目录号 | 产品详情 | 靶点 | |
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T62916 | |||
GEM144 是一种有效的、口服具有活力的 DNA polymerase α(POLA1) 和HDAC 11 双重抑制剂。GEM144 能够诱导 p53 乙酰化、激活 p21,将细胞周期阻滞在 G1/S 期,并诱导细胞凋亡。 | |||
T70778 | |||
Depudecin is a polyketide obtained from the fungus Alternaria brassicicola and having a highly unusual structure of an 11-carbon chain containing two epoxides and six stereogenic centres. It is an inhibitor of histone deacetylase (HDAC) both in vivo and in vitro and also exhibits anti-angiogenic activity. | |||
T21749 | |||
4-Iodo-SAHA (1k) 是一种具有口服活性的I 类和II 类histone deacetylase (HDAC)抑制剂,对 Skbr3、 HT29、 U937、 JA16 和 HL60细胞的EC50值分别为1.1、0.95、0.12、0.24、0.85和1.3 μM。4-Iodo-SAHA (1k) 可用于癌症的研究。 | |||
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。 | |||
T74453 | |||
JPS014, 基于苯甲酰胺的Von Hippel-Lindau (VHL) E3-连接酶蛋白水解靶向嵌合体 (PROTAC),有效降解I 类组蛋白脱乙酰酶 (HDAC)。它作为HDAC1/2的强效降解剂,与HCT116细胞中的总差异表达基因更大和增强的细胞凋亡 (apoptosis) 密切相关。 | |||
T77937 | HDAC | ||
JPS014 TFA是一种VHL E3连接酶蛋白水解靶向嵌合体(PROTAC),以苯甲酰胺为基础,专门降解I类组蛋白脱乙酰酶(HDAC)。作为一种高效的HDAC1/2降解剂,JPS014 TFA与HCT116细胞中广泛的基因表达差异及促进细胞凋亡(apoptosis)密切相关。 | |||
T74454 | |||
JPS016 是一种基于苯甲酰胺的Von Hippel-Lindau (VHL)E3-连接酶蛋白水解靶向嵌合体 (PROTAC)。JPS016 降解 I 类组蛋白脱乙酰酶 (HDAC)。JPS016 是一种有效的 HDAC1/2 降解剂,与 HCT116 细胞中更大的总差异表达基因和增强的细胞凋亡 (apoptosis) 相关。 | |||
T36303 | |||
Psammaplin A, a marine metabolite, functions as a robust inhibitor of HDAC and DNA methyltransferases, displaying notable potency and selectivity as a DAC1 inhibitor, with an IC50 value of 0.9 nM. It exhibits antimicrobial effects against Gram-positive bacteria and inhibits both DNA synthesis and DNA gyrase activity, also demonstrating antitumor activity[1][2]. | |||
T70962 | |||
MHY219 is a novel HDAC inhibitor. MHY219 induces apoptosis via up-regulation of androgen receptor expression in human prostate cancer cells. MHY219 was shown to enhance the cytotoxicity on DU145 cells (IC50, 0.36 μM) when compared with LNCaP (IC50, 0.97 μM) and PC3 cells (IC50, 5.12 μM). MHY219 showed a potent inhibition of total HDAC activity when compared with SAHA. MHY219 increased histone H3 hyperacetylation and reduced the expression of class I HDACs (1, 2 and 3) in prostate cancer cells. MHY219 effectively increased the sub-G1 fraction of cells through p21 and p27 dependent pathways in DU145 cells. MHY219 significantly induced a G2/M phase arrest in DU145 and PC3 cells and arrested the cell cycle at G0/G1 phase in LNCaP cells. Furthermore, MHY219 effectively increased apoptosis in DU145 and LNCaP cells, but not PC3 cells, according to Annexin V/PI staining and Western blot analysis. These results indicate that MHY219 is a potent HDAC inhibitor that targets regulating mu...... | |||
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。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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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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TMPY-01333 | HDAC8 Protein, Human, Recombinant (GST) | Human | Baculovirus Insect Cells | ||
HDAC8 Protein, Human, Recombinant (GST) is expressed in Baculovirus insect cells with GST tag. The predicted molecular weight is 68 kDa and the accession number is Q9BY41-1.
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TMPH-01476 | HDAC9 Protein, Human, Recombinant (His) | Human | E. coli | ||
HDAC9 Protein, Human, Recombinant (His) is expressed in E. coli.
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TMPH-01472 | HDAC11 Protein, Human, Recombinant (GST) | Human | E. coli | ||
Responsible for the deacetylation of lysine residues on the N-terminal part of the core histones (H2A, H2B, H3 and H4). Histone deacetylation gives a tag for epigenetic repression and plays an important role in transcriptional regulation, cell cycle progression and developmental events. Histone deacetylases act via the formation of large multiprotein complexes. HDAC11 Protein, Human, Recombinant (GST) is expressed in E. coli expression system with N-GST tag. The predicted molecular weight is 66.2 kDa and the accession number is Q96DB2.
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TMPY-02317 | HDAC8 Protein, Mouse, Recombinant (His) | Mouse | Baculovirus Insect Cells | ||
HDAC8 Protein, Mouse, Recombinant (His) is expressed in Baculovirus insect cells with His tag. The predicted molecular weight is 43.1 kDa and the accession number is Q8VH37-1.
