2. Epigenetics Apoptosis Immunology/Inflammation
  3. HuR Apoptosis COX
  4. MS-444

MS-444 (BE-34776) is a HuR (ELAVL1) inhibitor that blocks the cytoplasmic translocation of HuR and inhibits its dimerization. MS-444 reduces cytoplasmic HuR levels by preventing the binding of HuR to ARE-mRNA, without altering the total expression of HuR. MS-444 induces apoptosis, inhibits cell growth, angiogenesis and invasion, and also regulates immune function and microbiota. MS-444 effectively alters the number, size and invasiveness of tumors in various cancer models. MS-444 is tolerable to intraperitoneal injection in vivo and can be applied to research related to colorectal cancer, familial adenomatous polyposis, colitis-associated cancer and glioblastoma.

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MS-444

MS-444 Chemical Structure

CAS No. : 150045-18-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 2 publication(s) in Google Scholar

MS-444 Related Antibodies

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COX COX-1 COX-2 COX-3

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Description

MS-444 (BE-34776) is a HuR (ELAVL1) inhibitor that blocks the cytoplasmic translocation of HuR and inhibits its dimerization. MS-444 reduces cytoplasmic HuR levels by preventing the binding of HuR to ARE-mRNA, without altering the total expression of HuR. MS-444 induces apoptosis, inhibits cell growth, angiogenesis and invasion, and also regulates immune function and microbiota. MS-444 effectively alters the number, size and invasiveness of tumors in various cancer models. MS-444 is tolerable to intraperitoneal injection in vivo and can be applied to research related to colorectal cancer, familial adenomatous polyposis, colitis-associated cancer and glioblastoma[1][2][3].

IC50 & Target

COX-2

 

Cellular Effect
Cell Line Type Value Description References
Monocyte IC50
2.1 μM
Compound: 2, MS-444
Inhibition of COX-2 gene expression in LPS/INF-gamma-stimulated human primary monocytes by RT-PCR analysis
Inhibition of COX-2 gene expression in LPS/INF-gamma-stimulated human primary monocytes by RT-PCR analysis
[PMID: 17632515]
Monocyte IC50
2.4 μM
Compound: 2, MS-444
Inhibition of IL-6 gene expression in LPS/INF-gamma-stimulated human primary monocytes by RT-PCR analysis
Inhibition of IL-6 gene expression in LPS/INF-gamma-stimulated human primary monocytes by RT-PCR analysis
[PMID: 17632515]
Monocyte IC50
3.7 μM
Compound: 2, MS-444
Inhibition of IL1-beta gene expression in LPS/INF-gamma-stimulated human primary monocytes by RT-PCR analysis
Inhibition of IL1-beta gene expression in LPS/INF-gamma-stimulated human primary monocytes by RT-PCR analysis
[PMID: 17632515]
In Vitro

MS-444 (1-40.70 μM; 48 h) inhibits growth of HCT116, HCA-7, RKO, HT-29, and SW480 CRC cells with IC50 values ranging from 5.60 μM to 14.21 μM after 48 h, while non-transformed RIE-1 and YAMC intestinal cells are ~3- to 4-fold less sensitive with IC50 values of 40.70 μM and 28.16 μM, respectively[1].
MS-444 (10 μM; 48 h) induces apoptotic nuclear morphology in RKO, HCA-7, and HCT116 CRC cells after 48 h, but has no effect on non-transformed RIE-1 intestinal cells[1].
MS-444 (10 μM; 8 h) promotes nuclear localization of HuR in Ras-transformed RIE-iRas and YAMC-Ras intestinal cells after 8 h, while non-transformed RIE-1 and YAMC cells show no change in HuR localization[1].
MS-444 (1.5-25 μM; 8 h) inhibits COX-2 mRNA expression in HCA-7 CRC cells with an IC50 of 6.75 μM and reduces COX-2 protein levels in a dose-dependent manner after 8 h of treatment[1].
MS-444 (50 μM) reduces LPS-induced IL18 mRNA expression in RAW 264.7 wild-type macrophages[2].
MS-444 (5-80 μM; 24 h) dose-dependently inhibits invasion of JX12, U87, and U251 human glioblastoma cells and JX12 CD133+ BTICs in a matrigel transwell model, with maximal suppression at 20-80 μM depending on the cell type[3].

