目录号 | 产品详情 | 靶点 | |
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T63543 | |||
HDAC/Top-IN-1 是广谱的、口服具有活力的 HDAC/Top 双重抑制剂,能够作用于HDAC1 (IC50: 0.036 μM)、HDAC2 (IC50: 0.14 μM)、HDAC3 (IC50: 0.059 μM)、HDAC6 (IC50: 0.089 μM) 和 HDAC8 (IC50: 9.8 μM)。HDAC/Top-IN-1 能够将HEL 细胞的细胞阻滞在 S 期,并有效诱导细胞凋亡 (apoptosis)。 | |||
T74514 | PROTACs | ||
HD-TAC7 是一种有效的 PROTACHDAC 降解剂,对 HDAC1、HDAC2 和 HDAC3的 IC50分别为 3.6 μM、4.2 μM 和 1.1 μM。HD-TAC7 可降低 RAW 264.7 巨噬细胞NF-κBp65 表达。HD-TAC7 可用于哮喘和慢性阻塞性肺病(COPD)等炎症性疾病的研究。 | |||
T73181 | HDAC | ||
HDAC-IN-51 是一种 HDAC 抑制剂。 | |||
T78906 | HDAC | ||
CDK/HDAC-IN-3 是一种口服活性的 HDAC/CDK 双重抑制剂,对 CDK9、CDK12、CDK13 及 HDAC1、HDAC2、HDAC3 表现出有效且选择性的抑制,IC50 值分别为 98.32 nM、98.85 nM、100 nM、62.12 nM、93.28 nM 和 82.87 nM。该化合物主要用于急性髓性白血病 (AML) 的相关研究。 | |||
T78839 | HDAC | ||
HDAC6-IN-19(Compound 14g)是一种选择性HDAC6抑制剂,具有2.68 nM的IC50值。同时,该化合物对HDAC1、HDAC2和HDAC3也表现出一定的抑制作用,其IC50值分别为61.6 nM、98.7 nM和103 nM。此外,HDAC6-IN-19在抑制包括白血病、结肠癌、黑色素瘤和乳腺癌等多种癌细胞系的增殖方面显示出有效性。 | |||
T62109 | |||
HDAC-IN-31 是一种选择性的、有效的、口服具有活力的 HDAC 抑制剂,能够作用于 HDAC1 (IC50: 84.90 nM)、HDAC2 (IC50: 168.0 nM)、HDAC3 (IC50: 442.7 nM)、HDAC8 (IC50>10000 nM)。 HDAC-IN-31 能够将细胞周期阻滞在 G2/M 期,并诱导细胞凋亡 (apoptosis)。HDAC-IN-31 具有良好的抗肿瘤效果。HDAC-IN-31 对弥漫性大 B 细胞淋巴瘤表现出潜在的研究价值。 | |||
T61572 | |||
FNDR-20123 free base 是一种有效、安全、首创的抗疟疾HDAC 抑制剂,对疟原虫和人类 HDAC 的IC50分别为 31 nM 和 3 nM。FNDR-20123 free base 对恶性疟原虫 (Plasmodium falciparum) 无性期 (IC50=41 nM) 和性血期 (雄性配子体 IC50=190 nM) 具有抗疟疾活性。FNDR-20123 free base 抑制 HDAC1,HDAC2,HDAC3,HDAC6,HDAC8 的 IC50分别为 25,29,2,11,282 nM,并在纳摩尔浓度下抑制 III 类 HDAC 亚型。 | |||
T27051 | |||
CM-414 is a dual inhibitor of HDACs and PDE5 for the Treatment of Alzheimer’s Disease (IC50 values of 60 nM, 310 nM, 490 nM, 322 nM, and 91 nM against PDE5, HDAC1, HDAC2, HDAC3, and HDAC6, respectively). Chronic treatment of Tg2576 mice with CM-414 dimini | |||
T79452 | |||
Tubulin/HDAC-IN-2 (Compound II-19k) 为Tubulin和HDAC的双重抑制剂,IC50分别对HDAC1、HDAC2、HDAC3和HDAC6为0.403 μM、0.591μM、3.552μM和0.459μM。该化合物能够导致细胞周期在G2期的阻滞及诱导细胞凋亡。Tubulin/HDAC-IN-2 有效抑制血肿和实体瘤细胞增殖,降低肿瘤转移,并在肝肿瘤同种异体移植的小鼠模型中抑制肿瘤生长。 | |||
T62072 | |||
HDAC-IN-47 是一种口服具有活力的组蛋白去乙酰化酶 (HDAC) 的抑制剂,对 HDAC1、HDAC2、HDAC3、HDAC6、HDAC8 的 IC50 值分别为 19.75 nM、57.8 nM、40.27 nM、5.63 nM、302.73 nM。HDAC-IN-47 可以将细胞周期阻滞在 G2/M 期,抑制细胞自噬,能够利用 Bax/Bcl-2 和 caspase-3 通路诱导凋亡,在体内具有抗癌活性。 |
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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