目录号 | 产品详情 | 靶点 | |
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T60856 | |||
HDAC6-IN-9 (compound 12c) 是 HDAC6的强效选择性抑制剂,具有抗增殖活性。HDAC6-IN-9 对 HDAC6、HDAC1、HDAC3、HDAC8 和 HDAC10 的 IC50值分别为 4.2, 11.8, 15.2, 139.6, 21.3 nM。 | |||
T73031 | |||
HDAC6-IN-14 是一种高选择性 HDAC6(HDAC) 抑制剂,IC50为 42 nM。HDAC6-IN-14 的选择性是 HDAC1/HDAC2/HDAC3/HDAC4 的 100 倍以上。 | |||
T21898 | |||
MI-192 是一种选择性 HDAC2和 HDAC3抑制剂,IC50分别为 30 nM 和 16 nM。MI-192 比其他 HDAC 异构体对 HDAC2/3 具有更高选择性。MI-192 诱导髓系白血病细胞凋亡 (apoptosis)。抗癌和神经保护活性。 | |||
T21719 | |||
m-Carboxycinnamic acid bishydroxamide 是一种有效的HDAC 抑制剂,在体外对 HDAC1 和 HDAC3 的ID50值分别为 10 nM 和 70 nM。m-Carboxycinnamic acid bishydroxamide 也可诱导细胞凋亡并且抑制肿瘤生长。 | |||
T3205 | HDAC | ||
UF010 是一种有效的选择性 HADC 抑制剂,对 HDAC 1、2、3 和 8 的 IC50 分别为 0.5 μM、0.1 μM、0.06 μM 和 1.5 μM。它比作用于其他HDACs 选择性高6倍多。 | |||
T63422 | |||
HDAC-IN -45 是小分子 HDAC 抑制剂,能够与 Y303 残基形成氢键,表现出抗癌作用。HDAC-IN-45 能够明显抑制 HDAC1、HDAC2 和 HDAC3 亚型,他们的 IC50值分别为 0.108、0.585 和 0.563 μM。 | |||
T2025 | HDAC | ||
HDAC-IN-7 (HBI-8000) 是 Chidamide 的一种杂质。Chidamide 是一种可口服的 HDAC 酶 I 类 HDAC1/2/3 和 IIb 类 HDAC10 抑制剂。 | |||
T62006 | |||
HDAC-IN-30 是多种HDAC 蛋白的抑制剂,包括HDAC1(IC50=13.4 nM),HDAC2(IC50=28.0 nM),HDAC3(IC50=9.18 nM),HDAC6(IC50=42.7 nM),HDAC8(IC50=131 nM)。HDAC-IN-30 显示除强大的抗肿瘤作用。 | |||
T62644 | |||
HDAC-IN-41 (Compound 7c) 是一种口服具有活力的、选择性的的 I 类 HDAC 抑制剂,能够作用于 HDAC1 (IC50: 0.62 μM)、HDAC2 (IC50: 1.46 μM)和 HDAC3 (IC50: 0.62 μM)。HDAC-IN-41 显示出 NO 释放的活性。 | |||
T63509 | |||
Top/HDAC-IN-1 是拓扑异构酶 (Top)/HDAC 双重抑制剂,能够作用于 HDAC1 (IC50: 18 nM)、HDAC2 (IC50: 230 nM)、HDAC3 (IC50: 790 nM)、HDAC6 (IC50: 87 nM) 和 HDAC8 (IC50: 5250 nM)。Top/HDAC-IN-1 对 HCT116 细胞表现出有效的抗肿瘤作用 (IC50: 180 nM),可将 HCT116 细胞的细胞周期阻滞 G2 期,有效诱导其凋亡 (apoptosis)。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPH-01473 | HDAC3 Protein, Human, Recombinant (His & SUMO) | Human | E. coli | ||
HDAC3 Protein, Human, Recombinant (His & SUMO) is expressed in E. coli expression system with N-6xHis-SUMO tag. The predicted molecular weight is 64.8 kDa and the accession number is O15379.
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TMPY-03431 | HDAC4 Protein, Human, Recombinant (aa 612-1084) | Human | Baculovirus Insect Cells | ||
HDAC4 (histone deacetylase 4), belongs to class II of the histone deacetylase/AcuC/APhA family. Histone Deacetylases (HDACs) are a group of enzymes closely related to sirtuins. They catalyze the removal of acetyl groups from lysine residues in histones and non-histone proteins, resulting in transcriptional repression. In general, they do not act autonomously but as components of large multiprotein complexes, such as pRb-E2F and mSin3A, that mediate important transcription regulatory pathways. There are three classes of HDACs; classes 1, 2, and 4, which are closely related to Zn2+-dependent enzymes. HDACs are ubiquitously expressed and they can exist in the nucleus or cytosol. Their subcellular localization is affected by protein-protein interactions and by the class to which they belong. HDACs have a role in cell growth arrest, differentiation, and death and this has led to substantial interest in HDAC inhibitors as possible antineoplastic agents. HDAC4 possesses histone deacetylase activity and represses transcription when tethered to a promoter. It does not bind DNA directly but through transcription factors MEF2C and MEF2D. HDAC4 seems to interact in a multiprotein complex with RbAp48 and HDAC3.
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