目录号 | 产品详情 | 靶点 | |
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T36102 | |||
4-Chloro-6,7-bis(2-methoxyethoxy)quinazoline is a building block and synthetic intermediate.1,2,3,4,5It has been used as a precursor in the synthesis of receptor tyrosine kinase (RTK) inhibitors, dual RTK and histone deacetylase (HDAC) inhibitors, and anticancer compounds.1,2,3It is also a synthetic intermediate in the synthesis of EGFR inhibitors, including erlotinib , with antiproliferative activity.4,5 | |||
T71420 | |||
RO314724 is a HDAC inhibitor. RO314724 is also a a reversible, tightly binding, MMP inhibitor with a Ki of 26 nm. Matrix metalloproteinases (MMPs) belong to the key enzymes of the proteolytic destruction of cartilage matrix during chronic rheumatic diseases. Ro314724 displayed MMP-proteoglycanase inhibitory activity both in vitro and ex vivo and proved to be not harmful to the morphology, viability and proteoglycan biosynthesis of bovine articular cartilage explants. | |||
T79407 | Others | ||
HL23是一种HDAC抑制剂,对抗HCC具有活性。通过增强TXNIP启动子乙酰化,此化合物上调TXNIP表达,进而介导钾通道活性并触发TXNIP依赖性钾剥夺,抑制HCC的进展和转移。HL23与Sorafenib联合应用时显示出协同作用,并且其效力超过Sorafenib与Vorinostat的联用。 | |||
T64152 | |||
Purinostat mesylate 是一种选择性的 HDAC 抑制剂。Purinostat mesylate 能够抑制 I 型和 IIb 型 HDACs (IC50: 0.81-11.5 nM)。Purinostat mesylate 能够影响LAMA84 和 188 BL-2 细胞的细胞周期,并诱导其凋亡,在体内显示出较强的抗白血病效果。Purinostat mesylate 能够用于研究淋巴细胞白血病。 | |||
T9644 | |||
Triciferol 作为具有结合了 VDR 激动剂和 HDAC 拮抗剂活性的多重配体发挥作用。Triciferol 直接与 VDR 结合 (IC50=87 nM),在一些 1,25D 靶基因上作为具有 1,25D 样效力的激动剂发挥作用。Triciferol 诱导显著的微管蛋白高乙酰化,并增强组蛋白乙酰化。Triciferol 在体外癌细胞模型中也表现出有效的抗增殖和细胞毒性活性。 | |||
T35824 | |||
Trapoxin A 是一种微生物环状四肽,是 I 类组蛋白脱乙酰酶 (HDAC) 的不可逆抑制剂。 | |||
T36421 | |||
The Immuno-Oncology Screening Library consists of 2 plates and contains more than 90 cancer and immunology-associated compounds in a 96-well Matrix tube rack format as 10 mM stock solutions in DMSO. This library includes a variety of immuno-oncology target modulators, including but not limited to, adenosine, CCR, CXCR, and TLR agonists and antagonists, BTK, PI3K, VEGFR, and BRAF inhibitors, PD-1/PDL-1 interaction inhibitors, and HDAC inhibitors. Please review the product insert for a full list of targets. Stability data is not available for the compounds as supplied in the screening library. | |||
T70748 | |||
Bisthianostat, also known as CF367 or CF367;-C, is a novel Orally Efficacious Pan-HDAC Inhibitor. Bisthianostat selectively binds to and inhibits HDACs, which inhibits deacetylation of histone proteins and leads to the accumulation of highly acetylated histones. This may result in an induction of chromatin remodeling, the inhibition of tumor oncogene transcription, and the selective transcription of tumor suppressor genes. This prevents cell division, induces cell cycle arrest and apoptosis. This may inhibit the proliferation of susceptible tumor cells. HDACs, upregulated in many tumor cell types, are a family of enzymes that deacetylate histone proteins. | |||
T61753 | |||
MPT0G211 mesylate is a powerful and selective HDAC6 inhibitor (IC50 = 0.291 nM), with high oral bioavailability. It exhibits remarkable selectivity for HDAC6 over other HDAC isoforms (>1000-fold selectivity). Additionally, MPT0G211 mesylate can effectively cross the blood-brain barrier. In preclinical studies using an Alzheimer's disease model, MPT0G211 mesylate has shown promising results in reducing tau phosphorylation and cognitive deficits. Furthermore, this compound exhibits anti-metastatic and neuroprotective effects, making it a potential candidate for anticancer interventions. [1] [2] [3]. | |||
T83946 | |||
CHDI 00484077是一种强效且选择性的IIa类组蛋白去乙酰化酶(HDAC)抑制剂,其体内IC50值为10-30 nM,而在HEK293和Jurkat细胞中的IC50值分别为0.01 nM和0.04 nM。在细胞中对IIa类HDACs具有150倍的选择性,优于I/IIb类HDACs。具有口服生物可用性和中枢神经系统(CNS)穿透能力。 |
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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