HDAC
Histone deacetylases (HDACs) remove acetyl groups from lysine residues on histone and non-histone proteins, thereby regulating chromatin acetylation, gene transcription, and protein function[1]. Mechanistically, HDAC activity works opposite to histone acetyltransferases and controls chromatin conformation, with HDAC1/2 complexes also regulating histone crotonylation in vivo[2]. In disease research, altered HDAC expression or function is linked to cancer, neurological diseases, and immune disorders, making HDAC enzymes practical targets for cellular, animal, and translational models[3]. Compared with related isoforms, HDAC3 is distinguished by its dependence on SMRT/N-CoR corepressor complexes for enzymatic activity, whereas class II HDAC-associated deacetylase activity depends on multiprotein complexes containing HDAC3 and SMRT/N-CoR[4][5]. HDAC6 differs functionally because it localizes mainly in the cytoplasm, deacetylates α-tubulin, associates with microtubules, and regulates aggresome formation under misfolded-protein stress[6][7][8]. For experimental applications, HDAC inhibitors provide small-molecule tools to increase acetylation, induce p21-associated cell-cycle arrest, differentiation, or apoptosis, and interrogate isoform-selective HDAC biology in disease models[3][9][10].
References:
- [1]. Seto E, et al. Erasers of histone acetylation: the histone deacetylase enzymes. Cold Spring Harb Perspect Biol. 2014 Apr 1;6(4):a018713. [Content Brief]
- [2]. Kelly RDW, et al. Histone deacetylase (HDAC) 1 and 2 complexes regulate both histone acetylation and crotonylation in vivo. Sci Rep. 2018 Oct 2;8(1):14690. [Content Brief]
- [3]. Falkenberg KJ, et al. Histone deacetylases and their inhibitors in cancer, neurological diseases and immune disorders. Nat Rev Drug Discov. 2014 Sep;13(9):673-91. [Content Brief]
- [4]. Guenther MG, et al. The SMRT and N-CoR corepressors are activating cofactors for histone deacetylase 3. Mol Cell Biol. 2001 Sep;21(18):6091-101. [Content Brief]
- [5]. Fischle W, et al. Enzymatic activity associated with class II HDACs is dependent on a multiprotein complex containing HDAC3 and SMRT/N-CoR. Mol Cell. 2002 Jan;9(1):45-57. [Content Brief]
- [6]. Hubbert C, et al. HDAC6 is a microtubule-associated deacetylase. Nature. 2002 May 23;417(6887):455-8. [Content Brief]
- [7]. Zhang Y, et al. HDAC-6 interacts with and deacetylates tubulin and microtubules in vivo. EMBO J. 2003 Mar 3;22(5):1168-79. [Content Brief]
- [8]. Kawaguchi Y, et al. The deacetylase HDAC6 regulates aggresome formation and cell viability in response to misfolded protein stress. Cell. 2003 Dec 12;115(6):727-38. [Content Brief]
- [9]. Richon VM, et al. Histone deacetylase inhibitor selectively induces p21WAF1 expression and gene-associated histone acetylation. Proc Natl Acad Sci U S A. 2000 Aug 29;97(18):10014-9. [Content Brief]
- [10]. Delcuve GP, et al. Roles of histone deacetylases in epigenetic regulation: emerging paradigms from studies with inhibitors. Clin Epigenetics. 2012 Mar 12;4(1):5. [Content Brief]
All Product Categories
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HDAC Related Products (392)
Related Products (392)
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POI ligand-6-Linker Conjugate
0 ImagesCat. No.: HY-189509POI ligand-6-Linker Conjugate is a hydrophobic tag conjugate that binds to HDAC6. POI ligand-6-Linker Conjugate, as a target protein ligand-linker conjugate, is used to synthesize the hydrophobic tag degrader (Hyt) HDAC6 degrader-6 (HY-189299). POI ligand-6-Linker Conjugate is used in the study of leukemia.
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Pimelic Diphenylamide 106 analog
0 ImagesCat. No.: HY-19430CAS No.: 2070015-24-4Synonyms: RGFA-8 analog; TC-H 106 analogPimelic Diphenylamide 106 analog is the analog of Pimelic Diphenylamide 106, with unknown activity.
