MSAB
目录号 : GC61093
MSAB（methyl 3-{[(4-methylphenyl)sulfonyl]amino}benzoate）是一种选择性Wnt/β-catenin信号抑制剂，与β-catenin结合并促进其降解，其EC50为0.583μM。
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
MSAB（methyl 3-{[(4-methylphenyl)sulfonyl]amino}benzoate）是一种选择性Wnt/β-catenin信号抑制剂，与β-catenin结合并促进其降解，其EC50为0.583μM[1]。MSAB对癌症和骨关节炎的发展有积极作用[2,3]。
在体外，MSAB(0.25、0.5、1µM；72h)对头颈部鳞状细胞癌Cal 27 （hpv阴性）和SCC154 （hpv阳性）细胞系的治疗效果呈阳性[4]。MSAB(5μM; 72h)抑制kyna诱导小鼠原代骨髓间充质干细胞成骨分化[5]。
在体内，MSAB（每周2次，1mg/mL，关节内注射）通过抑制β-catenin-DDR2信号通路限制骨关节炎的发展和进展[6]。MSAB (20mg/kg；腹腔注射)可减弱SB216763在VILI中的抗炎和抗凋亡作用[7]。MSAB(10mg/kg; i.p.; every 2 days)在APCmin/+和裸鼠模型均促进结直肠癌转移[8]。
| 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 | ||
| 分子式 | C15H15NO4S | 分子量 | 305.35 |
| 溶解度 | DMSO: 250 mg/mL (818.73 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.2749 mL | 16.3747 mL | 32.7493 mL |
| 5 mM | 0.655 mL | 3.2749 mL | 6.5499 mL |
| 10 mM | 0.3275 mL | 1.6375 mL | 3.2749 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >99.00%
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