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> MS-444 [150045-18-4]

MS-444 [150045-18-4]

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Cat# HY-100685-1ml

Size : 10mM/1mL

Brand : MedChemExpress

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Phone : +1 850 650 7790

MS-444 inhibits the activity of purified smooth muscle myosin light chain kinase (MLCK) with an IC50 value of 10 μM.

For research use only. We do not sell to patients.

MS-444 Chemical Structure

MS-444 Chemical Structure

CAS No. : 150045-18-4

This product is a controlled substance and not for sale in your territory.

Based on 1 publication(s) in Google Scholar

Description

MS-444 inhibits the activity of purified smooth muscle myosin light chain kinase (MLCK) with an IC50 value of 10 μM.

IC50 & Target

IC50: 10 μM (myosin)[1].
In Vitro

MS-444 is a small molecule RNA-binding protein HuR (ELAVL1) inhibitor. Colorectal cancer (CRC) cells that display HuR overexpression are treated with MS-444 (1-100 μM) for 48 hr with IC50s of 10.98±1.76 μM, 12.84±2.10 μM, 5.60±0.90 μM, 14.21±2.11 μM, and 10.98±1.24 μM for HCT116, HCA-7, RKO, HT-29, and SW480 cells, respectively. Growth inhibition is observed in all CRC lines with IC50 values ranging from 5.60 μM to 14.21 μM with observable effects seen at 10 μM MS-444. Contrasting effects are observed using non-transformed small intestinal (RIE-1 (IC50=40.70±3.53 μM)) and colonic (YAMC (IC50=28.16±3.23 μM)) epithelial cells. Both cell types display properties of normal intestinal epithelial cells and are proficient in 3′UTR AU-rich elements (ARE)-mRNA decay. Both non-transformed cell lines are ~3- to 4-fold less responsive to MS-444-mediated growth inhibition, with IC50 values of 40.70 μM and 28.16 μM (P<0.05)[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

MS-444 Related Antibodies
In Vivo

To test the effects of MS-444 on CRC cell growth in vivo, mice bearing HCT116 cell xenografts receive IP injections of MS-444 (25 mg/kg bw) or vehicle every 48 hr. Over the experiment course, mice do not display any adverse effects and maintained similar weights. Anti-tumor effects of MS-444 are observed with approximately 1.7-fold reduction in tumor size. Mice treated with MS-444 show a marked 2- to 3-fold decrease in microvessel density (MVD), indicating the anti-angiogenic potential of MS-444[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

230.22

Formula

C13H10O4
CAS No.

150045-18-4
Appearance

Solid

Color

Light yellow to brown

SMILES

O=C(C1=C(C)OC=C1C2)C3=C2C(O)=CC=C3O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (217.18 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

1-Methyl-2-pyrrolidinone : 20 mg/mL (86.87 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.3437 mL 21.7184 mL 43.4367 mL
5 mM 0.8687 mL 4.3437 mL 8.6873 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 (protect from light, stored under nitrogen). 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
=
Concentration
×
Volume
×
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 mg/mL (8.69 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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 mg/mL (8.69 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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% NMP    90% PBS

    Solubility: 2 mg/mL (8.69 mM); Suspended solution; Need ultrasonic and warming and heat to 50°C

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

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

Purity: 99.45%

COA (257 KB) HNMR (375 KB) LCMS (98 KB)

Handling Instructions (2659 KB)
References

  • [1]. Satoshi Nakanishi. et al. MS-444, a new inhibitor of myosin light chain kinase from Micromonosporasp.KY7123. The Journal Of Antibiotics. 1995,48(9):948-951.  [Content Brief]

    [2]. Fernando F. Blanco.et al, Impact of HuR inhibition by the small molecule MS-444 on colorectal cancer cell tumorigenesis. Oncotarget. 2016 Nov 8; 7(45): 74043-74058.  [Content Brief]

Cell Assay
[2]

Human colorectal cancer cell lines RKO, HCA-7, HCT116, HT-29, SW480 and the non-transformed intestinal epithelial cell lines RIE-1, YAMC are treated with varying concentrations of MS-444 (1-100 μM) for 48 hr. Cell survival is measured by MTT assay after incubation of cells for 48 hr with MS-444. Relative cell survival is calculated as percentage normalized to DMSO vehicle-treated cells and plotted to determine IC50[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Mice[2]
Athymic nude (Nu/Nu) mice are used. HCT116 (2×106 cells) and HCA-7 (2.5×106) cells resuspended in PBS are injected into the dorsal subcutaneous tissue. Mice (n=5 per group) receive intraperitoneal (IP) injections of MS-444 (25 mg/kg) dissolved in PBS/5% N-Methyl Pyrrolidine (NMP) or vehicle control every 48 hr. Tumor growth is assayed[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

  • [1]. Satoshi Nakanishi. et al. MS-444, a new inhibitor of myosin light chain kinase from Micromonosporasp.KY7123. The Journal Of Antibiotics. 1995,48(9):948-951.  [Content Brief]

    [2]. Fernando F. Blanco.et al, Impact of HuR inhibition by the small molecule MS-444 on colorectal cancer cell tumorigenesis. Oncotarget. 2016 Nov 8; 7(45): 74043-74058.  [Content Brief]

  • [1]. Satoshi Nakanishi. et al. MS-444, a new inhibitor of myosin light chain kinase from Micromonosporasp.KY7123. The Journal Of Antibiotics. 1995,48(9):948-951.

    [2]. Fernando F. Blanco.et al, Impact of HuR inhibition by the small molecule MS-444 on colorectal cancer cell tumorigenesis. Oncotarget. 2016 Nov 8; 7(45): 74043-74058.

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 (protect from light, stored under nitrogen). 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
1-Methyl-2-pyrrolidinone / DMSO 1 mM 4.3437 mL 21.7184 mL 43.4367 mL 108.5918 mL
5 mM 0.8687 mL 4.3437 mL 8.6873 mL 21.7184 mL
10 mM 0.4344 mL 2.1718 mL 4.3437 mL 10.8592 mL
15 mM 0.2896 mL 1.4479 mL 2.8958 mL 7.2395 mL
20 mM 0.2172 mL 1.0859 mL 2.1718 mL 5.4296 mL
25 mM 0.1737 mL 0.8687 mL 1.7375 mL 4.3437 mL
30 mM 0.1448 mL 0.7239 mL 1.4479 mL 3.6197 mL
40 mM 0.1086 mL 0.5430 mL 1.0859 mL 2.7148 mL
50 mM 0.0869 mL 0.4344 mL 0.8687 mL 2.1718 mL
60 mM 0.0724 mL 0.3620 mL 0.7239 mL 1.8099 mL
80 mM 0.0543 mL 0.2715 mL 0.5430 mL 1.3574 mL
DMSO 100 mM 0.0434 mL 0.2172 mL 0.4344 mL 1.0859 mL
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MS-444 Related Classifications

Help & FAQs

Keywords:

MS-444150045-18-4BE-34776MS444MS 444BE34776BE 34776MyosinInhibitorinhibitorinhibit

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