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

MS-444 Related Antibodies

Cell Viability Assay[1]

Cell Line: colorectal cancer (CRC) cell lines (HCT116, HCA-7, RKO, HT-29, SW480), non-transformed intestinal epithelial cell lines (RIE-1, YAMC)
Concentration: 1-40.70 μM
Incubation Time: 48 h
Result: Inhibited growth in all CRC cell lines with IC50 values of 5.60 μM (RKO), 12.84 μM (HCA-7), 10.98 μM (HCT116), 14.21 μM (HT-29), and 10.98 μM (SW480).
Reduced growth of non-transformed RIE-1 and YAMC cells with IC50 values of 40.70 μM and 28.16 μM, respectively (P < 0.05).
Caused observable growth inhibition at 10 μM in CRC cells.

Cell Invasion Assay[3]

Cell Line: human glioblastoma xenolines (JX12 parent, CD133+ BTICs), U87 glioma cell line, U251 glioma cell line
Concentration: 5, 10, 20 µM (JX12 parent and CD133+ BTICs); 10, 20, 40, 80 µM (U87 and U251 cells)
Incubation Time: 24 h
Result: Significantly inhibited invasion in all tested glioblastoma cells at sub-lethal doses.
Reduced invading JX12 parent cells by 95% at 20 µM.
Reduced invading CD133+ BTICs by 80% at 10 µM.
Reduced invading U87 cells by 80-90% at 80 µM.
Showed dose-dependent attenuation of invasion in U251 cells, with maximal reduction at 40 µM.
Inhibited invasion at shorter 6 and 12 h treatment intervals, confirming effects were not due to cell death.
In Vivo

MS-444 (25 mg/kg; i.p.; every 48 hr) achieves an approximately 1.7-fold reduction in HCT116 colorectal cancer xenograft tumor volume in athymic nude mice, alongside enhanced tumor apoptosis and reduced angiogenesis[1].
MS-444 (25 mg/kg; i.p.; every 48 hr) significantly inhibits HCA-7 colorectal cancer xenograft tumor growth in athymic nude mice and reduces tumor COX-2 protein expression[1].
MS-444 (25 mg/kg; i.p.; every 72 hr for 15 days then daily for 7 days) significantly reduces established HCA-7 colorectal cancer xenograft tumor volume and COX-2 expression in athymic nude mice[1].
MS-444 (10 mg/kg; i.p.; biweekly; duration of AOM/DSS treatment cycles) increases colorectal tumor burden, size, and invasiveness in AOM/DSS-induced colorectal cancer mice, while reducing tumor cell apoptosis, serum IL18 levels, and tumor-infiltrating eosinophils[2].
MS-444 (10 mg/kg; i.p.; biweekly; 9 weeks) reduces total and small intestinal tumor numbers in APCMin mice, while altering the fecal microbiota composition and restoring spleen architecture[2].
MS-444 (10-25 mg/kg; i.p.; biweekly) promotes epithelial regeneration in acute DSS-induced colitis in mice at 10 mg/kg, while higher doses exacerbate epithelial damage[2].

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

Animal Model: Athymic nude (Nu/Nu)[1]
Dosage: 25 mg/kg
Administration: i.p.; every 72 hr for 15 days, then daily for 7 days
Result: Showed no significant tumor volume change until daily dosing began on day 14.
Reduced tumor volume significantly compared to controls by day 21.
Reduced COX-2 protein expression observed via ex vivo fluorescence imaging.
Reduced COX-2 mRNA expression significantly confirmed by qPCR.
Animal Model: C57BL/6J (3% DSS-induced)[2]
Dosage: 10 mg/kg; 25 mg/kg
Administration: i.p.; biweekly
Result: Resulted in only 9% loss of the epithelial lining (compared to higher loss in controls and 24% loss with 25 mg/kg MS-444) at 10 mg/kg dose.
Promoted epithelial regeneration at 10 mg/kg dose.
Shifted HuR from the nucleus to the cytoplasm in intestinal tissue in a dose-dependent manner.
Exacerbated epithelial damage at 25 mg/kg dose.
Molecular Weight

230.22

Formula

C13H10O4
CAS No.
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)

N-Methylpyrrolidone (NMP) : 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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:  Corn Oil

    Solubility: 5 mg/mL (21.72 mM); Suspended solution; Need ultrasonic

  • Protocol 2

    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:
%
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% 
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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: 99.42%

SDS (393 KB)

COA (257 KB) HNMR (178 KB) LCMS (96 KB)

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 (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
N-Methylpyrrolidone (NMP) / 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

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  • 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:

MS-444150045-18-4BE-34776MS444MS 444BE34776BE 34776HuRApoptosisCOXHuman Antigen RCyclooxygenasecolitis-associated cancercolorectal cancerHCT116HT-29familial adenomatosis polyposisglioblastomaRKOELAVL1SW480Inhibitorinhibitorinhibit

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