Nivitol
Based on 1 Customer Validation
Nivitol (UP302) is a natural phenolic compound discovered from Dianella ensifolia and also acts as a Tyrosinase inhibitor. Nivitol competitively and reversibly inhibits tyrosinase, suppressing melanin production. Nivitol inhibits homogentisate 1,2-dioxygenase (HGD). In human leukemia cells, Nivitol inhibits PI3K/AKT pathway phosphorylation, increases ROS, decreases mitochondrial membrane potential, and induces G2/M cell cycle arrest, apoptosis, and PINK1/Parkin-mediated mitophagy. Nivitol exhibits inhibition of tumor growth in the MV411 xenograft mouse model. Nivitol is used for research on exogenous ochronosis, hyperpigmentation, and leukemia.
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- Pureté : 98.41%
- CAS No.: 869743-37-3
- Formule: C18H22O4
- Masse moléculaire:302.37
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[3]|
Bax |
Akt |
PI3K |
Bcl-2 |
Caspase 3 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| B16-F1 | IC50 |
15 μM
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Inhibition of melanin production in murine B16-F1 melanoma cells incubated for 72 hrs in the presence of 2 nM alpha-MSH measured by absorbance at 490 nm.
Inhibition of melanin production in murine B16-F1 melanoma cells incubated for 72 hrs in the presence of 2 nM alpha-MSH measured by absorbance at 490 nm.
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18758104 |
In Vitro
Nivitol (UP302) is a novel, potent, competitive, and reversible mushroom tyrosinase inhibitor with a Ki of 0.3 μM; it inhibits DOPA oxidase activity in B16-F1 mouse melanoma cell homogenates with an IC50 of 12 μM[2].
Nivitol (0-62 μM; 72 h) inhibits melanin production in B16-F1 cells and primary human epidermal melanocytes with IC50 values of 15 μM and 8 μM, respectively, and exhibits no cytotoxicity at concentrations up to 62 μM[2].
Nivitol (0.05-0.1%; 4-14 days) significantly inhibits melanogenesis in reconstructed human skin[2].
Nivitol (UP302) (20-120 μM; 48 h) inhibits the growth of MV411 and K562 human leukemia cell lines[3].
Nivitol (30-120 μM; 16 h) induces ROS production and decreases mitochondrial membrane potential in MV411 and K562 cells[3].
Nivitol (40-100 μM; 16 h) induces apoptosis in MV411 and K562 cells[3].
UP302 (30-90 μM; 16 h) alters the expression of apoptosis-related proteins in MV411 and K562 cells; activates mitophagy through the PINK1/Parkin pathway; inhibits the activation of the PI3K/AKT signaling pathway[3].
UP302 (50-100 μM; 16-48 h) induces autophagy and mitophagy in MV411 and K562 cells, and UP302-induced autophagy exerts a protective effect on leukemia cells MV411 and K562[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV411 and K562
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Concentration:20, 40, 60, 80, 100, 120 μM
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Incubation Time:48 h
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Result:Exhibited antiproliferative activity against leukemia cells MV411 and K562.
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Cell Line:MV411 and K562
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Concentration:0, 40, 60, 80, 100 μM
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Incubation Time:16 h
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Result:Significantly increased apoptosis in both MV411 and K562 compared to the control group.
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Cell Line:MV411 and K562
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Concentration:30, 60, 90 μM
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Incubation Time:16 h
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Result:Overexpressed AIF, Bax, and active-caspase 3.
Down-regulated relative protein levels of Bcl-2 compared with the control group.\nDramatically increased levels of LC3-II compared with the control group.
Upregulated expression levels of both PINK1 and Parkin.\nSignificantly inhibited the phosphorylation of PI3K/AKT.
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Cell Line:MV411 and K562
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Concentration:100 μM
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Incubation Time:48 h with or
without pretreatment with 20μM Chloroquine (HY-17589A) for 60
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Result:Significantly increased the number of apoptotic cells after autophagy inhibition.
