M344
(Synonyms: 4-(二甲氨基)-N-[7-(羟基氨基)-7-氧庚]苯甲酰胺,Histone Deacetylase Inhibitor III,MS344) 目录号 : GC16456
M344是一种组蛋白去乙酰化酶(HDAC)抑制剂,其IC50值为100nM。
Cas No.:251456-60-7
Sample solution is provided at 25 µL, 10mM.
M344 is a histone deacetylase (HDAC) inhibitor with an IC50 value of 100nM[1]. M344 exhibits potential for the treatment of Alzheimer's disease[2]. M344 effectively suppresses the growth and viability of various cancer cell types through multiple mechanisms[3-4].
In vitro, the addition of M344 (2.5–4μM) to HEK293 cells at 24 hours post-transfection during rAAV8 production significantly increased the genomic titer of recombinant adeno-associated virus[5]. Treatment of neuroblastoma cell lines SH-SY5Y, SK-N-BE(2), and KP-N-NS with M344 (1μM) for 12 hours markedly suppressed the mRNA and protein expression levels of c-Jun and Fra-1, while also reducing their phosphorylation activity[6].
In vivo, M344 (3–10mg/kg) was administered via intraperitoneal injection five days a week for 3-month-old Alzheimer's disease model mice for 4 months, which significantly improved their spatial memory and cognitive function[7].
References:
[1] Zhu M, Han Y, Gu T, et al. Class I HDAC inhibitors enhance antitumor efficacy and persistence of CAR-T cells by activation of the Wnt pathway. Cell Rep. 2024 Apr 23;43(4):114065.
[2] Jeong H, Shin S, Lee JS, et al. Pan-HDAC Inhibitors Promote Tau Aggregation by Increasing the Level of Acetylated Tau. Int J Mol Sci. 2019 Sep 1;20(17):4283.
[3] Yeung A, Bhargava RK, Ahn R, et al. HDAC inhibitor M344 suppresses MCF-7 breast cancer cell proliferation. Biomed Pharmacother. 2012 Apr;66(3):232-6.
[4] Knoche SM, Brumfield GL, Goetz BT, et al. The histone deacetylase inhibitor M344 as a multifaceted therapy for pancreatic cancer. PLoS One. 2022 Sep 20;17(9):e0273518.
[5] Scarrott JM, Johari YB, Pohle TH, et al. Increased recombinant adeno-associated virus production by HEK293 cells using small molecule chemical additives. Biotechnol J. 2023 Mar;18(3):e2200450.
[6] He W, Wu Y, Tang X, et al. HDAC inhibitors suppress c-Jun/Fra-1-mediated proliferation through transcriptionally downregulating MKK7 and Raf1 in neuroblastoma cells. Oncotarget. 2016 Feb 9;7(6):6727-47.
[7] Volmar CH, Salah-Uddin H, Janczura KJ, et al. M344 promotes nonamyloidogenic amyloid precursor protein processing while normalizing Alzheimer's disease genes and improving memory. Proc Natl Acad Sci U S A. 2017 Oct 24;114(43):E9135-E9144.
M344是一种组蛋白去乙酰化酶(HDAC)抑制剂,其IC50值为100nM[1]。M344具有治疗阿尔兹海默症的潜力[2]。M344可通过多种机制对多种肿瘤细胞的增殖和活性起到抑制作用[3-4]。
在体外,M344(2.5–4μM)在rAAV8生产过程中于转染后24小时添加至HEK293细胞,可显著提高重组腺相关病毒基因组滴度[5]。M344(1μM)处理神经母细胞瘤细胞系SH-SY5Y、SK-N-BE(2)及KP-N-NS 12小时,可显著抑制c-Jun与Fra-1的mRNA及蛋白表达水平,并降低其磷酸化活性[6]。
在体内,M344(3–10mg/kg;每周5天)通过每日腹腔注射3月龄阿尔茨海默病模型小鼠,持续4个月,可显著改善其空间记忆与认知功能[7]。
| Cell experiment [1]: | |
Cell lines | SH-SY5Y, SK-N-BE(2), and KP-N-NS cells (human neuroblastoma cell lines) |
Preparation Method | Cells were maintained in DMEM supplemented with 10% fetal bovine serum (FBS). Cells were treated with M344 at a concentration of 1μM for 12 hours |
Reaction Conditions | 1μM; 12h |
Applications | M344 significantly suppressed the mRNA and protein expression levels of both c-Jun and Fra-1, inhibition of cell growth. M344 treatment caused MKK7 downregulation at both the protein and mRNA levels. |
| Animal experiment [2]: | |
Animal models | Triple transgenic Alzheimer's disease (3xTg-AD) mice (APPsw/PS1M146v/TauP301L) |
Preparation Method | Mice were intraperitoneally administered M344 at doses of 3mg/kg or 10mg/kg, 5 days per week for approximately 4 months, starting at 3 months of age (presymptomatic stage). Behavioral tests were conducted following the treatment period. |
Dosage form | 3 or 10mg/kg; i.p.; 5 days per week for approximately 4 months |
Applications | Chronic M344 treatment significantly prevented cognitive decline. Treated mice showed improved performance in Y-maze spontaneous alternation, novel object recognition and Barnes maze spatial memory tests compared to vehicle controls. M344 treatment also significantly decreased hippocampal Aβ1-42 levels and tau phosphorylation at Ser396, while increasing ADAM10 gene expression in the hippocampus. |
References: | |
| Cas No. | 251456-60-7 | SDF | |
| 别名 | 4-(二甲氨基)-N-[7-(羟基氨基)-7-氧庚]苯甲酰胺,Histone Deacetylase Inhibitor III,MS344 | ||
| 化学名 | 4-(dimethylamino)-N-[7-(hydroxyamino)-7-oxoheptyl]benzamide | ||
| Canonical SMILES | CN(C)C1=CC=C(C=C1)C(=O)NCCCCCCC(=O)NO | ||
| 分子式 | C16H25N3O3 | 分子量 | 307.39 |
| 溶解度 | ≥ 14.75 mg/mL in DMSO, ≥ 12.88 mg/mL in EtOH with ultrasonic | 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 | 3.2532 mL | 16.266 mL | 32.532 mL |
| 5 mM | 650.6 μL | 3.2532 mL | 6.5064 mL |
| 10 mM | 325.3 μL | 1.6266 mL | 3.2532 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 | |||
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| % 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: >98.00%
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