ML192
Based on 1 Customer Validation
ML192 is a selective ligand antagonist of GPR55. ML192 inhibits the β-arrestin trafficking, ERK1/2 phosphorylation and PKCβII translocation.
For research use only. We do not sell to patients.
- Purity : 99.70%
- CAS No.: 460331-61-7
- Formula: C20H22N4O2S
- Molecular Weight:382.48
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Storage:Powder -20°C, 3 years , 4°C, 2 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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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HY-111083
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6-OAUGPR84 Agonist -
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AR420626FFAR3 Agonist -
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CID 16020046 (Standard)GPR55 Antagonist -
HY-107541R
O-1602 (Standard)GPR55 Agonist -
HY-10480R
Fasiglifam (Standard)Reference Standard -
HY-W008613R
Pamoic acid (Standard)GPR35 Agonist
All Arrestin Isoforms
More
Biological Activity
Description
IC50 & Target
[1]|
ERK2 |
ERK1 |
PKCβII |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| U2OS | IC50 |
0.7 μM
Compound: ML192; CID 1434953
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Antagonist activity at HA-epitope tagged GRP55E expressed with GFP-tagged beta-arr2 in human U2OS cells assessed as LPI-stimulated redistribution of beta-arr2 preincubated for 15 mins by beta-arrestin translocation assay
Antagonist activity at HA-epitope tagged GRP55E expressed with GFP-tagged beta-arr2 in human U2OS cells assessed as LPI-stimulated redistribution of beta-arr2 preincubated for 15 mins by beta-arrestin translocation assay
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[PMID: 26916440] |
In Vitro
ML192 inhibits the β-arrestin trafficking induced by 10 μM L-α lysophosphatidylinositol (LPI) or 1 μM ML186 with IC50 values of 0.70 µM and 0.29 µM, respectively[1].
ML192 significantly inhibits ERK1/2 phosphorylation in GPRSS-expressing U2OS cells with an IC50 value of 1.1 µM[1].
ML192 (0, 10, 30 and 100 µM) reduces the translocation of PKCβII in cells with the Wild-Type GPR55 receptor[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 460331-61-7
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Appearance Solid
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Molecular Weight 382.48
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Formula C20H22N4O2S
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Color White to off-white
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SMILES
O=C(N1CCN(CC1)C2=C3C(CCCC4)=C4SC3=NC(C)=N2)C5=CC=CO5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (261.45 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: ≥ 2.5 mg/mL (6.54 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.54 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Protocols
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Kinase activity and phosphorylation assays
Kinase activity assays measure the ability of kinases to transfer phosphate groups from ATP to specific substrates, while phosphorylation assays detect the presence and levels of phosphorylated proteins. Common methods include radiolabeled ATP incorporation (e. g. ,), ADP release detection via bioluminescence (e. g. ,[3]), enzyme-linked immunosorbent assays (ELISA) for phospho-specific epitopes (e. g. ,[6]), and microtiter-based formats for high-throughput screening (e. g. ,[8]). The ADP-Glo assay quantifies kinase activity by measuring ADP produced during phosphorylation using a luciferase-based system. Radiometric assays involve autoradiography or scintillation counting after incorporation of 32P-labeled ATP into substrate proteins. ELISA-based approaches rely on phospho-specific antibodies to detect activated kinases in cell lysates or purified samples.
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Western Blot
Western blotting (WB) is a commonly used experimental method in molecular biology, biochemistry, and immunogenetics for identifying and quantifying target proteins. It combines gel electrophoresis with immunoassay, enabling researchers to analyze protein expression, post-translational modifications, and molecular weight.
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Protocol for Kinase activity and phosphorylation assays
Kinase activity assays measure transfer of phosphate from ATP to a protein or peptide substrate, generating phosphorylated substrate, ADP, or incorporated radiolabeled phosphate as the readout; phosphorylation assays measure site-specific phosphorylation in cells or tissues as a proxy for kinase-pathway activation, inhibition, or substrate regulation. Phosphorylation can be detected by phospho-specific Western blot, immunoprecipitation kinase assay, phospho-immunofluorescence, phospho-flow cytometry, luminescent ADP detection, radiolabeled ATP incorporation, or reporter-based pathway assays, and these readouts can be applied to cancer cells, primary neurons, mouse tumors, organoids, inflammatory macrophages, ferroptosis studies, and mitophagy studies when the kinase target is biologically relevant.
Purity & Documentation
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Data Sheet (278 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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Handling Instructions (2659 KB)
References
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6145 mL | 13.0726 mL | 26.1452 mL | 65.3629 mL |
| 5 mM | 0.5229 mL | 2.6145 mL | 5.2290 mL | 13.0726 mL | |
| 10 mM | 0.2615 mL | 1.3073 mL | 2.6145 mL | 6.5363 mL | |
| 15 mM | 0.1743 mL | 0.8715 mL | 1.7430 mL | 4.3575 mL | |
| 20 mM | 0.1307 mL | 0.6536 mL | 1.3073 mL | 3.2681 mL | |
| 25 mM | 0.1046 mL | 0.5229 mL | 1.0458 mL | 2.6145 mL | |
| 30 mM | 0.0872 mL | 0.4358 mL | 0.8715 mL | 2.1788 mL | |
| 40 mM | 0.0654 mL | 0.3268 mL | 0.6536 mL | 1.6341 mL | |
| 50 mM | 0.0523 mL | 0.2615 mL | 0.5229 mL | 1.3073 mL | |
| 60 mM | 0.0436 mL | 0.2179 mL | 0.4358 mL | 1.0894 mL | |
| 80 mM | 0.0327 mL | 0.1634 mL | 0.3268 mL | 0.8170 mL | |
| 100 mM | 0.0261 mL | 0.1307 mL | 0.2615 mL | 0.6536 mL |
ML192 Related Classifications
HY-122246 Related Classifications
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