| CAS NO: | 90-33-5 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 100mg | 电议 |
| 500mg | 电议 |
| Physical Appearance | A solid |
| Storage | Desiccate at -20°C |
| M.Wt | 176.17 |
| Cas No. | 90-33-5 |
| Formula | C10H8O3 |
| Solubility | insoluble in H2O; ≥2.45 mg/mL in EtOH with gentle warming and ultrasonic; ≥8.8 mg/mL in DMSO |
| Chemical Name | 7-hydroxy-4-methyl-2H-chromen-2-one |
| Canonical SMILES | CC(C1=C(O2)C=C(O)C=C1)=CC2=O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
IC50：0.4 mM
4-Methylumbelliferone是一种透明质酸（HA）合成抑制剂。许多转移性肿瘤细胞系中存在 HAS2的激活和HA的过量产生。HA合成的增加常与肿瘤细胞中转移潜能以及侵袭性的增加相关联。
体外：4-Methylumbelliferone（MU），一种HA合成抑制剂，已作为基于抑制原发性肿瘤生长和肿瘤细胞远端转移的潜在抗肿瘤药物进行研究。尽管一些研究表明MU的抗癌效果由抑制HA信号通路介导，该作用机制仍需证实。前期研究表明，HA合成由神经酰胺调节，现在显示MU激活的NSMase2如何产生神经酰胺并介导MU调控的HA合成抑制（细胞迁移和侵袭，和肿瘤细胞凋亡）。使用HA富集的小鼠少突神经胶质瘤细胞系G26-24发现，MU提高NSMase2的活性并增强神经酰胺水平，这反过来又增强磷酸酶PP2A的活性。此外，活化的PP2A 降低Akt磷酸化，减少HA 合成酶2（HAS2）和钙蛋白酶的活性，并阻断HA合成以及G26-24肿瘤细胞的迁移和侵袭。此外，MU介导的神经酰胺诱导p53和caspase-3的活化，降低SIRT1的表达以及减少G26-24的活力。因此，MU的抗癌机制最初涉及NSMase2 /神经酰胺/ PP2A / AKT / HAS2 / caspase-3 / p53/ SIRT1和钙蛋白酶信号通路，表明神经酰胺在肿瘤变成恶性转移和生长方面具有重要作用[1]。
体内：目前尚未进行体内研究。
临床试验：已进行临床研究。
参考文献：
[1] Qin J, Kilkus J, Dawson G. The hyaluronic acid inhibitor 4-methylumbelliferone is an NSMase2 activator-role of Ceramide in MU anti-tumor activity. Biochim Biophys Acta. 2016 Feb;1861(2):78-90.
| Cell experiment:[1] | |
Cell lines | HMEC and RF-24 endothelial cells |
Reaction Conditions | 0 ~ 2 mM 4-MU for 3 d incubation |
Applications | 4-MU inhibited the proliferation of actively growing HMEC and RF-24 endothelial cells in a dose-response manner. The half-maximal inhibitory concentration (IC50) values in the proliferation assay were 0.65 ± 0.04 and 0.37 ± 0.03 mM for HMEC and RF-24 cells, respectively. |
| Animal experiment:[1] | |
Animal models | Embryos from a transgenic (TG(fli1:EGFP)y1) zebrafish line |
Dosage form | 0.2 mM 24 h treatment |
Applications | A 24 h treatment with 0.2 mM 4-MU inhibited the proper growth of intersegmental vessels, which indicated the antiangiogenic effect of this compound. Thus, 4-MU could be potentially used for antiangiogenic therapy. |
Note | The technical data provided above is for reference only. |
References: 1. García-Vilas JA, Quesada AR, Medina MA. 4-methylumbelliferone inhibits angiogenesis in vitro and in vivo. Journal of Agricultural and Food Chemistry, 2013, 61(17): 4063-4071. | |
| Description | 4-Methylumbelliferone(4-MU) is an inhibitor of hyaluronic acid (HA) synthesis with an IC50 value of 0.4 mM. | |||||
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