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TMPH-01474 | HDAC6 Protein, Human, Recombinant (His) | Human | E. coli | ||
HDAC6 Protein, Human, Recombinant (His) is expressed in E. coli.
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TMPH-01471 | HDAC1 Protein, Human, Recombinant (His & SUMO) | Human | E. coli | ||
HDAC1 Protein, Human, Recombinant (His & SUMO) is expressed in E. coli expression system with N-6xHis-SUMO tag. The predicted molecular weight is 71.1 kDa and the accession number is Q13547.
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TMPH-01475 | HDAC7 Protein, Human, Recombinant (His) | Human | E. coli | ||
N/A. HDAC7 Protein, Human, Recombinant (His) is expressed in E. coli expression system with N-6xHis tag. The predicted molecular weight is 26 kDa and the accession number is Q8WUI4 (BC064840).
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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-03056 | LSD1 Protein, Human, Recombinant (His & GST) | Human | Baculovirus Insect Cells | ||
LSD1 belongs to the flavin monoamine oxidase family. It contains 1 SWIRM domain and is a component of an RCOR/GFI/LSD1/HDAC complex. LSD1 interacts directly with GFI1 and GFI1B. LSD1 specifically removes histone H3K4me2 to H3K4me1 or H3K4me0 through a FAD-dependent oxidative reaction. When forming a complex with an androgen receptor (and possibly other nuclear hormone receptors), LSD1 changes its substrates to H3K9me2. Thus LSD1 is considered to act as a coactivator or a corepressor. It may play a role in the repression of neuronal genes. Alone, LSD1 is unable to demethylate H3 'Lys-4' on nucleosomes and requires the presence of RCOR1/CoREST to achieve such activity.
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TMPY-03283 | HBP1 Protein, Human, Recombinant (GST) | Human | E. coli | ||
HBP1 is a sequence-specific DNA-binding transcription factor. It is involved in many biological processes. It was reported that HBP1 binds to p16(INK4A) promoter and activates p16(INK4A) expression. We found that trichostatin A (TSA), an inhibitor of HDAC (histone deacetylase), induces p16(INK4A) expression in an HBP1-dependent manner. HBP1 activates or represses the expression of some specific genes during cell growth and differentiation. HBP1 was acetylated by p3/CBP in two regions: repression domain (K297/35/37) and P domain (K171/419). HBP1 acetylation after TSA treatment was confirmed by immunoprecipitation assay. HBP1 interacted with histone acetyltransferase p3 and CREB-binding protein (CBP) and also recruited p3/CBP to p16(INK4A) promoter. HBP1 acetylation at K419 plays an important role in HBP1-induced p16(INK4A) expression.
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TMPH-02217 | SMARCA4 Protein, Human, Recombinant (His) | Human | P. pastoris (Yeast) | ||
Involved in transcriptional activation and repression of select genes by chromatin remodeling (alteration of DNA-nucleosome topology). Component of SWI/SNF chromatin remodeling complexes that carry out key enzymatic activities, changing chromatin structure by altering DNA-histone contacts within a nucleosome in an ATP-dependent manner. Component of the CREST-BRG1 complex, a multiprotein complex that regulates promoter activation by orchestrating the calcium-dependent release of a repressor complex and the recruitment of an activator complex. In resting neurons, transcription of the c-FOS promoter is inhibited by SMARCA4-dependent recruitment of a phospho-RB1-HDAC repressor complex. Upon calcium influx, RB1 is dephosphorylated by calcineurin, which leads to release of the repressor complex. At the same time, there is increased recruitment of CREBBP to the promoter by a CREST-dependent mechanism, which leads to transcriptional activation. The CREST-BRG1 complex also binds to the NR2B promoter, and activity-dependent induction of NR2B expression involves the release of HDAC1 and recruitment of CREBBP. Belongs to the neural progenitors-specific chromatin remodeling complex (npBAF complex) and the neuron-specific chromatin remodeling complex (nBAF complex). During neural development, a switch from a stem/progenitor to a postmitotic chromatin remodeling mechanism occurs as neurons exit the cell cycle and become committed to their adult state. The transition from proliferating neural stem/progenitor cells to postmitotic neurons requires a switch in subunit composition of the npBAF and nBAF complexes. As neural progenitors exit mitosis and differentiate into neurons, npBAF complexes which contain ACTL6A/BAF53A and PHF10/BAF45A, are exchanged for homologous alternative ACTL6B/BAF53B and DPF1/BAF45B or DPF3/BAF45C subunits in neuron-specific complexes (nBAF). The npBAF complex is essential for the self-renewal/proliferative capacity of the multipotent neural stem cells. The nBAF complex along with CREST plays a role regulating the activity of genes essential for dendrite growth. SMARCA4/BAF190A may promote neural stem cell self-renewal/proliferation by enhancing Notch-dependent proliferative signals, while concurrently making the neural stem cell insensitive to SHH-dependent differentiating cues. Acts as a corepressor of ZEB1 to regulate E-cadherin transcription and is required for induction of epithelial-mesenchymal transition (EMT) by ZEB1. Binds via DLX1 to enhancers located in the intergenic region between DLX5 and DLX6 and this binding is stabilized by the long non-coding RNA (lncRNA) Evf2. Binds to RNA in a promiscuous manner. Binding to RNAs including lncRNA Evf2 leads to inhibition of SMARCA4 ATPase and chromatin remodeling activities.
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