| Size | Price | Stock | Qty |
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| 5mg |
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| Other Sizes |
| Targets |
MIND4-17 targets KEAP1 (Kelch-like ECH-associated protein 1) by covalently modifying the C151 residue. This disrupts the KEAP1-NRF2 association, leading to NRF2 protein stabilization and nuclear translocation.
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|---|---|
| ln Vitro |
In a concentration-dependent manner, MIND4-17 (0.1-2 μM; 24 hours) strongly enhances the expression of characteristic ARE genes Nqo1, Hmox1, Srx1, and to a lesser extent Gclc[1]. In both WT and HD mutant ST14A cells, MIND4-17 (0.1-2 μM; 24 hours) exhibits concentration-dependent stimulation of NQO1 and GCLM proteins [1]. In microglia, MIN4-17 (0.1–10 μM) lowers the generation of nitrogen intermediates and ROS [1]. The expression of the canonical ARE genes Nqo1, Hmox1, Srx1, and to a lesser extent Gclc was significantly and concentration-dependently enhanced using RT-PCR[1] on rat corticostriatal neurons. The concentrations were 1 μM, 5 μM, and the incubation times were 4 hours and 16 hours.
In vitro, MIND4-17 potently activates NRF2 signaling. It promotes Nrf2 protein stabilization, nuclear translocation, and enhances the cellular antioxidant response by upregulating NRF2 target genes (e.g., NQO1, HMOX1). |
| ln Vivo |
MIND4-17 (2 mg/kg; intravitreal injection; once) alleviates photodamage-induced retinal impairment in mice by activating Nrf2 signaling [2].
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| Enzyme Assay |
A non-cell assay is performed using a biotinylated or fluorescently labeled MIND4-17 analog. Purified KEAP1 protein is incubated with the compound, and covalent modification of the C151 residue is detected by mass spectrometry or by Western blot using a labeled antibody.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: Wild-type (WT) and Huntington's disease (HD) mutant ST14A cells Tested Concentrations: 0.1 μM, 0.2 μM, 0.5 μM, 0.7 μM, 1 μM, 1.5 μM, 2 μM Incubation Duration: 24 hrs (hours) Experimental Results: demonstrated a concentration-dependent induction of NQO1 and GCLM proteins. For cell studies, MIND4-17 is dissolved in DMSO and diluted in culture medium (final DMSO <0.1%). Cells (e.g., HEK293, HepG2, primary neurons) are treated for 4-24 hours. NRF2 translocation is assessed by immunofluorescence. Target gene expression is measured by qPCR or Western blot. |
| Animal Protocol |
Animal/Disease Models: balb/c (Bagg ALBino) mouse bearing white fluorescent light exposure[2]
Doses: 2 mg/kg Route of Administration: Intravitreal injection; once Experimental Results: Activated Nrf2 signaling and attenuated retinal dysfunction by light damage in mice. In animal studies, MIND4-17 (2 mg/kg; intravitreal injection; once) alleviates photodamage-induced retinal impairment in mice by activating Nrf2 signaling. It is also studied in models of neurodegenerative diseases and oxidative stress-related disorders. |
| ADME/Pharmacokinetics |
Limited PK data are available. The compound is administered via intravitreal injection for ocular studies or systemically for other applications. It shows promise as a tool for research in cancer, neurodegenerative diseases, and other disorders related to protein misfolding.
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| Toxicity/Toxicokinetics |
In preclinical studies, MIND4-17 has been well-tolerated at efficacious doses. No significant toxicity has been reported. Standard laboratory safety precautions apply.
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| References |
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| Additional Infomation |
5-Nitro-2-[[5-(phenoxymethyl)-4-phenyl-1,2,4-triazol-3-yl]sulfanyl]pyridine is an organic molecular entity.
MIND4-17 is a research tool for studying the KEAP1-NRF2 pathway. It has potential therapeutic applications in diseases characterized by oxidative stress, such as neurodegenerative diseases, retinal degeneration, and inflammatory disorders. It is not an approved drug. |
| Molecular Formula |
C20H15N5O3S
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|---|---|
| Molecular Weight |
405.43
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| Exact Mass |
405.089
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| CAS # |
345989-24-4
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| PubChem CID |
1327659
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
667.5±65.0 °C at 760 mmHg
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| Flash Point |
357.5±34.3 °C
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| Vapour Pressure |
0.0±2.0 mmHg at 25°C
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| Index of Refraction |
1.698
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| LogP |
5.49
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
29
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| Complexity |
525
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C=C1)N2C(=NN=C2SC3=NC=C(C=C3)[N+](=O)[O-])COC4=CC=CC=C4
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| InChi Key |
OZUBDKIROJPQGE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H15N5O3S/c26-25(27)16-11-12-19(21-13-16)29-20-23-22-18(14-28-17-9-5-2-6-10-17)24(20)15-7-3-1-4-8-15/h1-13H,14H2
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| Chemical Name |
5-nitro-2-[[5-(phenoxymethyl)-4-phenyl-1,2,4-triazol-3-yl]sulfanyl]pyridine
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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: ~100 mg/mL (~246.7 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.17 mM) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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: 2.5 mg/mL (6.17 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4665 mL | 12.3326 mL | 24.6652 mL | |
| 5 mM | 0.4933 mL | 2.4665 mL | 4.9330 mL | |
| 10 mM | 0.2467 mL | 1.2333 mL | 2.4665 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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