- iScience. 2020 Apr.
- Funct Integr Genomics. 2026 May 29;26(1):111. [Abstract]
- Adv Ther (Weinh). 2024 Nov 13.
- Am J Reprod Immunol. 2020 Nov;142:103192. [Abstract]
- Exp Ther Med. 2022 Jun;23(6):394. [Abstract]
- Res Sq. 2025 Nov 19:rs.3.rs-7983397. [Abstract]
- SSRN. 2025 May 27.
- Research Square Preprint. 2023 Oct 28.
- Aging. 2020 Nov 7;12(21):21161-21185. [Abstract]
Customer Validation & Images
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WB
Actividad biológica
Nrf2[1]
The luciferase activity in Huh-7.5 cells treated with Oltipraz (OPZ) or NK-252 shows activation of the NAD(P)H quinone oxidoreductase 1 (NQO1)-ARE in a dose-dependent manner. NK-252 displays this effect with higher potency than OPZ based on the fact that the EC2 value (concentration for a 2-fold induction above background), calculated with linear extrapolation from the values above and below the induction threshold, is 20.8 μM for OPZ and 1.36 μM for NK-252. NK-252 has potential as an Nrf2 activator in hepatic cells. Prototypical Nrf2 activators that include OPZ have been reported to protect microglial cells from H2O2-induced cytotoxicity. The protective effects of OPZ and NK-252 are examined against H2O2-induced cytotoxicity using Huh-7 cells to evaluate their antioxidant properties. The cells treated with OPZ or NK-252 show increased resistance to H2O2-induced cytotoxicity compared with control cells[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 1414963-82-8
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Appearance Solid
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Peso molecular 285.26
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Fòrmula C13H11N5O3
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Color White to off-white
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SMILES
O=C(NCC1=NC=CC=C1)NC2=NN=C(C3=CC=CO3)O2
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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 (24)
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Journal Impact Factor
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Most Recent
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Nature
2025 Jan;637(8045):461-469. PMID: 39743585 -
Cell Metab
Neutrophils resist ferroptosis and promote breast cancer metastasis through aconitate decarboxylase 1. [Abstract]2023 Oct 3;35(10):1688-1703.e10. PMID: 37793345 -
Cell Death Dis
ω-6 Polyunsaturated fatty acids (linoleic acid) activate both autophagy and antioxidation in a synergistic feedback loop via TOR-dependent and TOR-independent signaling pathways. [Abstract]2020 Jul 30;11(7):607. PMID: 32732901
NK-252 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2020 Jul 30;11(7):607. [Abstract]
The levels of nuclear Nrf2 and the mRNA expression levels of Nrf2, SOD1, SOD3, CAT, and Gpx are significantly increased after LA+NK-252 (2 μM) treatment.
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Phytomedicine
Ethanol extract of Eclipta prostrata induces multiple myeloma ferroptosis via Keap1/Nrf2/HO-1 axis. [Abstract]2024 Jun:128:155401. PMID: 38507850 -
Int J Biol Macromol
Chlorogenic acid mitigates heat stress-induced oxidative damage in bovine mammary epithelial cells by inhibiting NF-κB-mediated NLRP3 inflammasome activation via upregulating the Nrf2 signaling pathway. [Abstract]2025 Jan 20:140133. PMID: 39842566 -
Clin Transl Med
ACOD1, rather than itaconate, facilitates p62-mediated activation of Nrf2 in microglia post spinal cord contusion. [Abstract]2024 Apr;14(4):e1661. PMID: 38644791 -
Ecotoxicol Environ Saf
Aristolochic acid-induced dyslipidemia and hepatotoxicity: The potential role of FXR and AHR receptors. [Abstract]2024 Nov 5:287:117266. PMID: 39509784 -
Biochem Pharmacol
WWOX-mediated p53/SAT1 and NRF2/FPN1 axis contribute to toosendanin-induced ferroptosis in hepatocellular carcinoma. [Abstract]2025 Jan 31:116790. PMID: 39894307 -
Biochem Pharmacol
Furanodienone induces apoptosis via regulating the PRDX1/MAPKs/p53/caspases signaling axis through NOX4-derived mitochondrial ROS in colorectal cancer cells. [Abstract]2024 Jul 28:116456. PMID: 39079582 -
Inflamm Res
Cynarin inhibits microglia-induced pyroptosis and neuroinflammation via Nrf2/ROS/NLRP3 axis after spinal cord injury. [Abstract]2024 Nov;73(11):1981-1994. PMID: 39340662 -
Drug Des Devel Ther
Plumbagin Induces Ferroptosis in Nonfunctioning Pituitary Adenomas via Nrf2/FTH1-Dependent Ferritinophagy. [Abstract]2026 Jun 26:20:564608. PMID: 42381973 -
Int Immunopharmacol
Zinc deficiency exacerbates and supplementation attenuates early-stage obesity-related podocyte injury via Nrf2/HO-1-mediated pyroptosis. [Abstract]2026 Jul 1:180:116703. PMID: 42025422 -
Int J Mol Sci
LRRC8A Inhibition Overcomes Chemoresistance by Downregulating MRP3 and CYP3A4 in the 3D Spheroid Model of Human Breast Cancer Cells. [Abstract]2026 Mar 13;27(6):2646. PMID: 41898509 -
Int J Mol Sci
Downregulation of IL-8 and IL-10 by LRRC8A Inhibition through the NOX2-Nrf2-CEBPB Transcriptional Axis in THP-1-Derived M2 Macrophages. [Abstract]2024 Sep 5;25(17):9612. PMID: 39273558 -