Showed apoptosis of tumor cells in the combination group.
Parmacokinetics
| Species | Dose | Route | T1/2 | Vd | CL | MRT |
|---|---|---|---|---|---|---|
| Rat[4] | 5 mg/kg | i.v. | 0.87 h | 6.90 L/kg | 5.89 L/kg | 0.34 h |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (female, 4 weeks old, received a subcutaneous injection of 8×106 cells (100μl cell suspension) in the right back)[3]
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Dosage:10 mg/kg
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Administration:i.p.; every two days; two weeks
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Result:Significantly reduced tumor volume compared to the control group.
Showed no significant difference in body weight among the groups.
Showed blood biochemical indicators for liver (ALT, AST), kidney (CREA, urea, UA), and heart (CK) functions all within the normal reference range.
Showed no prominent abnormal structures in H&E staining of major organs (heart, liver, spleen, lung, and kidney) compared to the PBS group.
- Western Blot
- Mitochondrial membrane-potential fluorescent assay
- Annexin V plus membrane-impermeant dye apoptosis staining
- ROS/oxidative-stress fluorescent staining
- BrdU Incorporation Assay
- Patient-Derived Orthotopic Xenograft (PDOX)
- Protocol for Cell Cycle
- How to Choose the Right Model Animal
- Kinase activity and phosphorylation assays
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Fluorescent plasma-membrane potential dye assay
- Mitochondrial membrane-potential and mitochondrial mass staining
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Protocol for Kinase activity and phosphorylation assays
- Mitophagy Solutions
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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CAS No. 869743-37-3
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Appearance Solid
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Masse moléculaire 302.37
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Formule C18H22O4
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Color White to off-white
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SMILES
OC1=CC=C(C(O)=C1)CCCC2=CC=C(OC)C(=C2OC)C
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Synonyms
UP302
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (330.72 mM; Need ultrasonic; 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)
In Vivo:
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: ≥ 5 mg/mL (16.54 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (16.54 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
In Vivo Dissolution Calculator
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.
Pureté et documentation
Références
[1]. Ramia de Cap M, et al. Exogenous ochronosis associated with dimethoxytolyl propylresorcinol (UP302). J Dermatol. 2021 Jul;48(7):e312-e313. [Content Brief]
[4]. Zhang SQ, et al. Quantification of a novel natural antioxidant (UP302) in rat plasma using ultra-high performance liquid chromatography-tandem mass spectrometry. Journal of chromatography. B, Analytical technologies in the biomedical and life sciences. 2011 Dec 01;879(31):3763-6. [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, 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 |
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| DMSO | 1 mM | 3.3072 mL | 16.5360 mL | 33.0721 mL | 82.6802 mL |
| 5 mM | 0.6614 mL | 3.3072 mL | 6.6144 mL | 16.5360 mL | |
| 10 mM | 0.3307 mL | 1.6536 mL | 3.3072 mL | 8.2680 mL | |
| 15 mM | 0.2205 mL | 1.1024 mL | 2.2048 mL | 5.5120 mL | |
| 20 mM | 0.1654 mL | 0.8268 mL | 1.6536 mL | 4.1340 mL | |
| 25 mM | 0.1323 mL | 0.6614 mL | 1.3229 mL | 3.3072 mL | |
| 30 mM | 0.1102 mL | 0.5512 mL | 1.1024 mL | 2.7560 mL | |
| 40 mM | 0.0827 mL | 0.4134 mL | 0.8268 mL | 2.0670 mL | |
| 50 mM | 0.0661 mL | 0.3307 mL | 0.6614 mL | 1.6536 mL | |
| 60 mM | 0.0551 mL | 0.2756 mL | 0.5512 mL | 1.3780 mL | |
| 80 mM | 0.0413 mL | 0.2067 mL | 0.4134 mL | 1.0335 mL | |
| 100 mM | 0.0331 mL | 0.1654 mL | 0.3307 mL | 0.8268 mL |
Nivitol Related Classifications
HY-108046 Related Classifications
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