HDAC Substrate, Colorimetric
- Known as:
- HDAC Substrate, Colorimetric
- Catalog number:
- 2207-100
- Product Quantity:
- 100 mg
- Category:
- -
- Supplier:
- Biovis
- Gene target:
- HDAC Substrate Colorimetric
Ask about this productRelated genes to: HDAC Substrate, Colorimetric
- Gene:
- HDAC4 NIH gene
- Name:
- histone deacetylase 4
- Previous symbol:
- BDMR
- Synonyms:
- KIAA0288, HDAC-A, HDACA, HD4, HA6116, HDAC-4
- Chromosome:
- 2q37.3
- Locus Type:
- gene with protein product
- Date approved:
- 2000-11-28
- Date modifiied:
- 2015-09-11
- Gene:
- HDAC7 NIH gene
- Name:
- histone deacetylase 7
- Previous symbol:
- HDAC7A
- Synonyms:
- DKFZP586J0917
- Chromosome:
- 12q13.11
- Locus Type:
- gene with protein product
- Date approved:
- 2001-07-13
- Date modifiied:
- 2016-10-05
- Gene:
- HDAC8 NIH gene
- Name:
- histone deacetylase 8
- Previous symbol:
- HDACL1, WTS, MRXS6
- Synonyms:
- RPD3, KDAC8
- Chromosome:
- Xq13.1
- Locus Type:
- gene with protein product
- Date approved:
- 2000-11-28
- Date modifiied:
- 2019-02-19
- Gene:
- HDAC9 NIH gene
- Name:
- histone deacetylase 9
- Previous symbol:
- -
- Synonyms:
- KIAA0744, HDAC, MITR, HD7, HDAC7B
- Chromosome:
- 7p21.1
- Locus Type:
- gene with protein product
- Date approved:
- 2002-09-06
- Date modifiied:
- 2015-09-11
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- Tropolone and thailandepsin B are naturally occurring substances that are primarily isolated from fungi and plants, although they can also be found in certain bacteria. Tropolones belong to an important class of aromatic compounds with a seven-membered nonbenzenoid ring structure. Thailandepsins are a group of natural products that were initially discovered in the culture broth of the Gram-negative bacterium Burkholderia thailandensis. Tropolonebased structures have been identified in over 200 natural compounds, ranging from simple tropolone derivatives to complex multicyclic systems like pycnidione and pyrerubrine A. These natural compounds exhibit a diverse range of pharmacological effects, including antibacterial, antifungal, insecticidal, phytotoxic, anti-inflammatory, antimitotic, anti-diabetic, enzyme inhibitory, anticancer, cytoprotective, and ROS scavenging properties. It is worth noting that thujaplicane, a compound similar to tropolone, displays all of the listed biological activities except for antimitotic action, which has only been observed in one natural tropolone compound, colchicine. Tropolone can be synthesized from commercially available seven-membered rings or derived through various cyclization and cycloaddition reactions. Thailandepsin B, on the other hand, can be synthesized by macro-lactonization of the corresponding secoacid, followed by the formation of internal disulfide bonds. It is important to mention that thailandepsin B exhibits different selective inhibition profiles compared to FK228. - Source: PubMed
Pal DilipkumarLal Padum - The present study aims to identify the effect of ZnHDACs expression on the survival of the patients. Further, reveal the unique and common genes associated with each ZnHDACs and their associated pathways. - Source: PubMed
Publication date: 2022/03/01
Ukey ShwetaRamteke AbhilashChoudhury ChinmayeePurohit PurviSharma Praveen - Histone deacetylases (HDACs) are key regulators of gene expression in cells and have been investigated as important therapeutic targets for cancer and other diseases. Different subtypes of HDACs appear to play disparate roles in the cells and are associated with specific diseases. Therefore, substantial effort has been made to develop subtype-selective HDAC inhibitors. In an effort to discover existing scaffolds with HDAC inhibitory activity, we screened a drug library approved by the US Food and Drug Administration and a National Institutes of Health Clinical Collection compound library in HDAC enzymatic assays. Ebselen, a clinical safe