CMLD-2
Based on 2 publication(s) in Google Scholar
CMLD-2, an inhibitor of HuR-ARE interaction, competitively binds HuR protein disrupting its interaction with adenine-uridine rich elements (ARE)-containing mRNAs (Ki=350 nM). CMLD-2 induces apoptosis exhibits antitumor activity in different cancer cells as colon, pancreatic, thyroid and lung cancer cell lines. Hu antigen R (HuR) is an RNA binding protein, can regulate target mRNAs stability and translation.
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- Pureté : 98.66%
- CAS No.: 958843-91-9
- Formule: C31H31NO6
- Masse moléculaire:513.58
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) CMLD-2
More
Activité biologique
Description
IC50 & Target
HuR[1]
In Vitro
CMLD-2 (1-75 μM; 24-72 h) inhibits thyroid cancer cell viability[2].
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CMLD-2 (20-30 μM; 24-48 h) activates caspases and induces apoptotic cell death in H1299 and A549 cells[3].
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CMLD-2 (30 μM; 24-48 h) induces G1 cell cycle arrest and mitochondrial perturbation in H1299 and A549 cell[3].
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CMLD-2 (30 μM; 24-48 h) reduces expression of HuR and HuR-regulated mRNAs and proteins in H1299 cells[3].
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CMLD-2 (35 μM; 72 h) decreases directional migration capability in SW1736, 8505C, BCPAP and K1 cells. CMLD-2 induces a strong decrease of MAD2 mRNA levels in SW1736, 8505C, BCPAP and K1 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:SW1736, 8505C, BCPAP and K1 cells
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Concentration:1, 5, 10, 25, 35, 50, 75 μM
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Incubation Time:24, 48, 72 hours
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Result:Reduced the viability of all the four cell lines when used at 35, 50 and 75 μM concentration and at different time points.
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Cell Line:H1299, A549, H1975, HCC827, MRC-9 and CCD16 cells
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Concentration:20, 30 μM
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Incubation Time:24, 48 hours
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Result:Marked activated the caspase-9 and -3 in lung tumor cells.
Induce the cleavage of PARP in lung tumor cells.
Significantly increased the annexin-V-positive staining in lung tumor cells.
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Cell Line:H1299, A549, MRC-9 and CCD16 cells
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Concentration:30 μM
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Incubation Time:24, 48 hours
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Result:Induced greater G1 phase cell cycle arrest in H1299 and A549 cells than in MRC-9 and CCD16 cells.
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Cell Line:H1299, A549, H1975, HCC827, CCD16 and MRC-9 cells
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Concentration:20, 30 μM
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Incubation Time:24, 48 hours
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Result:Diminished protein expression of HuR, Bcl-2, Cyclin E and Bcl-XL and increased expression of p27 and BAX in lung tumor cells.
Chemical Information
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CAS No. 958843-91-9
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Appearance Solid
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Masse moléculaire 513.58
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Formule C31H31NO6
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Color White to off-white
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SMILES
O=C1C=C(C2=CC=CC=C2)C3=C(OC)C=C(OC)C(C(C4=CC=C(OC)C=C4)CC(N5CCCC5)=O)=C3O1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Nat Commun
Subversion of mRNA degradation pathways by EWSR1::FLI1 represents a therapeutic vulnerability in Ewing sarcoma. [Abstract]2025 Jul 16;16(1):6537. PMID: 40664627 -
Acta Pharmacol Sin
2025 Mar 25. PMID: 40133626
Solvant et solubilité
In Vitro:
DMSO : 50 mg/mL (97.36 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 (4.87 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 (4.87 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.
Protocole
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Detection of Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
Pureté et documentation
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Fiche technique (284 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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Instruction de manipulation (2659 KB)
Références
[1]. Wu X, et, al. Identification and validation of novel small molecule disruptors of HuR-mRNA interaction. ACS Chem Biol. 2015 Jun 19;10(6):1476-84. [Content Brief]
[2]. Allegri , et, al. The HuR CMLD-2 inhibitor exhibits antitumor effects via MAD2 downregulation in thyroid cancer cells. Sci Rep. 2019 May 14;9(1):7374. [Content Brief]
[3]. Muralidharan R, et, al. HuR-targeted small molecule inhibitor exhibits cytotoxicity towards human lung cancer cells. Sci Rep. 2017 Aug 30;7(1):9694. [Content Brief]
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 | 1.9471 mL | 9.7356 mL | 19.4712 mL | 48.6779 mL |
| 5 mM | 0.3894 mL | 1.9471 mL | 3.8942 mL | 9.7356 mL | |
| 10 mM | 0.1947 mL | 0.9736 mL | 1.9471 mL | 4.8678 mL | |
| 15 mM | 0.1298 mL | 0.6490 mL | 1.2981 mL | 3.2452 mL | |
| 20 mM | 0.0974 mL | 0.4868 mL | 0.9736 mL | 2.4339 mL | |
| 25 mM | 0.0779 mL | 0.3894 mL | 0.7788 mL | 1.9471 mL | |
| 30 mM | 0.0649 mL | 0.3245 mL | 0.6490 mL | 1.6226 mL | |
| 40 mM | 0.0487 mL | 0.2434 mL | 0.4868 mL | 1.2169 mL | |
| 50 mM | 0.0389 mL | 0.1947 mL | 0.3894 mL | 0.9736 mL | |
| 60 mM | 0.0325 mL | 0.1623 mL | 0.3245 mL | 0.8113 mL | |
| 80 mM | 0.0243 mL | 0.1217 mL | 0.2434 mL | 0.6085 mL |
CMLD-2 Related Classifications
HY-124828 Related Classifications
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