目录号 | 产品详情 | 靶点 | |
---|---|---|---|
T60082 | HDAC | ||
HDAC-IN-40 是一种有效的基于烷氧基酰胺的 HDAC 抑制剂,对 HDAC2 和 HDAC6 的 Ki 分别为 60 nM 和 30 nM。HDAC-IN-40 具有抗肿瘤作用。 | |||
T8508 | HDAC | ||
HDAC-IN-3 (GSK3117391A)是组蛋白脱乙酰酶抑制剂,可治疗慢性炎症性疾病。 | |||
T77334 | Apoptosis HDAC | ||
HDAC-IN-57 是一种具有口服活性的组蛋白脱乙酰酶 (HDAC) 泛抑制剂,对 HDAC1, HDAC2, HDAC6, HDAC8 具有抑制作用, IC50 值分别为 2.07 nM, 4.71 nM, 2.4 nM 和 107 nM。HDAC-IN-57 对 LSD1具有抑制作用, IC50 值为 1.34 μΜ。HDAC-IN-57 具有抗肿瘤活性,可诱导凋亡 (apoptosis)。 | |||
T7082 | HDAC | ||
HDAC8-IN-1 是一种 HDAC8 抑制剂,在癌细胞系中的 IC50 为 27.2 nM,有抗增殖作用。 | |||
T63399L | HDAC mTOR | ||
mTOR/HDAC-IN-1 HCl 是一种有效的 mTOR 和 HDAC 双重抑制剂,具有潜在的抗炎、抗增殖、自噬和诱导凋亡作用,可用于研究癌症。mTOR/HDAC-IN-1 HCl 是一种有效的 mTOR 和 HDAC 双重抑制剂,具有潜在的抗炎、抗增殖、自噬和凋亡诱导作用,可用于研究癌症。 | |||
T6327 | Virus Protease HDAC | ||
Tubacin 是一种高效、选择性、可逆、可渗透细胞的 HDAC6 抑制剂,IC50 为 4 nM,选择性是 HDAC1 的约 350 倍。 | |||
T2025 | HDAC | ||
HDAC-IN-7 (HBI-8000) 是 Chidamide 的一种杂质。Chidamide 是一种可口服的 HDAC 酶 I 类 HDAC1/2/3 和 IIb 类 HDAC10 抑制剂。 | |||
T10245 | HDAC | ||
ACY-957 (HDAC Inhibitor C001) 是一种具有口服活性,选择性的 HDAC1 和 HDAC2 抑制剂,对 HDAC1/2/3 的 IC50 值分别为 7 nM,18 nM 和 1300 nM,对 HDAC4/5/6/7/8/9 无作用。 | |||
T24133 | HDAC | ||
HDAC8-IN-20a (HDAC8 inhibitor-20a) 是一种有效的、具有选择性的HDAC8抑制剂,IC50为27 nM。HDAC8-IN-20a 可阻断生长受体存活信号的激活。 | |||
T39990 | |||
HDAC-IN-26 is a highly selective class I HDAC inhibitor with an EC 50 value of 4.7 nM. |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
---|---|---|---|---|---|
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.
|
|||||
TMPH-01476 | HDAC9 Protein, Human, Recombinant (His) | Human | E. coli | ||
HDAC9 Protein, Human, Recombinant (His) is expressed in E. coli.
|
|||||
TMPY-02317 | HDAC8 Protein, Mouse, Recombinant (His) | Mouse | Baculovirus-Insect Cells | ||
Histone deacetylase 8, also known as HDAC8 and HDACL1, is a nucleus and cytoplasm protein that belongs to the histone deacetylase family and HD type 1 subfamily. Histone deacetylases (HDACs) are a growing family of enzymes implicated in transcriptional regulation by affecting the acetylation state of core histones in the nucleus of cells. HDAC8 / HDACL1 is weakly expressed in most tissues. It is expressed at a higher level in the heart, brain, kidney, and pancreas and also in the liver, lung, placenta, prostate, and kidney. HDAC8 / HDACL1 is 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. HDAC8 / HDACL1 may play a role in smooth muscle cell contractility. HDAC8 / HDACL1 may be a potential drug target for neuroblastoma differentiation therapy using selective inhibitors, avoiding unspecific side effects.
|
|||||
TMPH-01472 | HDAC11 Protein, Human, Recombinant (GST) | Human | E. coli | ||
HDAC11 Protein, Human, Recombinant (GST) is expressed in E. coli.
|
|||||
TMPH-01474 | HDAC6 Protein, Human, Recombinant (His) | Human | E. coli | ||
HDAC6 Protein, Human, Recombinant (His) is expressed in E. coli.
|
|||||
TMPH-01471 | HDAC1 Protein, Human, Recombinant (His & SUMO) | Human | E. coli | ||
HDAC1 Protein, Human, Recombinant (His & SUMO) is expressed in E. coli.
|
|||||
TMPY-01333 | HDAC8 Protein, Human, Recombinant (GST) | Human | Baculovirus-Insect Cells | ||
Histone deacetylase 8, also known as HDAC8 and HDACL1, is a nucleus and cytoplasm protein that belongs to the histone deacetylase family and HD type 1 subfamily. Histone deacetylases (HDACs) are a growing family of enzymes implicated in transcriptional regulation by affecting the acetylation state of core histones in the nucleus of cells. HDAC8 / HDACL1 is weakly expressed in most tissues. It is expressed at a higher level in the heart, brain, kidney, and pancreas and also in the liver, lung, placenta, prostate, and kidney. HDAC8 / HDACL1 is 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. HDAC8 / HDACL1 may play a role in smooth muscle cell contractility. HDAC8 / HDACL1 may be a potential drug target for neuroblastoma differentiation therapy using selective inhibitors, avoiding unspecific side effects.
