Mocetinostat (MGCD0103)是一种有效的HDAC抑制剂，对HDAC1抑制作用最强，IC50为0.15 μM，比作用于HDAC2， 3，和11选择性高2到10倍，对HDAC4， 5， 6， 7，和8没有抑制活性。Phase 2。A potent inhibitor of HDAC1, HDAC2, HDAC3, and HDAC11.

Information

Mocetinostat (MGCD0103, MG0103) is a potent HDAC inhibitor with most potency forHDAC1withIC50of 0.15 μM in a cell-free assay, 2- to 10- fold selectivity against HDAC2, 3, and 11, and no activity to HDAC4, 5, 6, 7, and 8. Mocetinostat (MGCD0103) inducesapo
In vitro

MGCD0103 inhibits only a subset of the nine human recombinant HDACs, including HDAC1, HDAC2, HDAC3, and HDAC11 at nanomolar or low micromolar concentrations, in a dose-dependent manner. MGCD0103 reveals most potent inhibitory activity against human HDAC1 and HDAC2 enzymes in vitro, and it does not inhibit class II HDACs. The exocyclic amino group in MGCD0103 is necessary for enzyme inhibitory activity because HDAC-inhibitory activity against HDAC1 and HDAC2 is completely abolished with the desamino analogue. The inhibitory activity of MGCD0103 reaches the maximum plateau at 6 μM, and the maximal inhibitable enzyme pool affected by MGCD0103 is 75% of the total enzyme activity in HCT116 cells whereas NVP-LAQ824 inhibits almost 100% of that in these cells. In A549 cells, MGCD0103 also exhibits dose-dependent inhibition of HDAC activity in whole cells.

In vivo

MGCD0103 significantly inhibites growth of human tumor xenografts in nude mice and the antitumor activity correlated with induction of histone acetylation in tumors. P.O. administration of MGCD0103 (2HBr salt) significantly decreases growth of implanted advanced A549 tumors in nude mice in a dose-dependent manner after 13 days of daily administration. MGCD0103 (170 mg/kg for 2HBr salt, corresponding to 120 mg/kg of free base) significantly blockes growth of tumors compared with vehicle treatment alone with no change in body weight. In addition, MGCD0103 does not reduce WBC counts and is well tolerated. MGCD0103 is also orally active in many other human tumor xenograft models including NSCLC H1437. MGCD0103 at 80 mg/kg (free base) almost completely blocks the growth of H1437 tumors after 13 days of daily p.o. administration with no reduction of body weight in animals. MGCD0103 reduces pulmonary arterial pressure more dramatically than tadalafil, a standard-of-care therapy for human pulmonary hypertension that functions as a vasodilator. Moreover, MGCD0103 improves pulmonary artery acceleration time and reduced systolic notching of the pulmonary artery flow envelope, which suggests a positive impact of the HDAC inhibitor on pulmonary vascular remodeling and stiffening.
Cell Data

cell lines：MDA-MB-231, and MDA-MB-436

Concentrations：0-60 μM

Incubation Time：72 hours

Powder Purity:≥97%

规格

别名

莫西替诺特 (MGCD0103)

英文别名

MG0103 | N-(2-aminophenyl)-4-((4-(pyridin-3-yl)pyrimidin-2-ylamino)methyl)benzamide

规格或纯度

Moligand™, 10mM in DMSO

英文名称

Mocetinostat (MGCD0103)

生化机理

莫西司他（MGCD0103，MG0103）是一种强效 HDAC 抑制剂，对 HDAC1 的作用最强，在无细胞试验中的 IC50 为 0.15 μM，对 HDAC2、3 和 11 的选择性为 2 到 10 倍，对 HDAC4、5、6、7 和 8 没有活性。莫西司他（MGCD0103）可诱导细胞凋亡和自噬。第二阶段

储存条件

-80℃储存

运输条件

特低温运输

作用类型

抑制剂

作用机制

组蛋白去乙酰化酶 1 抑制剂；组蛋白去乙酰化酶 2 抑制剂；组蛋白去乙酰化酶 3 抑制剂

名称和识别符

分子类型

小分子

Isomeric SMILES

C1=CC=C(C(=C1)N)NC(=O)C2=CC=C(C=C2)CNC3=NC=CC(=N3)C4=CN=CC=C4

分子量

396.44

Reaxy-Rn

14262919

Reaxys-RN link address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=14262919&ln=

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高级数据

产品属性

ALogP	2.8

关联靶点（人）

CYP3A4 Tclin 细胞色素P450 3A4(Cytochrome P450 3A4) (1 活性数据)

点击查看靶蛋白信息： CYP3A4

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

HDAC1 Tclin 组蛋白去乙酰化酶1(Histone deacetylase 1) (17 活性数据)

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活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

HDAC11 Tclin 组蛋白去乙酰化酶11(Histone deacetylase 11) (3 活性数据)

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活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

HDAC2 Tclin 组蛋白去乙酰化酶2(Histone deacetylase 2) (11 活性数据)

点击查看靶蛋白信息： HDAC2

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

HDAC3 Tclin 组蛋白去乙酰化酶3(Histone deacetylase 3) (5 活性数据)

点击查看靶蛋白信息： HDAC3

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

化学和物理性质

溶解性

Solubility (25°C) In vitro DMSO: 68 mg/mL (198.62 mM); Water: 5 mg/mL (14.6 mM); Ethanol: 3 mg/mL (8.76 mM);

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找到1个结果

批号(Lot Number)	证书类型	货号
F2414227	分析证书	M409032

技术文档和文章

表观遗传调控剂

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极光激酶表观遗传学 DNMTs 组蛋白甲基转移酶抑制剂 HDACs

Epigenetic Modifiers

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Aurora Kinases DNMTs HDACs Epigenetics Histone Methyltransferase Inhibitors

组蛋白去乙酰化酶抑制剂

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HDAC抑制剂

Histone Deacetylase Inhibitors

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HDAC inhibitors

DNA 序列不变，基因表达为何改变？表观遗传调控的核心机制与研究方法

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If the DNA Sequence Remains Unchanged, Why Does Gene Expression Change? Core Mechanisms and Research Methods of Epigenetic Regulation

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DNA Epigenetics gene expression

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引用文献

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