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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Tubastatin A (Standard)
0 ImagesTubastatin A (Standard) is the analytical standard of Tubastatin A. This product is intended for research and analytical applications. Tubastatin A is a potent and selective HDAC6 inhibitor with an 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 also inhibits HDAC10 and metallo-β-lactamase domain-containing protein 2 (MBLAC2).
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JNJ-16241199 (Standard)
0 ImagesCat. No.: HY-10226RCAS No.: 604769-01-9Synonyms: R306465 (Standard)JNJ-16241199 (Standard) is the analytical standard of JNJ-16241199 (HY-10226). This product is intended for research and analytical applications. JNJ-16241199 (R306465) is an orally active, selectivehydroxamate-based histone deacetylase (HDAC) inhibitor, with theIC50of 3.3 nM and 23 nM for HDAC1and HDAC8, respectively.JNJ-16241199induces histone 3 acetylation and strongly increases the expression of p21waf1, cip1 in A2780 ovarian carcinoma cells.JNJ-16241199 inducescell apoptosisand shows anticancer activityin a broad spectrum of human malignancies. JNJ-16241199 can be used for cancer study.
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CUDC-101 (Standard)
0 ImagesCat. No.: HY-10223RCAS No.: 1012054-59-9CUDC-101 (Standard) is the analytical standard of CUDC-101 (HY-10223). This product is intended for research and analytical applications. CUDC-101 is a potent inhibitor of HDAC, EGFR, and HER2 with IC50s of 4.4, 2.4, and 15.7 nM, respectively. CUDC-101 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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Martinostat
0 ImagesCat. No.: HY-160092CAS No.: 1629052-58-9Martinostat is a HDAC inhibitor and can be labeled with radionuclides for quantitative imaging of HDACs in vivo in the central nervous system and major peripheral organs.
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Pracinostat (Standard)
0 ImagesSynonyms: SB939 (Standard)Pracinostat (Standard) is the analytical standard of Pracinostat. This product is intended for research and analytical applications. Pracinostat is a potent histone deacetylase (HDAC) inhibitor, with IC50s of 40-140 nM, used for cancer research. Pracinostat also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2) hydrolase activity with an EC50 below 10 nM.
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Abexinostat (Standard)
0 ImagesCat. No.: HY-10990RCAS No.: 783355-60-2Synonyms: CRA 024781 (Standard); PCI-24781 (Standard)Abexinostat (Standard) is the analytical standard of Abexinostat (HY-10990). This product is intended for research and analytical applications. Abexinostat (CRA 024781) is a novel pan-HDAC inhibitor mostly targeting HDAC1 with Ki of 7 nM. Abexinostat also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2) hydrolase activity with an EC50 below 10 nM.
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HDAC-IN-2
0 ImagesCat. No.: HY-115585CAS No.: 1026295-98-6
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4-Phenylbutyric acid (Standard)
0 Images4-Phenylbutyric acid (Standard) is the analytical standard of 4-Phenylbutyric acid (HY-A0281). This product is intended for research and analytical applications. 4-Phenylbutyric acid (4-PBA) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research.
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YF438
0 ImagesCat. No.: HY-164550CAS No.: 2247210-09-7YF438 is an HDAC inhibitor with effective anticancer activity both in vitro and in vivo. YF438 inhibits the growth and metastasis of triple-negative breast cancer (TNBC) cells by blocking the interaction between HDAC and MDM2, inducing the dissociation of MDM2-MDMX, and promoting the degradation of MDM2.
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KBH-A42
0 ImagesCat. No.: HY-126211CAS No.: 798543-50-7KBH-A42 is a novel histone deacetylase (HDAC) inhibitor with significant anti-inflammatory properties. KBH-A42 against TNF-α and NO production with IC50 values of 1.10 and 2.71 µM, respectively, in the LPS-induced murine macrophage RAW 264.7 cells.
