2. GPCR/G Protein Neuronal Signaling TGF-beta/Smad Epigenetics Stem Cell/Wnt MAPK/ERK Pathway
  3. GPR55 PKC ERK Arrestin
  4. ML192

ML192 is a selective ligand antagonist of GPR55. ML192 inhibits the β-arrestin trafficking, ERK1/2 phosphorylation and PKCβII translocation.

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ML192 Chemical Structure

ML192 Chemical Structure

CAS No. : 460331-61-7

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Customer Review

Based on 1 publication(s) in Google Scholar

ML192 Related Antibodies

Top Publications Citing Use of Products

View All PKC Isoform Specific Products:

View All Isoforms
PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

View All ERK Isoform Specific Products:

View All Isoforms
ERK ERK1 ERK2 ERK5 ERK8

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

ML192 is a selective ligand antagonist of GPR55. ML192 inhibits the β-arrestin trafficking, ERK1/2 phosphorylation and PKCβII translocation[1].

IC50 & Target[1]

ERK2

 

ERK1

 

PKCβII

 

Cellular Effect
Cell Line Type Value Description References
U2OS IC50
0.7 μM
Compound: ML192; CID 1434953
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
[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.

ML192 Related Antibodies
Molecular Weight

382.48

Formula

C20H22N4O2S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1CCN(CC1)C2=C3C(CCCC4)=C4SC3=NC(C)=N2)C5=CC=CO5
Shipping

Room temperature in continental US; may vary elsewhere.
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6145 mL 13.0726 mL 26.1452 mL
5 mM 0.5229 mL 2.6145 mL 5.2290 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    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.
  • Protocol 2

    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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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
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
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ML192 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ML192460331-61-7ML 192ML-192GPR55PKCERKArrestinG protein-coupled receptor 55Protein kinase CExtracellular signal regulated kinasesβ-arrestinERK1/2PKCβIIInhibitorinhibitorinhibit

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