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 (393)
Related Products (393)
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H8-A5
0 ImagesCat. No.: HY-117093CAS No.: 423731-10-6H8-A5 is a novel human histone deacetylase 8 (HDAC8) inhibitor. A highly specific ZBG-based pharmacophore model was developed by incorporating a custom zinc-binding group (ZBG) feature. Pharmacophore-based virtual screening identified three novel HDAC8 inhibitors with low micromolar IC50 values (1.8-1.9 μM). Further studies showed that H8-A5 was more selective for HDAC8 than HDAC1/4 and exhibited antiproliferative activity in MDA-MB-231 cancer cells. Molecular docking and molecular dynamics studies showed that H8-A5 could bind to HDAC8, providing a good starting point for the development of HDAC8 inhibitors for cancer treatment.
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HDAC6-IN-37
0 ImagesCat. No.: HY-158030CAS No.: 2986486-82-0HDAC6-IN-37 (compound W5) is an inhibitor of HDAC6 and has neuroprotective effects. HDAC6-IN-37 can restore the morphology of hippocampal neurons, reduce the expression of Aβ, Tau, and p-Tau proteins in the hippocampus of AD rats, and inhibit the formation of senile plaques and neurofibrillary tangles. Thus, HDAC6-IN-37 improves the Aβ/Cu2+-induced AD model in rats, regulates oxidative stress status, and balances neurotransmitter disorders in brain tissue.
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HDAC-IN-61
0 ImagesCat. No.: HY-155695HDAC-IN-61 (compound 12k) is a potent and orally active HDAC inhibitor. HDAC-IN-61 has anticancer active with an IC50 value of 30 nM for Bel-7402 cell. HDAC-IN-61 can be used in research of cancer.
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W2A-28
0 ImagesCat. No.: HY-184177CAS No.: 2803203-72-5W2A-28 is a daul modulator of class I HDACs and Wnt/β-catenin. W2A-28 inhibits HDAC1, 2 and 3 activities with IC50 values of 512, 675, and 217 nM, respectively. W2A-28 shows selectivity over other HDACs and Sirtuin family members. W2A-28 activates Wnt/β-catenin signaling via reduced LRP6 degradation, enhances histone acetylation, suppresses tau phosphorylation, and reduces Aβ40 and Aβ42 levels. W2A-28 can be used for the research of Alzheimer's disease.
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PARP7/HDACs-IN-1
0 ImagesCat. No.: HY-162349CAS No.: 3030144-11-4PARP7/HDACs-IN-1 (compound 9l) is a dual-target inhibitor targeting PARP7/HDAC with anti-tumor activity. PARP7/HDACs-IN-1 inhibits different subtypes of PARPs and HDACs with IC50s of 83.3 nM (PARP1), 3.1 nM (PARP7), 35 nM (HDAC1), 30.3 nM (HDAC2), 35.4 nM (HDAC3), and 6.4 nM respectively. (HDAC6). br/.
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HDAC-IN-102
0 ImagesCat. No.: HY-185554CAS No.: 626200-64-4HDAC-IN-102 (Compound 21) is a histone deacetylase (HDAC) inhibitor with an IC50 of 58 μM. HDAC-IN-102 inhibits total HDAC activity and exhibits partial subtype selectivity, with the R-isomer targeting HDAC2 and the S-isomer targeting HDAC8. HDAC-IN-102 exerts antioxidant effects by scavenging DPPH free radicals. HDAC-IN-102 can be used in cancer-related research.
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WJ35435
0 ImagesCat. No.: HY-117688CAS No.: 1620054-84-3WJ35435 is a dual-targeted anticancer hybrid that induces anti-HDAC (in particular HDAC1 and HDAC6) and anti-topoisomerase I activities that causes DNA damage associated with a low DNA repair capability and induces cell cycle arrest at G1- and G2-phase to apoptosis. WJ35435 induces histone H3 acetylation and phosphorylation, α-tubulin acetylation and γ-H2AX formation to achieve anti-HDAC effect. WJ35435 is promising for research of cancer.
