MSAB |
Katalog-Nr.GC61093
One-Click Copy Product Info
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MSAB ist ein potenter und selektiver Inhibitor der Wnt/β-Catenin-Signalgebung. MSAB bindet an β-Catenin, fÖrdert dessen Abbau und reguliert gezielt Wnt/β-Catenin-Zielgene herunter. MSAB zeigt starke Antitumorwirkungen selektiv auf Wnt-abhÄngige Krebszellen.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 173436-66-3
Sample solution is provided at 25 µL, 10mM.
MSAB (methyl 3-{[(4-methylphenyl)sulfonyl]amino}benzoate) is a selective Wnt/β-catenin signaling inhibitor binding to β-catenin and promoting its degradation with an EC50 of 0.583μM[1]. MSAB shows positive effects on cancer and osteoarthritis development[2,3].
In vitro, MSAB (0.25, 0.5, and 1µM; 72h) in head and neck squamous cell carcinoma in Cal 27 (HPV-negative) and SCC154 (HPV-positive) cell lines shows therapeutic positive effects[4]. MSAB (5μM; 72h) inhibites KynA-induced osteogenic differentiation in primary bone marrow mesenchymal stem cells from mice[5].
In vivo, MSAB (twice a week; 1mg/mL; intra-articular injection) limits osteoarthritis development and progression through inhibition of β-catenin-DDR2 signaling pathway[6]. MSAB (20mg/kg; abdominal cavity injection) attenuates the anti-inflammatory and antiapoptotic effects of SB216763 in VILI[7].MSAB (10mg/kg; i.p.; every 2 days) promoted colorectal cancer metastasis in APCmin/+ and nude mice models[8].
References:
[1] Hwang, So-Young et al. “Direct Targeting of β-Catenin by a Small Molecule Stimulates Proteasomal Degradation and Suppresses Oncogenic Wnt/β-Catenin Signaling.” *Cell reports*vol. 16,1 (2016): 28-36. doi:10.1016/j.celrep.2016.05.071
[2] Chen, Zongyu et al. “The Wnt/β-catenin pathway regulates inflammation and apoptosis in ventilator-induced lung injury.” *Bioscience reports* vol. 43,3 (2023): BSR20222429. doi:10.1042/BSR20222429
[3] Cui, Can et al. “Is β-Catenin a Druggable Target for Cancer Therapy?.” *Trends in biochemical sciences*vol. 43,8 (2018): 623-634. doi:10.1016/j.tibs.2018.06.003
[4] Maier, Tobias et al. “Inhibition of beta-catenin shows therapeutic potential in head and neck squamous cell carcinoma in vitro.” *European archives of oto-rhino-laryngology : official journal of the European Federation of Oto-Rhino-Laryngological Societies (EUFOS) : affiliated with the German Society for Oto-Rhino-Laryngology - Head and Neck Surgery*vol. 280,1 (2023): 399-408. doi:10.1007/s00405-022-07598-y
[5] Ma, Jiangwei et al. “Kynurenic acid promotes osteogenesis via the Wnt/β-catenin signaling.” *In vitro cellular & developmental biology. Animal* vol. 59,5 (2023): 356-365. doi:10.1007/s11626-023-00774-2
[6] Lu, Ke et al. “MSAB limits osteoarthritis development and progression through inhibition of β-catenin-DDR2 signaling.” *Bioactive materials* vol. 46 259-272. 24 Dec. 2024, doi:10.1016/j.bioactmat.2024.10.023
[7] Zhang, Yi-De et al. “SB-216763, a GSK-3β inhibitor, protects against aldosterone-induced cardiac, and renal injury by activating autophagy.” Journal of cellular biochemistry vol. 119,7 (2018): 5934-5943. doi:10.1002/jcb.26788
[8] Li, Xue et al. “Colorectal cancer cells secreting DKK4 transform fibroblasts to promote tumour metastasis.” *Oncogene*vol. 43,20 (2024): 1506-1521. doi:10.1038/s41388-024-03008-1
| Cell experiment [1]: | |
Cell lines | Cal 27 and SCC154 |
Preparation Method | A colony formation assay was used to determine the anticlonogenic potential of the MSAB. As SCC154 cells require cell-to-cell contact to proliferate, the observed results in the clonogenic assay were not reliable nor replicable. The Cal 27 cells were seeded in 12-well plates with a density of 250cells/well in 1ml. Twenty-four h after seeding, cells were treated with MSAB at final concentrations of 0.25, 0.5, and 1µM, or DMSO (all diluted in 1ml culture medium). The medium was aspirated 72h after treatment, and 1ml fresh culture medium was added. 9 days after seeding, colonies of sufficient size formed. To eliminate floating or dead cells, as well as cell debris, wells were washed with 1ml 1 × DPBS directly before the measurement. The TECAN multimode microplate reader was used to take pictures of the wells and a self-written macro for ImageJ 1.53e.3 was used to count the generated colonies. |
Reaction Conditions | 0.25, 0.5, and 1µM; 72h |
Applications | MSAB showed promising antineoplastic effects in-vitro and the underlining mechanism could potentially revolve around the inhibition of the epithelial-to-mesenchymal transition (EMT). |
| Animal experiment [2]: | |
Animal models | male C57BL/6 mice |
Preparation Method | Ten-week-old male C57BL/6 mice, weights ranging from 25g to 30g were used in this study. These mice are housed in specific pathogen-free (SPF) animal care facilities at a temperature (22–25°C), 12-h/12-h day-night cycle, and animals are free to draw water and food in cages. Before the experiment, the mice were left undisturbed for one week to acclimate to the new environment. For the toxicity test of MSAB/HSA, mice were randomly divided into two groups (n=7 in each group) including Vehicle injection group and MSAB/HSA injection group. PBS was used in Vehicle injection group. After 4 weeks injection (twice a week, 1mg/mL, 20μL per intra-articular injection), mice behaviors were assessed by the Laboratory Animal Behavior Observation Registration and Analysis System and tissues including liver, kidney, heart, spleen, knee joint were harvested for histological analysis. For OA treatment study, mice were randomly allocated into three groups (n=10 in each group), including the Ctrl group (Sham operation, vehicle injection), destabilization of the medial meniscus (DMM) surgery with intra-articular injection of vehicle, DMM surgery with intra-articular injection of MSAB/HSA twice a week. Under general anesthesia in mice, DMM surgery was performed by sectioning the medial meniscotibial ligament anchoring medial meniscus to tibial plateau. The control group underwent Sham surgery in which a similar incision was made into the joint capsule and then closed. |
Dosage form | twice a week; 1mg/mL; intra-articular injection |
Applications | MSAB ameliorated OA progression and OA-associated pain through inhibition of β-catenin-DDR2 signaling. |
References: | |
| Cas No. | 173436-66-3 | SDF | |
| Canonical SMILES | O=C(C1=CC=CC(NS(=O)(C2=CC=C(C=C2)C)=O)=C1)OC | ||
| Formula | C15H15NO4S | M.Wt | 305.35 |
| Löslichkeit | DMSO: 250 mg/mL (818.73 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.2749 mL | 16.3747 mL | 32.7493 mL |
| 5 mM | 655 μL | 3.2749 mL | 6.5499 mL |
| 10 mM | 327.5 μL | 1.6375 mL | 3.2749 mL |
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Quality Control & SDS
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- Purity: >99.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 28 reference(s) in Google Scholar.)