目录号 | 产品详情 | 靶点 | |
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T36110 | |||
L-Pyrohomoglutamic acid is an amino acid building block.1,2It has been used in the synthesis of ligands for FK506-binding proteins (FKBPs) and histone deacetylase (HDAC) inhibitors. 1.Pomplun, S., Wang, Y., Kirschner, A., et al.Rational design and asymmetric synthesis of potent and neurotrophic ligands for FK506-binding proteins (FKBPs)Angew. Chem. Int. Ed.54(1)345-348(2015) 2.Taddei, M., Cini, E., Giannotti, L., et al.Lactam based 7-amino suberoylamide hydroxamic acids as potent HDAC inhibitorsBioorg. Med. Chem. Lett.24(1)61-64(2014) | |||
T71011 | |||
Perfluorinated SAHA is an HDAC inhibitor for use in cancer treatment regimens, with demonstrated greater antiproliferative properties than SAHA . PFSAHA has also been shown to have higher selectivity for PA3774, an HDAC-like enzyme from P. aeruginosa, as well as other HDACs, which may prove beneficial for developing novel chemotherapeutic treatments for cancer. | |||
T74368 | |||
OKI-006 是一种有效的、具有口服活性的组蛋白脱乙酰酶 (HDAC) 抑制剂。OKI-006 是天然产物HDAC 抑制剂 largazole 的独特同系物。组蛋白去乙酰化酶 (HDAC) 在表观基因组调控中起关键作用,并且组蛋白乙酰化在许多人类癌症中失调。OKI-006 具有研究癌症疾病的潜力。 | |||
T79543 | HDAC | ||
J27644为一高效HDAC抑制剂,能缓解TGF-β所引发的肺纤维化现象。 | |||
T77773 | |||
KT-531(KT531)是高效的选择性HDAC6抑制剂,具有8.5 nM的IC50值,其对其他HDAC同工酶的选择性高出39倍。 | |||
T79840 | HDAC | ||
Bocodepsin hydrochloride (OKI-179) 是一种口服活性的选择性HDAC抑制剂,具抗肿瘤特性,适用于治疗实体瘤和血液系统恶性肿瘤。 | |||
T81974 | HDAC | ||
KPZ560作为HDAC1和HDAC2的有效抑制剂,在IC50数值上分别达到12 nM 和68 nM 。此化合物能提升小鼠颗粒神经元树突的棘密度,同时也能抑制MCF乳腺癌细胞系的生长。 | |||
T81725 | HDAC | ||
Mz325为HDAC与Sirt2的双重抑制剂,针对Sirt2展现9.7 μM的IC50,其在癌症和神经退行性疾病的发病机制中扮演关键角色。 | |||
T78709 | HDAC | ||
NT160,一种IIa类HDAC高效抑制剂,IC50为0.046 μM,适用于中枢神经系统疾病研究。 | |||
T81100 | |||
ST8155AA1为一种抗体偶联药物(ADCs)成分,载有HDAC抑制剂并连接物,展现出对抗肿瘤的活性。 |
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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