| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
IC50: 10 μM (myosin)[1]. |
|---|---|
| ln Vitro |
MS-444 is a little chemical that inhibits the RNA-binding HuR (ELAVL1) protein. HuR overexpressing colorectal cancer (CRC) cells are treated with MS-444 (1-100 μM) for 48 hours, with IC50s for HCT116, HCA-7, RKO, HT-29, and SW480 cells being 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, respectively. All CRC lines exhibit growth suppression, with IC50 values ranging from 5.60 μM to 14.21 μM. Significant effects are evident at 10 μM MS-444. Non-transformed small intestinal (RIE-1; IC50=40.70±3.53 μM) and colonic (YAMC; IC50=28.16± 3.23 μM)) epithelial cells are used to observe contrasts. Both cell types are skilled in the degradation of 3′UTR AU-rich elements (ARE)-mRNA and exhibit characteristics of typical intestinal epithelial cells. With IC50 values of 40.70 μM and 28.16 μM (P<0.05), both non-transformed cell lines are approximately three to four times less susceptible to MS-444-mediated growth inhibition[2].
MS-444 demonstrates in vitro inhibition of HuR, an RNA-binding protein involved in post-transcriptional gene regulation. It also inhibits smooth muscle MLCK with an IC50 of 10 μM. However, detailed IC50 or EC50 values for HuR inhibition are not extensively reported in the available literature. The compound's activity as a HuR inhibitor is confirmed in cell-based assays measuring the expression of HuR target genes. |
| ln Vivo |
Mice containing HCT116 cell xenografts are given IP injections of MS-444 (25 mg/kg bw) or vehicle every 48 hours in order to examine the impact of the drug on CRC cell proliferation in vivo. The mice maintained their weights and showed no negative effects during the experiment. Tumor size is reduced by around 1.7 times as a result of MS-444's anti-tumor activities. Microvessel density (MVD) in mice treated with MS-444 decreases noticeably by two to three times, suggesting that the compound has anti-angiogenic properties[2].
In vivo data for MS-444 are not extensively reported in the available literature. As a HuR inhibitor, the compound has potential for in vivo applications in cancer and inflammatory diseases. However, specific in vivo efficacy data, including animal models, dosing regimens, and pharmacokinetic-pharmacodynamic relationships, are not detailed in the available sources. The compound is classified as a research-use-only chemical. |
| Enzyme Assay |
In vitro enzyme assays for MS-444 typically involve measuring its inhibition of MLCK activity. Purified smooth muscle MLCK is incubated with a peptide substrate and ATP in the presence of varying concentrations of MS-444. The incorporation of phosphate into the substrate is measured, and the IC50 for inhibition is calculated, with MS-444 showing an IC50 of 10 μM.
|
| Cell Assay |
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].
Cellular assays for MS-444 are performed in cells to assess its effects on HuR function and the expression of HuR target genes. Cells are treated with MS-444, and the levels of HuR target mRNAs and proteins are measured by quantitative PCR and Western blotting. The compound's effects on cell proliferation, apoptosis, and other HuR-dependent processes are assessed. |
| Animal Protocol |
In vivo animal studies with MS-444 are not extensively documented in the available literature. Based on its inhibition of HuR, potential in vivo models could include xenograft models for colorectal cancer or models of inflammatory diseases. However, specific protocols are not detailed in the available sources. The compound is intended for laboratory research use only.
|
| ADME/Pharmacokinetics |
MS-444 has a molecular weight that is not specified in the available literature. It is a small molecule originally isolated from Micromonospora sp. KY7123. The compound is typically dissolved in DMSO for in vitro studies. However, detailed pharmacokinetic parameters such as absorption, distribution, metabolism, excretion, half-life, and bioavailability are not available in the literature for this research compound.
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| Toxicity/Toxicokinetics |
Comprehensive toxicology data for MS-444 are not extensively reported. The compound is classified as a research-use-only chemical and is not intended for human consumption. As a HuR inhibitor, it may have effects on gene expression that could contribute to toxicity at high concentrations. Specific toxicological data, including acute toxicity, genotoxicity, and target organ effects, are not reported in the available literature.
|
| References |
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| Additional Infomation |
MS-444 is a naphthofuran compound. 5,8-Dihydroxy-3-methyl-4-(9H)-naphtho(2,3-c)furanone has been reported in the genus Micromonospora, and relevant data are available for reference.
MS-444 is a research-grade compound not approved for clinical use. Its primary application is as a pharmacological tool for studying the RNA-binding protein HuR (ELAVL1). The compound is used to investigate the role of HuR in post-transcriptional gene regulation, immune homeostasis, and cancer. It is also used to study the function of smooth muscle myosin light chain kinase (MLCK). |
| Molecular Formula |
C13H10O4
|
|---|---|
| Molecular Weight |
230.21
|
| Exact Mass |
230.058
|
| CAS # |
150045-18-4
|
| Related CAS # |
150045-18-4
|
| PubChem CID |
132904
|
| Appearance |
Light yellow to brown solid powder
|
| Density |
1.452g/cm3
|
| Boiling Point |
448.7ºC at 760mmHg
|
| Flash Point |
225.2ºC
|
| Vapour Pressure |
1.15E-08mmHg at 25°C
|
| Index of Refraction |
1.673
|
| LogP |
2.134
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
0
|
| Heavy Atom Count |
17
|
| Complexity |
329
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(C1=C(C)OC=C1C2)C3=C2C(O)=CC=C3O
|
| InChi Key |
TZUYDLKHNQUNKS-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C13H10O4/c1-6-11-7(5-17-6)4-8-9(14)2-3-10(15)12(8)13(11)16/h2-3,5,14-15H,4H2,1H3
|
| Chemical Name |
5,8-Dihydroxy-3-methyl-naphtho[2,3-c]furan-4(9H)-one
|
| Synonyms |
MS-444 BE-34776 BE34776 MS 444 MS444
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~217.18 mM)
1-Methyl-2-pyrrolidinone : 20 mg/mL (~86.87 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2 mg/mL (8.69 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2 mg/mL (8.69 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 2 mg/mL (8.69 mM) in 10% 1-Methyl-2-pyrrolidinone 90% PBS (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication (<50°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.3439 mL | 21.7193 mL | 43.4386 mL | |
| 5 mM | 0.8688 mL | 4.3439 mL | 8.6877 mL | |
| 10 mM | 0.4344 mL | 2.1719 mL | 4.3439 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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