MSN-125
目录号 : GC61096
MSN-125是一种Bax和Bak寡聚化的抑制剂，其IC50为4μM。
Cas No.:1592908-16-1
Sample solution is provided at 25 µL, 10mM.
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MSN-125 is an inhibitor of Bax and Bak oligomerization, with an IC50 of 4μM[1]. Bax and Bak are key proteins in the apoptosis process[2]. Bax and Bak oligomerization increases the permeability of the mitochondrial outer membrane (MOMP), leads to the release of pro-apoptotic factors such as cytochrome c, thereby initiating the apoptosis program[3]. MSN-125 inhibits the oligomerization of Bax and Bak, prevents the increase of MOMP, and inhibits cell apoptosis[4]. MSN-125 is usually used to study the molecular mechanisms of apoptosis, especially in the fields of cancer and neuroprotection[5][6].
In vitro, MSN-125(5-10μM; 27h) inhibited cell death in HCT-116 or BMK cells treated with actinomycin D (ActD) or staurosporine (STS) and protected primary cortical neurons from glutamate excitotoxicity[1].
References:
[1] Niu X, Brahmbhatt H, Mergenthaler P, et al. A Small-Molecule Inhibitor of Bax and Bak Oligomerization Prevents Genotoxic Cell Death and Promotes Neuroprotection. Cell Chem Biol. 2017;24(4):493-506.e5.
[2] Pena-Blanco A, Garcia-Saez AJ. Bax, Bak and beyond - mitochondrial performance in apoptosis. FEBS J. 2018;285(3):416-431.
[3] Yamazaki T, Galluzzi L. BAX and BAK dynamics control mitochondrial DNA release during apoptosis. Cell Death Differ. 2022;29(6):1296-1298.
[4] Jensen K, WuWong DJ, Wong S, Matsuyama M, Matsuyama S. Pharmacological inhibition of Bax-induced cell death: Bax-inhibiting peptides and small compounds inhibiting Bax. Exp Biol Med (Maywood). 2019;244(8):621-629.
[5] Zhang Z, Hou L, Liu D, Luan S, Huang M, Zhao L. Directly targeting BAX for drug discovery: Therapeutic opportunities and challenges. Acta Pharm Sin B. 2024;14(6):2378-2401.
[6] Spitz AZ, Gavathiotis E. Physiological and pharmacological modulation of BAX. Trends Pharmacol Sci. 2022;43(3):206-220.
MSN-125是一种Bax和Bak寡聚化的抑制剂，其IC50为4μM[1]。Bax和Bak是细胞凋亡过程中的关键蛋白[2]。Bax和Bak的寡聚化可增加线粒体外膜的通透性（MOMP），导致细胞色素C等促凋亡因子的释放，从而启动细胞凋亡程序[3]。MSN-125通过抑制Bax和Bak的寡聚化，阻止线粒体外膜通透性（MOMP）的增加，从而抑制细胞凋亡[4]。MSN-125通常用于研究细胞凋亡的分子机制，特别是在癌症和神经保护领域[5][6]。
在体外实验中，MSN-125（5-10μM；24小时）能够抑制经放线菌素D（ActD）或司他霉素（STS）处理的HCT-116或BMK细胞的细胞死亡，并保护原代皮层神经元免受谷氨酸兴奋毒性损伤[1]。
| Cell experiment [1]: | |
Cell lines | HCT-116 and BMK cells |
Preparation Method | HCT-116 and BMK cells were seeded at a cell density of 3000 cells/well in a 96 well plate. Cells were plated in in DMEM containing 10% FBS and after adhering, cells were treated with MSN-125 (5-10μM) for 4 hours followed by addition of actinomycin D (ActD) or staurosporine (STS) for another 24 hours. Then cell death was analyzed by measuring lactate dehydrogenase release. |
Reaction Conditions | 5-10μM; 27h |
Applications | MSN-125 inhibited cell death in HCT-116 or BMK cells treated with actinomycin D (ActD) or staurosporine (STS). |
References: | |
| Cas No. | 1592908-16-1 | SDF | |
| Canonical SMILES | O=C(C1=CC=CC=C1)N[C@@H](CC2=CC=CC=C2)C(N(CC3=CC=C(C=C3)Br)[C@@H]4[C@H](OC5=CC(OCOCCOC)=CC=C45)CN)=O | ||
| 分子式 | C36H38BrN3O6 | 分子量 | 688.61 |
| 溶解度 | 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 | 1.4522 mL | 7.261 mL | 14.522 mL |
| 5 mM | 290.4 μL | 1.4522 mL | 2.9044 mL |
| 10 mM | 145.2 μL | 726.1 μL | 1.4522 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
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet