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Mesalamine (also named as 5ASA; Z-206; AJG-501; MAX-002; 5-aminosalicylic acid; Asacol; mesalazine; 5-ASA) orally bioavailable inhibitor of TNFα-induced IKK activity with potential anti-inflammatory activity. Additionally, it stimulates the PPARγ receptor and inhibits both NF-κB and p21-activated kinase 1 (PAK1). It has been approved for the treatment of ulcerative colitis, a type of inflammatory bowel disease.
| Targets |
PPARγ; PAK1; p65
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| ln Vitro |
5-Aminosalicylic acid (5-ASA) is a specific agonist for PPARγ, and only PPARγ but not PPARα or PPARδ induces p65 degradation. P65 protein is degraded by 5-aminosalicylic acid, demonstrating the E3 ubiquitin ligase activity of PPARγ. Additionally, PAK1 is inhibited by 5-aminosalicylic acid at the mRNA level, suggesting a second mechanism distinct from PPARγ ligand activation. Through PAK1 inhibition, 5-aminosalicylic acid prevents NF-κB from operating in intestinal epithelial cells (IECs). The growth of HT-29 colon carcinoma cells is inhibited by pretreatment with 5-Aminosalicylic acid (5-ASA) or nimesulide at various concentrations (10-1000 mol/L) for 12-96 h in a dose- and time-dependent manner. Nimesulide or 5-Aminosalicylic Acid's suppression, however, has no statistically significant effect. Pretreatment with varying doses of combined 5-Aminosalicylic acid and Nimesulide inhibits the growth of HT-29 colon carcinoma cells in a dose-dependent manner. A combination of 5-Aminosalicylic acid (final concentration 100 μM) and Nimesulide (final concentration 10-1000 μM) has a stronger inhibitory effect than a single dose of Nimesulide on the proliferation of HT-29 colon carcinoma cells. The proliferation of these cells is also inhibited by the combination of nimesulide (final concentration 100 μM) and 5-aminosalicylic acid (final concentration 10-1000 μM) in a dose-dependent manner[2].
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| ln Vivo |
5-Aminosalicylic acid (5-ASA) has an antineoplastic effect in a xenograft tumor model. SCID mice engrafted with HT-29 colon cancer cells are given daily treatments for 21 days in a row with 5-Aminosalicylic acid at a concentration of 50 mM to assess the in vivo antineoplasic effect of the compound. Comparing SCID mice receiving 5-Aminosalicylic acid to control mice or mice receiving GW9662 alone at the end of the treatment, a reduction of 80–86% in tumor weight and volume is seen. After 10 days of treatment, the 5-Aminosalicylic Acid's anti-cancer effects are already apparent. Mice given 5-Aminosalicylic acid at 5 mM produced results that were similar. By simultaneously administering GW9662 intraperitoneally, 5-Aminosalicylic acid's antitumorigenic effect is completely eliminated at day 21.
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| Enzyme Assay |
5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.
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| Cell Assay |
The MTT assay is used to measure cytostatic effects. A 0.25% trypsin solution is used to separate HT-29 colon cancer cells for 5 minutes. The cells are then seeded onto 96-well plates (1×106 cells/well), supplemented with 10% FCS, and given 24 hours to attach before test chemicals (5-Aminosalicylic acid 10, 50, 100, 500, and 1000 μM; Nimesulide; and their mixtures) are added. In a culture medium devoid of serum, test compounds are diluted. After 48 hours of incubation in a medium or with various drug concentrations, 20 μL of MTT solution (5 g/L) in PBS is added. After four hours, the medium in each well is taken out, and 120 L of muriatic isopropanol (0.04 mM) is added after being lightly concussed for ten minutes. Using an ELISA reader, dye uptake is measured at 490 nm. Each concentration or control group is divided into five wells. The cells, on the other hand, are seeded onto 96-well plates (1×106 cells/well) and allowed to adhere for 24 hours before being exposed to the test chemicals (5-Aminosalicylic acid, Nimesulide, and their combination). It has a 100 μM final concentration. The control group receives the identical medium after which dye uptake is assessed. For each test compound or control group, five wells are used[2].
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| Animal Protocol |
Mice: Pathogen-free BALB/c SCID mice that are six to seven weeks old are used. Animals' flanks are implanted subcutaneously with 107 HT-29 human colon cancer cells, which have either been pretreated with GW9662 for 24 hours or not. Mice are given daily peritumoral injections of 5-Aminosalicylic Acid (5 or 50 mM) for 10 or 21 days starting two days after cell inoculation. By injecting GW9662 (1 mg/kg/day) intraperitoneally every day during treatment with 5-Aminosalicylic acid, the impact of PPAR is assessed. In the control group, 5-Aminosalicylic acid is substituted with saline. Three times per week, tumor development in mice is monitored. Tumor volume and size are determined after killing at 10 or 21 days. Prior to paraffin embedding for histological analysis, tumors are weighted.
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| References |
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| Molecular Formula |
C7H7NO3
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| Molecular Weight |
153.14
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| Exact Mass |
153.04
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| Elemental Analysis |
C, 54.90; H, 4.61; N, 9.15; O, 31.34
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| CAS # |
89-57-6
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| Related CAS # |
5-Aminosalicylic acid-d3;1309283-32-6;5-Aminosalicylic Acid-d3 hydrochloride;1346601-18-0;5-Aminosalicylic acid-13C6;1189709-96-3
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| Appearance |
Solid powder
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| SMILES |
C1=CC(=C(C=C1N)C(=O)O)O
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| InChi Key |
KBOPZPXVLCULAV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C7H7NO3/c8-4-1-2-6(9)5(3-4)7(10)11/h1-3,9H,8H2,(H,10,11)
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| Chemical Name |
5-amino-2-hydroxybenzoic acid
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (16.32 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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: ≥ 2.5 mg/mL (16.32 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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: 7.14 mg/mL (46.62 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Solubility in Formulation 4: 16.67 mg/mL (108.85 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 6.5300 mL | 32.6499 mL | 65.2997 mL | |
| 5 mM | 1.3060 mL | 6.5300 mL | 13.0599 mL | |
| 10 mM | 0.6530 mL | 3.2650 mL | 6.5300 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT06013696 | Active Recruiting |
Other: Adding household bleach to urine sample |
Ulcerative Colitis | Meir Medical Center | April 2023 | Phase 2 |
| NCT05663775 | Not yet recruiting | Drug: Mesalamine | Diarrhea Advanced Melanoma |
AHS Cancer Control Alberta | April 2023 | Phase 2 |
| NCT05316220 | Not yet recruiting | Drug: Mesalamine Drug: Placebo |
Ulcerative Colitis (UC) | AbbVie | December 31, 2022 | Phase 3 |
| NCT04920149 | Recruiting | Drug: Mesalamine Drug: Placebo |
Lynch Syndrome Colon Cancer |
Ann-Sofie Backman | March 21, 2022 | Phase 2 |
| NCT05119140 | Recruiting | Drug: Hydroxychloroquine Drug: Mesalamine |
Ulcerative Colitis (Disorder) |
Icahn School of Medicine at Mount Sinai |
June 10, 2022 | Phase 1 Phase 2 |
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