compound, was identified as a weak inhibitor of several HDACs, including HDAC1, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, and HDAC9 with half maximal inhibitory concentrations approximately single digit of µM. Two ebselen analogs, ebselen oxide and ebsulfur (a diselenide analog of ebselen), also inhibited these HDACs, however with improved potencies on HDAC8. Benzisothiazol, the core structure of ebsulfur, specifically inhibited HDAC6 at a single digit of µM but had no inhibition on other HDACs. Further efforts on structure-activity relationship based on the core structure of ebsulfur led to the discovery of a novel class of potent and selective HDAC6 inhibitors with RBC-2008 as the lead compound with single-digit nM potency. This class of histone deacetylase inhibitor features a novel pharmacophore with an ebsulfur scaffold selectively targeting HDAC6. Consistent with its inhibition on HDAC6, RBC-2008 significantly increased the acetylation levels of α-tubulin in PC-3 cells. Furthermore, treatment with these compounds led to cell death of multiple tumor cell lines in a dose-dependent manner. These results demonstrated that ebselen and ebsulfur analogs are inhibitors of HDACs, supporting further preclinical development of this class of compounds for potential therapeutic applications. - Source: PubMed
Publication date: 2017/05/02
Wang YurenWallach JasonDuane StephanieWang YuanWu JianghongWang JeffreyAdejare AdeboyeMa Haiching - Histone deacetylase (HDAC) inhibitors radiosensitize tumor cells. To elucidate mechanisms underlying radiosensitization by HDAC inhibition, understanding of differential contributions of HDAC isotypes is needed. The aim of this study was to investigate involvement of known HDAC isotypes in modulation of cellular radiosensitivity. - Source: PubMed
Publication date: 2015/11/17
Kim Jin HoMoon Sung HoNo MinaKim Jae JinChoi Eun JungCho Bong JunKim Jae SungKim Il HanKim In Ah - Epigenetics is the study of heritable alterations in gene expression that are not accompanied by the corresponding change in DNA sequence. Three interlinked epigenetic processes regulate gene expression at the level of chromatin, namely DNA methylation, nucleosomal remodeling and histone covalent modifications. Post-translational modifications that occur on certain amino acid residues of the tails of histone proteins modify chromatin structure and form the basis for "histone code". The enzymes Histone Acetyl Transferase (HAT) and Histone Deacetylase (HDAC) control the level of acetylation of histones and thereby alter gene expression. In many cancers, the balance between HAT and HDAC is altered. HDAC enzymes are grouped into four different classes namely Class I (HDAC1, HDAC2, HDAC3, and HDAC8), Class II (HDAC4, HDAC5, HDAC6, HDAC7, HDAC9, and HDAC10), Class III HDAC and Class IV (HDAC11). Histone Deacetylase Inhibitors (HDACI) exert anticancer activity by promoting acetylation of histones as well as by promoting acetylation of non-histone protein substrates. The effects of HDACI on gene transcription are complex. They cause cell cycle arrest, inhibit DNA repair, induce apoptosis and acetylate non histone proteins causing downstream alterations in gene expression. HDACI are a diverse group of compounds, which vary in structure, biological activity, and specificity. In general, HDACIs contain a zinc-binding domain, a capping group, and a straight chain linker connecting the two. They are classified into four classes namely short chain fatty acids, hydroxamic acids, cyclic peptides and synthetic benzamides. This review describes the clinical utility of HDACI as monotherapy as well as combination therapy with other treatment modalities such as chemotherapy and radiotherapy. Adverse effects and shortcomings of treatment with HDACI are also discussed in detail. - Source: PubMed
Lakshmaiah K CJacob Linu AAparna SLokanatha DSaldanha Smitha C