|
|||||
TMPH-01475 | HDAC7 Protein, Human, Recombinant (His) | Human | E. coli | ||
HDAC7 Protein, Human, Recombinant (His) is expressed in E. coli.
|
|||||
TMPH-01473 | HDAC3 Protein, Human, Recombinant (His & SUMO) | Human | E. coli | ||
HDAC3 Protein, Human, Recombinant (His & SUMO) is expressed in E. coli.
|
|||||
TMPH-01242 | IKZF1 Protein, Human, Recombinant (Avi & His) | Human | E. coli | ||
Transcription regulator of hematopoietic cell differentiation. Binds gamma-satellite DNA. Plays a role in the development of lymphocytes, B- and T-cells. Binds and activates the enhancer (delta-A element) of the CD3-delta gene. Repressor of the TDT (fikzfterminal deoxynucleotidyltransferase) gene during thymocyte differentiation. Regulates transcription through association with both HDAC-dependent and HDAC-independent complexes. Targets the 2 chromatin-remodeling complexes, NuRD and BAF (SWI/SNF), in a single complex (PYR complex), to the beta-globin locus in adult erythrocytes. Increases normal apoptosis in adult erythroid cells. Confers early temporal competence to retinal progenitor cells (RPCs). Function is isoform-specific and is modulated by dominant-negative inactive isoforms.
|
|||||
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.
|
|||||
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.
|
|||||
TMPY-01713 | RbAp48 Protein, Human, Recombinant (His) | Human | Baculovirus-Insect Cells | ||
Histone-binding protein RBBP4, also known as Retinoblastoma-binding protein 4, Retinoblastoma-binding protein p48, Chromatin assembly factor 1 subunit C, Chromatin assembly factor I p48 subunit, Nucleosome-remodeling factor subunit RBAP48 and RBBP4, is a nucleus protein which belongs to the WD repeat RBAP46/RBAP48/MSI1 family. RBBP4 is a core histone-binding subunit that may target chromatin assembly factors, chromatin remodeling factors and histone deacetylases to their histone substrates in a manner that is regulated by nucleosomal DNA. RBBP4 is a component of several complexes which regulate chromatin metabolism. These include the chromatin assembly factor 1 (CAF-1) complex, which is required for chromatin assembly following DNA replication and DNA repair; the core histone deacetylase (HDAC) complex, which promotes histone deacetylation and consequent transcriptional repression; the nucleosome remodeling and histone deacetylase complex (the NuRD complex), which promotes transcriptional repression by histone deacetylation and nucleosome remodeling and the NURF (nucleosome remodeling factor) complex. One common myth is that age-related memory loss is an early indication of Alzheimer's disease. But researchers at the Columbia University Medical Center in New York City have found a specific protein, RbAp48, that they believe is responsible for age-related memory problems. What's more, by replenishing RbAp48 in the brains of mice, the researchers were able to undo existing age-related memory damage. To find RbAp48, researchers focused on the hippocampus, the region of the brain where memories are formed. After studying eight healthy brains donated to science by people between the ages of 33 and 88, they found that RbAp48 was reduced by nearly 5 percent in the older brains. The researchers found that when they turned off RbAp48 in younger mice, they became more forgetful, while increasing RbAp48 in older mice restored memory. The mice were given memory tests that included object recognition and water maze problems.
|
|||||
TMPY-05251 | RbAp48 Protein, Mouse, Recombinant (His) | Mouse | Baculovirus-Insect Cells | ||
Histone-binding protein RBBP4, also known as Retinoblastoma-binding protein 4, Retinoblastoma-binding protein p48, Chromatin assembly factor 1 subunit C, Chromatin assembly factor I p48 subunit, Nucleosome-remodeling factor subunit RBAP48 and RBBP4, is a nucleus protein which belongs to the WD repeat RBAP46/RBAP48/MSI1 family. RBBP4 is a core histone-binding subunit that may target chromatin assembly factors, chromatin remodeling factors and histone deacetylases to their histone substrates in a manner that is regulated by nucleosomal DNA. RBBP4 is a component of several complexes which regulate chromatin metabolism. These include the chromatin assembly factor 1 (CAF-1) complex, which is required for chromatin assembly following DNA replication and DNA repair; the core histone deacetylase (HDAC) complex, which promotes histone deacetylation and consequent transcriptional repression; the nucleosome remodeling and histone deacetylase complex (the NuRD complex), which promotes transcriptional repression by histone deacetylation and nucleosome remodeling and the NURF (nucleosome remodeling factor) complex. One common myth is that age-related memory loss is an early indication of Alzheimer's disease. But researchers at the Columbia University Medical Center in New York City have found a specific protein, RbAp48, that they believe is responsible for age-related memory problems. What's more, by replenishing RbAp48 in the brains of mice, the researchers were able to undo existing age-related memory damage. To find RbAp48, researchers focused on the hippocampus, the region of the brain where memories are formed. After studying eight healthy brains donated to science by people between the ages of 33 and 88, they found that RbAp48 was reduced by nearly 5 percent in the older brains. The researchers found that when they turned off RbAp48 in younger mice, they became more forgetful, while increasing RbAp48 in older mice restored memory. The mice were given memory tests that included object recognition and water maze problems.
|
|||||
TMPH-00841 | SMARCA4 Protein, Human, Recombinant (His) | Human | E. coli | ||
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.
|
|||||
TMPH-02217 | SMARCA4 Protein, Human, Recombinant (His) | Human | 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.
|