目录号 | 产品详情 | 靶点 | |
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T62708 | |||
HDAC-IN-37 是一种 HDAC 的有效抑制剂,作用于 HDAC1 (IC50: 0.0551 μM)、HDAC3 (IC50: 1.24 μM)、HDAC8 (IC50: 0.948 μM) 和 HDAC6 (IC50: 34.2 μM)。HDAC-IN-37 能够缓慢诱导组蛋白乙酰化。HDAC-IN-37 阻碍细胞由 G1 期向 S 期转变,诱导早期细胞凋亡。 | |||
T1890 | Apoptosis HDAC | ||
Pracinostat (SB939) 是一种组蛋白去乙酰化酶抑制剂,对 HDACs 的IC50值为 40-140 nM,可用于研究癌症。 | |||
T6637 | HDAC | ||
Resminostat (4SC-201) 是一种可口服的HDAC1、HDAC3和HDAC6抑制剂,IC50值分别为 42.5、50.1和71.8 nM,具有潜在抗肿瘤活性。 | |||
T63416 | |||
HDAC-IN-39 是 HDAC 的有效抑制剂,能够作用于HDAC1、HDAC2、HDAC3,他们的IC50值分别为 1.07 μM、1.47 μM 和 2.27 μM。HDAC-IN-39 能够诱导细胞周期阻滞在 G2/M 期,同时也能够明显抑制微管聚合。HDAC-IN-39 对耐药癌细胞表现出良好的抗癌作用。 | |||
T62366 | |||
TH-6 是一种 HDAC 的有效抑制剂,能够作用于 HDAC1 (IC50: 0.115 μM)、HDAC2 (IC50: 0.135 μM)、HDAC3 (IC50: 0.242 μM)、HDAC6 (IC50: 0.138 μM)、HDAC8 (IC50: 2.120 μM)。TH-6 能够将细胞周期阻滞在 G2/M 期,诱导细胞凋亡。TH-6 对细胞迁移和侵袭具有抑制作用,表现出抗肿瘤作用。 | |||
T73167 | |||
HDAC-IN-49 是一种有效的非选择性 HDAC(HDAC) 抑制剂,对 HDAC1、HDAC2、HDAC3、HDAC4 和 HDAC6的 IC50分别为 13 nM、14 nM、21 nM、1880 nM 和 10 nM 。HDAC-IN-49 表现出显着的抗白血病活性, 但对健康细胞具有低细胞毒性。 | |||
T61139 | |||
HDAC6-IN-3 (Compound 14) is a potent anti-prostate cancer agent that acts as an orally active inhibitor of HDAC6. It has IC50 values ranging from 0.02-1.54 μM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10. Additionally, HDAC6-IN-3 also demonstrates effective inhibition of MAO-A (IC50 = 0.79 μM) and LSD1 [1]. | |||
T73520 | |||
TNG260 是一种CoREST 选择性脱乙酰酶(CoreDAC) 抑制剂。 TNG260 抑制HDAC1的选择性是HDAC3的 10 倍。 TNG260 导致HDAC1抑制,逆转由 STK11 缺失驱动的抗 PD1 耐药性。 TNG260 减少嗜中性粒细胞的瘤内浸润。 TNG260 表现出免疫介导的细胞杀伤。 | |||
T81499 | PI3K | ||
PH14,作为一种PI3K/HDAC双重抑制剂,对PI3Kα和HDAC3表现出强效抑制能力,其IC50值分别为20.3 nM 和24.5 nM 。该化合物不仅具备抗增殖特性,还能有效诱导Jeko-1细胞走向凋亡,是研究癌症(例如淋巴瘤)的有力工具。 | |||
T61474 | |||
HDAC6-IN-13 (Compound 35m) is a potent and highly selective orally active inhibitor of HDAC6, with an IC50 of 0.019 μM. It also demonstrates inhibitory activity against HDAC1, HDAC2, and HDAC3, with IC50 values of 1.53 μM, 2.06 μM, and 1.03 μM, respectively. HDAC6-IN-13 exhibits substantial blood-brain barrier permeability and displays anti-inflammatory properties [1]. |
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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