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]。