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Tinostamustine hydrochloride
0 ImagesCat. No.: HY-101780ACAS No.: 1793059-58-1Synonyms: EDO-S101 hydrochloride; NL-101 hydrochlorideTinostamustine hydrochloride (EDO-S101 hydrochloride) is a compound with anti-multiple myeloma activity and the ability to promote CD38 expression. Tinostamustine hydrochloride enhances the sensitivity of tumor cells to the anti-CD38 monoclonal antibody daratumumab by increasing the acetylation level of histone H3. Tinostamustine hydrochloride can increase the expression of MICA and MICB, thereby activating NK cells. Tinostamustine hydrochloride can significantly delay tumor growth and improve the survival rate of mice.
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HDAC6-IN-8
0 ImagesCat. No.: HY-147730CAS No.: 2796282-49-8A variety of compounds were designed and synthesized by modifying cap groups. The enzyme inhibition test showed that compound 12C had broad-spectrum enzyme inhibitory activity, and compounds 9m and 9q were more inclined to inhibit HDAC6, showing a certain selective inhibitory activity among the representative subtypes.
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Curcuphenol
0 ImagesCat. No.: HY-119505CAS No.: 69301-27-5Curcuphenol is a compound with histone deacetylase enhancing activity and has the activity of reversing immune escape. Curcuphenol can reverse the immune escape of tumors by restoring the expression of antigen presentation machinery. Its two synthetic analogs have histone deacetylase enhancing activity and play an important role in the immune recognition of metastatic tumors.
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Sodium butyrate (Standard)
0 ImagesCat. No.: HY-B0350ARCAS No.: 156-54-7Synonyms: Butanoic acid sodium (Standard); Butyric acid sodium (Standard)Sodium butyrate (Standard) is the analytical standard of Sodium butyrate (HY-B0350A). This product is intended for research and analytical applications. Sodium Butyrate (sodium butanoate) is an inhibitor of HDAC, possessing anti-tumor activity.
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Largazole thiol
0 ImagesCat. No.: HY-170890CAS No.: 1132667-11-8
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XP5
0 ImagesCat. No.: HY-115885CAS No.: 2760511-91-7XP5 is a potent, orally active HDAC6 inhibitor with an IC50 of 31 nM. XP5 displays high antiproliferative activity against various cancer cell lines including the HDACi-resistant YCC3/7 gastric cancer cells (IC50=0.16-2.31 μM). XP5 enhances antitumor immunity when combined with a PD-L1 inhibitor in melanoma.
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HDAC8-IN-12
0 ImagesCat. No.: HY-161954CAS No.: 3028095-13-5HDAC8-IN-12 (compound 5k) is a non-hydroxamic acid, selective inhibitor of HDAC8 (IC50: 0.12 nM) and a potent inhibitor of breast cancer. HDAC8-IN-12 triggers anti-tumor immunity by activating T cells, increasing the proportion of M1 macrophages and decreasing the proportion of M2 macrophages. HDAC8-IN-12 (50 mg/kg) exerts tumor suppressive effects in an orthotopic mouse model of breast cancer.
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Dihydrochlamydocin
0 ImagesCat. No.: HY-115761CAS No.: 52574-64-8Dihydrochlamydocin is a histone deacetylases (HDAC) inhibitor. Dihydrochlamydocin shows strong cytostatic activity towards mastocytoma cells.
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Romidepsin (GMP)
0 ImagesCat. No.: HY-15149GSynonyms: FK 228 (GMP); FR 901228 (GMP); NSC 630176 (GMP)Romidepsin (GMP) (FK 228 (GMP)) is Romidepsin (HY-15149) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Romidepsin (FK 228) is a Histone deacetylase (HDAC) inhibitor with anti-tumor activities. Romidepsin (FK 228) inhibits HDAC1, HDAC2, HDAC4, and HDAC6 with IC50s of 36 nM, 47 nM, 510 nM and 1.4 μM, respectively. Romidepsin (FK 228) is produced by Chromobacterium violaceum, induces cell G2/M phase arrest and apoptosis.
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Top/HDAC-IN-1
0 ImagesCat. No.: HY-145851CAS No.: 2775446-49-4Top/HDAC-IN-1 (Compound 29b) is a topoisomerase/HDAC dual inhibitor with IC50s of 18, 230, 790, 87, and 5250 nM for HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, respectively. Top/HDAC-IN-1 exhibits potent antitumor activities against the HCT116 cell line with the IC50 of 180 nM. Top/HDAC-IN-1 efficiently induces apoptosis with G2 cell cycle arrest in HCT116 cells.
