目录号 | 产品详情 | 靶点 | |
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T24131 | Histone Demethylase Antiviral | ||
HDAC3-IN-T247 (HDAC3 inhibitor T247) 是一种具有选择性和有效性的组蛋白去乙酰化酶 3(HDAC3) 抑制剂,具有抗癌和抗病毒活性。HDAC3-IN-T247 以剂量依赖的方式诱导人结肠癌 HCT116 细胞中 NF-κB 乙酰化。HDAC3-IN-T247 抑制癌细胞增殖。 | |||
T36575 | |||
HDAC3 inhibitor is an allosteric inhibitor of histone deacetylase 3 (HDAC3; Ki = 0.16 nM). It is selective for HDAC3 over HDAC1 and HDAC2 (IC50s = 0.95, 11.81, and 95.45 nM, respectively, using recombinant HDACs). In addition, it is selective for acute myeloid, monocytic, and lymphoblastic leukemia cell lines (EC50s = 36.37, 76.64, and 151.7 nM, respectively) over chronic myeloid, acute promyelocytic, and acute lymphoblastic cells (EC50s = 2,160, >10,000, and >10,000 nM, respectively). | |||
T24132 | |||
HDAC3-IN-T326 is a potent and selective HDAC3 inhibitor that acts by increasing NF-κB acetylation and activating HIV gene expression in latent HIV-infected cells. | |||
T10255 | HDAC | ||
AES-135 是一种基于羟肟酸的泛HDAC 抑制剂,抑制 HDAC3、HDAC6和 HDAC11,IC50为 654、190 和 636 nM,具有抗肿瘤活性。 | |||
T5347 | HDAC | ||
CXD101 是一种选择性和具有口服活性的 I 类HDAC 抑制剂,有抗肿瘤活性,对HDAC1、HDAC2和HDAC3的IC50分别为 63、570 和 550 nM。 | |||
T8233 | Apoptosis HIV Protease HDAC | ||
BRD3308 是一种高选择性的HDAC3抑制剂,IC50为 54 nM。它可激活HIV-1转录并破坏HIV-1潜伏期。它抑制由炎性细胞因子或糖脂毒性应激诱导的胰腺 β 细胞凋亡,并增加功能性胰岛素释放。 | |||
T74003 | |||
HDAC3/6-IN-2 (化合物 15) 是一种高效的HDAC6和HDAC3抑制剂,IC50值分别为0.368 μM和0.635 μM。此化合物不仅具备抗肿瘤活性,能够诱导癌细胞凋亡,同时通过降低HDAC6和HDAC3水平,与H3乙酰化和α-微管蛋白的上调有关。 | |||
T6481 | Apoptosis HDAC | ||
Droxinostat (NS 41080) 是HDAC3、HDAC6和HDAC8抑制剂,IC50分别为16.9、2.47和1.46 μM。 | |||
T79714 | HDAC | ||
HDAC3-IN-2 (compound 4i) 是一种具有纳摩尔级效力的吡嗪酰肼基HDAC3抑制剂,IC50值为14 nM,针对三阴性乳腺癌细胞表现出高效抑制作用。该化合物在细胞内毒性测定中显示,对4T1细胞株的IC50为0.55 μM,对MDA-MB-231细胞株的IC50为0.74 μM。HDAC3-IN-2通过增加乙酰化水平(如H3K9、H3K27和H4K12),促进细胞凋亡(涉及caspase-3、caspase-7和细胞色素c的水平提升),并抑制细胞增殖相关蛋白(如Bcl-2、CD44、EGFR和Ki-67)的表达,从而在荷瘤小鼠模型中表现出显著的体内抗肿瘤作用。 | |||
T6286 | HDAC | ||
RGFP966 是一种 HDAC3 抑制剂,IC50 为 0.08 μM,比其他 HDAC 选择性高 200 倍以上。 |
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.
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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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