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Tucidinostat (Standard)
0 ImagesSynonyms: Chidamide (Standard); HBI-8000 (Standard); CS 055 (Standard)Tucidinostat (Standard) is the analytical standard of Tucidinostat. This product is intended for research and analytical applications. Tucidinostat (Chidamide) is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, less active on HDAC8 and HDAC11 (IC50s, 733 nM, 432 nM, respectively), and shows no effect on HDAC4/5/6/7/9.
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Romidepsin-d7
0 ImagesCat. No.: HY-15149S2Synonyms: FK 228-d7; FR 901228-d7; NSC 630176-d7Romidepsin-d7 (FK 228-d7) is deuterium labeled Romidepsin. 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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HDAC8-IN-1 (Standard)
0 ImagesCat. No.: HY-111342RCAS No.: 1417997-93-3HDAC8-IN-1 (Standard) is the analytical standard of HDAC8-IN-1 (HY-111342). This product is intended for research and analytical applications. HDAC8-IN-1 is a HDAC8 inhibitor with an IC50 of 27.2 nM.
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Nampt-IN-3 (Standard)
0 ImagesCat. No.: HY-108701RCAS No.: 2121591-52-2Nampt-IN-3 (Standard) is the analytical standard of Nampt-IN-3 (HY-108701). This product is intended for research and analytical applications. Nampt-IN-3 (Compound 35) simultaneously inhibit nicotinamide phosphoribosyltransferase (NAMPT) and HDAC with IC50s of 31 nM and 55 nM, respectively. Nampt-IN-3 effectively induces cell apoptosis and autophagy and ultimately leads to cell death.
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Zabadinostat (Standard)
0 ImagesSynonyms: CXD101 (Standard)Zabadinostat (Standard) is the analytical standard of Zabadinostat (HY-100748). This product is intended for research and analytical applications. Zabadinostat (CXD101) is a potent, selective and orally active class I HDAC inhibitor with IC50s of 63 nM, 570 nM and 550 nM for HDAC1, HDAC2 and HDAC3, respectively. Zabadinostat has no activity against HDAC class II. Zabadinostat has antitumor activity.
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BRD4097
0 ImagesCat. No.: HY-121315CAS No.: 1550053-19-4BRD4097 is an inhibitor of histone deacetylase (HDAC). BRD4097 acts by inhibiting the activity of HDACs, especially HDAC 1,2 and 3, through metal chelation and spatial rejection mechanisms, and this inhibition may help regulate gene expression and alter chromatin structure, thereby affecting a variety of biological processes. BRD4097 is used to study the role of HDAC in cholesterol metabolism and NPC1 diseases.
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Tacedinaline (Standard)
0 ImagesSynonyms: N-acetyldinaline (Standard); CI-994 (Standard); Goe-5549 (Standard)Tacedinaline (Standard) is the analytical standard of Tacedinaline. This product is intended for research and analytical applications. Tacedinaline (N-acetyldinaline) is an inhibitor of the histone deacetylase (HDAC) with IC50s of 0.9, 0.9, 1.2 μM for recombinant HDAC 1, 2 and 3 respectively.
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(Rac)-Nanatinostat
0 ImagesCat. No.: HY-124559CAS No.: 914937-68-1Synonyms: (Rac)-CHR-3996(Rac)-Nanatinostat ((Rac)-CHR-3996, example 44) is a potent HDAC inhibitor with an IC50 of <330 nM. (Rac)-Nanatinostat has anticancer effects and can effectively inhibit the cell growth of HeLa, U937 and HUT cells.
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Tubacin (Standard)
0 ImagesCat. No.: HY-13428RCAS No.: 537049-40-4Tubacin (Standard) is the analytical standard of Tubacin. This product is intended for research and analytical applications. Tubacin is a potent and selective inhibitor of HDAC6, with an IC50 value of 4 nM and approximately 350-fold selectivity over HDAC1. Tubacin also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2).