Chem Biol Interact
Shikonin promotes ferroptosis in HaCaT cells through Nrf2 and alleviates imiquimod-induced psoriasis in mice. [Abstract]2023 Oct 27:110788. PMID: 39491143 -
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Funct Integr Genomics
DIA-based proteomic analysis reveals Scutellaria barbata D. Don Exosome-like nanovesicles promote ferroptosis in HCC through Nrf2/SLC7A11/GPX4 pathway. [Abstract]2026 May 29;26(1):111. PMID: 42209785 -
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Am J Reprod Immunol
Inhibition of TLR2/TLR4 alleviates the Neisseria gonorrhoeae infection damage in human endometrial epithelial cells via Nrf2 and NF-Kβsignaling. [Abstract]2020 Nov;142:103192. PMID: 32950783 -
Exp Ther Med
Oxaliplatin induces ferroptosis and oxidative stress in HT29 colorectal cancer cells by inhibiting the Nrf2 signaling pathway. [Abstract]2022 Jun;23(6):394. PMID: 35495610 -
Res Sq
Dietary Polyunsaturated Fatty Acids Regulate Dendritic Cell Function via Nrf2-dependent Control of Ferroptosis. [Abstract]2025 Nov 19:rs.3.rs-7983397. PMID: 41333438 -
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Aging
Tim-3 deteriorates neuroinflammatory and neurocyte apoptosis after subarachnoid hemorrhage through the Nrf2/HMGB1 signaling pathway in rats. [Abstract]2020 Nov 7;12(21):21161-21185. PMID: 33168786
Solvente y solubilidad
DMSO : ≥ 29 mg/mL (101.66 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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: ≥ 2.08 mg/mL (7.29 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (7.29 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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
The Huh-7.5 cells, a subline derived from Huh-7 cells, are transfected with ARE/pGL4.32 by lipofectamine LTX. The stable clonal transfectant is isolated by selection in hygromycin B (0.1 mg/mL). Cells derived from stable clones are transfected with control or Nrf2 small interfering RNA by lipofectamine RNAiMAX (30 hours), then treated with OPZ, NK-252 (0.1-30 μM, 16 hours) , or DMSO alone (control). The luciferase activity values are measured using the Steady-Glo Luciferase Assay System[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rats[1]
Six-week-old male Fischer 344 rats are randomly divided into four compound administration groups and four control groups. Compound administration groups of rats fed a CDAA diet receive oral administration as follows: 1) OPZ from 1 week after feeding at a dose of 60 mg/kg once daily for 9 weeks (CDAA+OPZ group; N=8), 2) NK-252 from 1 week after feeding at a dose of 20 mg/kg once daily for 9 weeks (CDAA+NK-252_low group; N=8), 3) NK-252 from 1 week after feeding at a dose of 60 mg/kg once daily for 9 weeks (CDAA+NK-252_high group; N=8), or 4) NK-252 from 6 weeks after feeding at a dose of 60 mg/kg once daily for 4 weeks (CDAA+NK-252_delayed administration: DA group; N=7). Two control groups of rats are fed a CDAA diet for 6 or 10 weeks (pre-CDAA control or CDAA control group; N=9 each), and the other two control groups of rats are fed standard rodent chow (CRF-1) for 6 or 10 weeks (prenaive or naive; N=3 each). Laparotomy and blood sampling are performed under isoflurane anesthesia. After blood sampling, rats are euthanized by exsanguination under isoflurane anesthesia, and the livers are immediately extirpated.
[2]Mice[2]
Six- to 8-week-old male BALB/c x DBA/2 F1 (hereafter called CD2F1) mice weighing 22 to 26 g are used. Male CD2F1 mice are inoculated i.p. with 106 cells of P388/S and P388/VCR cell line on day 0. Each group consist of six mice. NK-250 and NK-252 (100, 300, and 1000 mg/kg) are given p.o. daily from day 1 to 5. Mean survival days and the range of survival days are analysed.
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 (280 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]. Shimozono R et al. Nrf2 activators attenuate the progression of nonalcoholic steatohepatitis-related fibrosis in a dietary rat model. Mol Pharmacol. 2013 Jul, 84(1):62-70. [Content Brief]
[2]. Kiue A, et al. Enhancement of antitumour activity of etoposide by dihydropyridines on drug-sensitive and drug-resistant leukaemia in mice. Br J Cancer. 1991 Aug;64(2):221-6. [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 | 3.5056 mL | 17.5279 mL | 35.0557 mL | 87.6393 mL |
| 5 mM | 0.7011 mL | 3.5056 mL | 7.0111 mL | 17.5279 mL | |
| 10 mM | 0.3506 mL | 1.7528 mL | 3.5056 mL | 8.7639 mL | |
| 15 mM | 0.2337 mL | 1.1685 mL | 2.3370 mL | 5.8426 mL | |
| 20 mM | 0.1753 mL | 0.8764 mL | 1.7528 mL | 4.3820 mL | |
| 25 mM | 0.1402 mL | 0.7011 mL | 1.4022 mL | 3.5056 mL | |
| 30 mM | 0.1169 mL | 0.5843 mL | 1.1685 mL | 2.9213 mL | |
| 40 mM | 0.0876 mL | 0.4382 mL | 0.8764 mL | 2.1910 mL | |
| 50 mM | 0.0701 mL | 0.3506 mL | 0.7011 mL | 1.7528 mL | |
| 60 mM | 0.0584 mL | 0.2921 mL | 0.5843 mL | 1.4607 mL | |
| 80 mM | 0.0438 mL | 0.2191 mL | 0.4382 mL | 1.0955 mL | |
| 100 mM | 0.0351 mL | 0.1753 mL | 0.3506 mL | 0.8764 mL |
NK-252 Related Classifications
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