| Size | Price | Stock | Qty |
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| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
MJN228 targets nucleobindin-1 (NUCB1), a lipid-binding protein involved in lipid metabolism and cellular signaling. By binding to NUCB1, MJN228 inhibits its function, providing a tool to study the role of this protein in lipid metabolic pathways. The compound's selectivity for NUCB1 makes it a valuable probe for investigating the biology of this protein.
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|---|---|
| ln Vitro |
In Neuro2a cells, MJN228 (25 μM) dramatically lowers the enrichment of NUCB1 lipid probe [1]. MJN228 causes numerous lipid pathways in cells to malfunction [1].
In vitro, MJN228 inhibits NUCB1 with an IC50 of 3.3 μM. It blocks the AEA-DA probe labeling of endogenous NUCB1 in Neuro2a cells at concentrations as low as 10 μM. These activities confirm its mechanism as a NUCB1 inhibitor. |
| ln Vivo |
In vivo studies for MJN228 are limited. As a research tool, it is primarily used in cell-based assays to study NUCB1 function.
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| Enzyme Assay |
The in vitro binding assay for MJN228 involves measuring its ability to displace a labeled probe, such as AEA-DA, from NUCB1. The IC50 is determined from competition binding curves.
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| Cell Assay |
Western blot analysis[1]
Cell Types: A549 Tested Concentrations: 10 μM Incubation Duration: 6 hrs (hours) Experimental Results: Multiple NAEs, including AEA and OEA, were elevated in the shNUCB1-A549 cell line, but not in the control shRNA (shGFP-A549) There were no elevated cell lines. Cellular assays for MJN228 involve treating Neuro2a cells with the compound and measuring the inhibition of AEA-DA probe binding to endogenous NUCB1. The compound's effects on lipid metabolism are also assessed in relevant cell models. |
| Animal Protocol |
In vivo animal studies for MJN228 are not well-documented.
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| ADME/Pharmacokinetics |
MJN228 has a molecular weight of 364.40 g/mol and a molecular formula of C20H20N4O3. It is soluble in DMSO.
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| Toxicity/Toxicokinetics |
The toxicity profile of MJN228 is limited. As a research-grade compound, comprehensive toxicological evaluations have not been published.
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| References |
[1]. Niphakis MJ, et al. A Global Map of Lipid-Binding Proteins and Their Ligandability in Cells. Cell. 2015 Jun 18;161(7):1668-80.
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| Additional Infomation |
MJN228 is a research compound for studying NUCB1 and lipid metabolism. It has not entered clinical trials. Its mechanism involves inhibition of NUCB1.
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| Molecular Formula |
C20H20N4O3
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|---|---|
| Molecular Weight |
364.41
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| Exact Mass |
364.153
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| CAS # |
459168-97-9
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| PubChem CID |
22660592
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.3±0.0 g/cm3
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| Boiling Point |
629.8±0.0 °C at 760 mmHg
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| Flash Point |
334.7±0.0 °C
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| Vapour Pressure |
0.0±0.0 mmHg at 25°C
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| Index of Refraction |
1.675
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| LogP |
1.75
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
27
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| Complexity |
552
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN1CCN(C(C2=C(C3=CC=CC=C3)C3=C(C=CC([N+]([O-])=O)=C3)N2)=O)CC1
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| InChi Key |
BLSWPPPBUQFKHH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H20N4O3/c1-22-9-11-23(12-10-22)20(25)19-18(14-5-3-2-4-6-14)16-13-15(24(26)27)7-8-17(16)21-19/h2-8,13,21H,9-12H2,1H3
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| Chemical Name |
(4-methylpiperazin-1-yl)-(5-nitro-3-phenyl-1H-indol-2-yl)methanone
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| Synonyms |
MJN-228; MJN 228; MJN228
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7442 mL | 13.7208 mL | 27.4416 mL | |
| 5 mM | 0.5488 mL | 2.7442 mL | 5.4883 mL | |
| 10 mM | 0.2744 mL | 1.3721 mL | 2.7442 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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