Mocetinostat (MGCD0103, MG0103)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Mocetinostat(MGCD0103或MG0103)是一种同型选择性的人组蛋白去乙酰化酶(HDAC)抑制剂。HDAC是一个酶家族,参与基因转录的表观遗传调控以及细胞增殖、死亡和运动。Mocetinostat有效抑制I类HDAC(HDAC1、HDAC2和HDAC3)和IV类HDAC(HDAC11),IC50值分别为0.15 μmol/L、0.29 μmol/L、1.66 μmol/L和0.59 μmol/L,而不抑制II类HDAC。Mocetinostat通过抑制HDAC,对广泛的人类癌细胞具有抗肿瘤活性,以剂量依赖的方式诱导组蛋白超乙酰化、细胞凋亡和细胞周期停滞。
参考文献:
Fournel M, Bonfils C, Hou Y, Yan PT, Trachy-Bourget MC, Kalita A, Liu J, Lu AH, Zhou NZ, Robert MF, Gillespie J, Wang JJ, Ste-Croix H, Rahil J, Lefebvre S, Moradei O, Delorme D, Macleod AR, Besterman JM, Li Z. MGCD0103, a novel isotype-selective histone deacetylase inhibitor, has broad spectrum antitumor activity in vitro and in vivo. Mol Cancer Ther. 2008; 7(4): 759-768
- 1.Topper MJ, Vaz M, et al. "Epigenetic Therapy Ties MYC Depletion to Reversing Immune Evasion and Treating Lung Cancer." Cell. 2017 Nov 30;171(6):1284-1300.e21. PMID:29195073
- 2.Bagnall NH, Hines BM, et al. "Insecticidal activities of histone deacetylase inhibitors against a dipteran parasite of sheep, Lucilia cuprina." Int J Parasitol Drugs Drug Resist. 2017 Apr;7(1):51-60. PMID:28110187
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 396.44 |
Cas No. | 726169-73-9 |
Formula | C23H20N6O |
Synonyms | MGCD-0103 |
Solubility | insoluble in EtOH; insoluble in H2O; ≥19.8 mg/mL in DMSO |
Chemical Name | N-(2-aminophenyl)-4-[[(4-pyridin-3-ylpyrimidin-2-yl)amino]methyl]benzamide |
SDF | Download SDF |
Canonical SMILES | C1=CC=C(C(=C1)N)NC(=O)C2=CC=C(C=C2)CNC3=NC=CC(=N3)C4=CN=CC=C4 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。 |
细胞实验 [1]: | |
细胞系 |
A549细胞 |
溶解方法 |
该化合物在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月 |
反应条件 |
50 μM,16 hours |
实验结果 |
MGCD0103以剂量依赖性方式抑制全细胞中HDAC的活性。在A549细胞中,MGCD0103在高浓度时最大抑制总活性的80%。随后用无药物培养基洗涤细胞。去除药物后MGCD0103抑制活性至少维持48小时,然后缓慢逆转。 |
动物实验[1]: | |
动物模型 |
注射A549细胞的雌性CD-1裸鼠 |
剂量 |
口服,120 mg/kg |
实验结果 |
在植入晚期A549肿瘤的裸鼠中,每日给药MGCD0103(2HBr盐)13天后, MGCD0103以剂量依赖性方式显著降低肿瘤生长。与对照组相比,MGCD0103(2HBr salt,170mg/kg;对应于游离碱,120 mg/kg)显著阻断肿瘤生长,不影响体重变化。此外,MGCD0103不影响WBC计数并且耐受性良好。 |
注意事项 |
请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。 |
References: [1] Fournel M, Bonfils C, Hou Y, et al. MGCD0103, a novel isotype-selective histone deacetylase inhibitor, has broad spectrum antitumor activity in vitro and in vivo. Molecular Cancer Therapeutics, 2008, 7(4): 759-768. |
描述 | Mocetinostat (MGCD0103)是一种有效的HDAC抑制剂,对HDAC1的作用最强,IC50值为0.15 μM,比对HDAC2、3和11的选择性高2-10倍,对HDAC4、 5、6、7和8没有作用。 | |||||
靶点 | HDAC1 | HDAC2 | HDAC3 | |||
IC50 | 0.15 μM | 0.29 μM | 1.66 μM |
质量控制和MSDS
- 批次: