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 (391)
Related Products (391)
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Givinostat hydrochloride monohydrate (Standard)
0 ImagesSynonyms: ITF-2357 hydrochloride monohydrate (Standard)Givinostat (hydrochloride monohydrate) (Standard) is the analytical standard of Givinostat (hydrochloride monohydrate). This product is intended for research and analytical applications. Givinostat hydrochloride monohydrate (ITF-2357 hydrochloride monohydrate) is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively.
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Entinostat (Standard)
0 ImagesCat. No.: HY-12163RCAS No.: 209783-80-2Synonyms: MS-275 (Standard); SNDX-275 (Standard)Entinostat (Standard) is the analytical standard of Entinostat (HY-12163). This product is intended for research and analytical applications. Entinostat is an oral and selective class I HDAC inhibitor, with IC50s of 243 nM, 453 nM, and 248 nM for HDAC1, HDAC2, and HDAC3, respectively.
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Remetinostat (Standard)
0 ImagesCat. No.: HY-100365RCAS No.: 946150-57-8Synonyms: SHP-141 (Standard)Remetinostat (Standard) is the analytical standard of Remetinostat (HY-100365). This product is intended for research and analytical applications. Remetinostat (SHP-141) is a hydroxamic acid-based histone deacetylase (HDAC) inhibitor. Remetinostat alleviates Imiquimod (HY-B0180)-induced psoriatic dermatitis. Remetinostat can be used for study of cutaneous T-cell lymphoma.
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ST7612AA1
0 ImagesCat. No.: HY-12926CAS No.: 1428535-92-5ST7612AA1 is a histone deacetylase (HDAC) inhibitor that controls chromatin condensation and DNA transcription by removing acetyl groups from histones. ST7612AA1 is also a potent HIV reactivation inducer, and its reactivation activity is exerted without activating or proliferating CD4+T cells, and can be used in the study of HIV reactivation strategies and elimination of viral reservoirs.
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Z-MAL
0 ImagesCat. No.: HY-176545CAS No.: 642463-22-7
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Butyrylhydroxamic acid
0 ImagesButyrylhydroxamic acid (N-Hydroxybutanamide) is a potent inhibitor of histone deacetylase (HDAC). Butyrylhydroxamic acid enhances memory in behavioral models of rodents and can be used as memory enhancers, mood stabilizers, and β-chain hemoglobin disease studies.
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J1038
0 ImagesCat. No.: HY-111028CAS No.: 949727-86-0Synonyms: T 5979345
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WT-161 (Standard)
0 ImagesCat. No.: HY-100871RCAS No.: 1206731-57-8WT-161 (Standard) is the analytical standard of WT-161 (HY-100871). This product is intended for research and analytical applications. WT-161 is a potent and selective HDAC6 inhibitor with an IC50 of 0.40 nM. WT-161 also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2).
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ACY-957 (Standard)
0 ImagesCat. No.: HY-104008RCAS No.: 1609389-52-7ACY-957 (Standard) is the analytical standard of ACY-957 (HY-104008). This product is intended for research and analytical applications. ACY-957 is an orally active and selective inhibitor of HDAC1 and HDAC2, with IC50s of 7 nM, 18 nM, and 1300 nM against HDAC1/2/3, respectively, and shows no inhibition on HDAC4/5/6/7/8/9.
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Givinostat (Standard)
0 ImagesSynonyms: ITF-2357 (Standard)Givinostat (Standard) is the analytical standard of Givinostat. This product is intended for research and analytical applications. Givinostat (ITF-2357) is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively. Givinostat can be used for Duchenne muscular dystrophy (DMD) research.
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CAY10603 (Standard)
0 ImagesCat. No.: HY-18613RCAS No.: 1045792-66-2Synonyms: BML-281 (Standard)CAY10603 (Standard) is the analytical standard of CAY10603. This product is intended for research and analytical applications. CAY10603 (BML-281) is a potent and selective HDAC6 inhibitor, with an IC50 of 2 pM; CAY10603 (BML-281) also inhibits HDAC1, HDAC2, HDAC3, HDAC8, HDAC10, with IC50s of 271, 252, 0.42, 6851, 90.7 nM.
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SR-4370 (Standard)
0 ImagesCat. No.: HY-111400RCAS No.: 1816294-67-3
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Ricolinostat (Standard)
0 ImagesSynonyms: ACY-1215 (Standard); Rocilinostat (Standard)Ricolinostat (Standard) is the analytical standard of Ricolinostat. This product is intended for research and analytical applications. Ricolinostat (ACY-1215) is a potent and selective HDAC6 inhibitor, with an IC50 of 5 nM. ACY-1215 also inhibits HDAC1, HDAC2, and HDAC3 with IC50s of 58, 48, and 51 nM, respectively.
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Tefinostat (Standard)
0 ImagesSynonyms: CHR-2845 (Standard)Tefinostat (Standard) is the analytical standard of Tefinostat (HY-106409). This product is intended for research and analytical applications. Tefinostat (CHR-2845) is a monocyte/macrophage targeted histone deacetylase (HDAC) inhibitor. Tefinostat can be cleaved into active acid CHR-2847 by the intracellular esterase human carboxylesterase-1 (hCE-1). Tefinostat can be used for the research of leukaemias.
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HDAC-IN-83
0 ImagesCat. No.: HY-169923HDAC-IN-83 (compound 9D) is an inhibitor of deacetylases (HDACs) (IC50=0.01 μM/0.44 μM HDAC1/HDAC6) with anticancer, antiproliferative and caspase 3/7 activation activities. HDAC-IN-83 inhibits Cal27, HepG2 and MRC-5 with IC50s of 0.693 μM, 0.427 μM and 3.19 μM, respectively.
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Tubastatin A Hydrochloride (Standard)
0 ImagesCat. No.: HY-13271RCAS No.: 1310693-92-5Synonyms: Tubastatin A HCl (Standard); TSA HCl (Standard)Tubastatin A (Hydrochloride) (Standard) is the analytical standard of Tubastatin A (Hydrochloride). This product is intended for research and analytical applications. Tubastatin A Hydrochloride (Tubastatin A HCl) is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more). Tubastatin A Hydrochloride also inhibits HDAC10 and metallo-β-lactamase domain-containing protein 2 (MBLAC2).
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FFK29
0 ImagesCat. No.: HY-180343CAS No.: 1795429-46-7FFK29 is a synthetic class II histone deacetylase inhibitor (HDACi). FFK29 can potently inhibit the growth and encystation of Acanthamoeba. FFK29 can be studied in research on protozoan and parasitic diseases.
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Diheteropeptin
0 ImagesCat. No.: HY-N14950CAS No.: 202869-98-5Diheteropeptin has similar activity to T ransforming growth factor-β, and inhibits the ability of HDAC.
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Corin (Standard)
0 ImagesCat. No.: HY-111048RCAS No.: 1808113-09-8Corin (Standard) is the analytical standard of Corin (HY-111048). This product is intended for research and analytical applications. Corin is a dual inhibitor of histone lysine specific demethylase (LSD1) and histone deacetylase (HDAC), with a Ki(inact) of 110 nM for LSD1 and an IC50 of 147 nM for HDAC1.