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Theophylline-13C2,d6
0 ImagesCat. No.: HY-143683SCAS No.: 1782458-84-7Synonyms: 1,3-Dimethylxanthine-13C2,d6; Theo-24-13C2,d6Theophylline-13C2,d6 (1,3-Dimethylxanthine-13C2,d6) is the deuterium labeled and 13C-labeled Theophylline (HY-B0809). Theophylline (1,3-Dimethylxanthine) is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) induces apoptosis. Theophylline (1,3-Dimethylxanthine) can be used for asthma and chronic obstructive pulmonary disease (COPD) research.
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HDAC-IN-29
0 ImagesCat. No.: HY-144102CAS No.: 2695593-95-2HDAC-IN-29 (compound 13b) is a potent pan-HDAC inhibitor. HDAC-IN-29 shows antitumor activity.
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MFDCH016
0 ImagesCat. No.: HY-178350MFDCH016 is a potent HDAC1/6 (IC50 = 38/59 nM) and CDK4/6 (IC50 = 680/720 nM) inhibitor. MFDCH016 induces apoptosis and cell cycle arrest in G2/M and G0/G1 phases in MCF-7 cells. MFDCH016 can modulate the HDAC-p21-CDK signaling pathway, increasing the levels of acetylated H3 and p21. MFDCH016 can be used for the study of breast cancer.
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JAK/HDAC-IN-4
0 ImagesCat. No.: HY-169290CAS No.: 3064994-08-4JAK/HDAC-IN-4 (compound 11 i) is a JAK/HDAC inhibitor with the IC50 values of 0.49 nM and 12 nM for JAK2 and HDAC6, respectively. JAK/HDAC-IN-4 inhibits the cell proliferation and the production of nitric oxide. JAK/HDAC-IN-4 ameliorates psoriasis-like skin lesions in an Imiquimod (HY-B0180)-induced murine model with low toxicity.
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LW479
0 ImagesCat. No.: HY-135606CAS No.: 1688677-89-5
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BChE/HDAC6-IN-2
0 ImagesCat. No.: HY-149418CAS No.: 2925457-33-4BChE/HDAC6-IN-2 (compound 29a) is a dual inhibitor of BChE and HDAC6 with IC50s of 1.8 nM and 71.0 nM, respectively. BChE/HDAC6-IN-2 has prominently neuroprotective effects and reactive oxygen species (ROS) scavenging activity. BChE/HDAC6-IN-2 is also an effective chelator of metal ion (Fe2+ and Cu2+). BChE/HDAC6-IN-2 inhibits phosphorylation of tau, and exhibits moderate immunomodulatory effect.
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CDK/HDAC-IN-4
0 ImagesCat. No.: HY-169075CDK/HDAC-IN-4 is a high selective dual cyclin-dependent kinase (CDK)/histone deacetylase (HDAC) inhibitor with IC50 values of 88.4 and 168.9 nM, respectively. CDK/HDAC-IN-4 exhibits antiproliferative capacities against hematological and solid tumor cells. CDK/HDAC-IN-4 also induces MV-4-11 cell Apoptosis and S cell cycle arrests. CDK/HDAC-IN-4 possesses a significant antitumor potency in the MV-4-11 xenograft model.
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HDAC/CD13-IN-1
0 ImagesCat. No.: HY-156016HDAC/CD13-IN-1 (Compound 12) is a HDAC/CD13 inhibitor (IC50: 0.34 μM for hCD13, 0.53 μM for porcine CD13, 0.03, 0.06, 0.02 μM for HDAC1/2/3). HDAC/CD13-IN-1 inhibits MV4-11, K562, Jeko-1, and HL60 cell proliferation (IC50: 0.25-2.04 μM). HDAC/CD13-IN-1 induces cancer cell apoptosis. HDAC/CD13-IN-1 has anti-metastasis and anti-invasion efficacy.
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HDAC6-IN-12
0 ImagesCat. No.: HY-150722CAS No.: 2803866-44-4HDAC6-IN-12 (compound GZ) is a potent HDAC6 inhibitor. HDAC6-IN-12 has anticancer activity through merges into DNA strands causing DNA damage. HDAC6-IN-12 can be used for cancer research.
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Tubastatin A (GMP)
0 ImagesCat. No.: HY-13271AGCAS No.: 1252003-15-8Tubastatin A (GMP) is the Tubastatin A (HY-13271A) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. 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).
