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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(E/Z)-Dacinostat
0 ImagesCat. No.: HY-116619CAS No.: 591207-53-3Synonyms: (E/Z)-NVP-LAQ824; (E/Z)-LAQ824(E/Z)-Dacinostat ((E/Z)-NVP-LAQ824) is a histone deacetylase inhibitor that has the ability to induce apoptosis and enhance the activity of fludarabine in killing leukemia cells. (E/Z)-Dacinostat can trigger the production of reactive oxygen species (ROS) and DNA damage, enhance the killing effect of fludarabine on leukemia cells, and induce apoptosis. Its mechanism is related to the regulation of DNA repair processes and intracellular signaling pathways.
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FITC-SAHA
0 ImagesCat. No.: HY-164816CAS No.: 1160823-10-8FITC-SAHA is SAHA (HY-10221) conjugated with fluorescein. SAHA is an inhibitor of histone deacetylase (HDAC). FITC-SAHA can be used in cancer and Alzheimer's disease related research.
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SK-7041
0 ImagesCat. No.: HY-121512CAS No.: 617690-98-9
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HDAC1-IN-4
0 ImagesCat. No.: HY-144298CAS No.: 2482998-39-8HDAC1-IN-4 (JX34) is a potent Plasmodium falciparum HDAC1 inhibitor shows antimalarial activity (IC50 < 5 nM) and lower cytotoxicity.
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HDAC3/BRD4-IN-1
0 ImagesCat. No.: HY-170841HDAC3/BRD4-IN-1 (compound 26n) is an inhibitor of HDAC3/BRD4 with an IC50 of 8 nM for HDAC3 (IC50s are 220 nM and 120 nM for HDAC1 and HDAC2, respectively). HDAC3/BRD4-IN-1 has anti-tumor and anti-proliferative effects by upregulating Ac-H3 and downregulating c-Myc. The half-life of HDAC3/BRD4-IN-1 in human liver microsomes is 29.36 min.
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Estrogen receptor β/HDAC probe 1
0 ImagesCat. No.: HY-D2280CAS No.: 3057270-84-2Estrogen receptor β/HDAC probe 1 (compound P1) is a near-infrared fluorescent probe that dual-targets the estrogen receptor (Estrogen Receptor/ERR) β/histone deacetylase HDAC.
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Belinostat-d5
0 ImagesCat. No.: HY-10225SCAS No.: 2130852-65-0Synonyms: PXD101-d5; PX105684-d5Belinostat-d5 (PXD101-d5) is the deuterium labeled Belinostat (HY-10225). Belinostat (PXD101; PX105684) is a potent HDAC inhibitor with an IC50 of 27 nM in HeLa cell extracts.
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YKL-05-093
0 ImagesCat. No.: HY-101149CAS No.: 2172616-44-1YKL-05-093 is a salt-induced kinase (SIK) inhibitor (SIK2: Kd = 7.1 nM). YKL-05-093 reduces the phosphorylation level of HDAC4/5/CRTC2, inhibits SOST expression, and stimulates RANKL expression in vitro and in vivo. YKL-05-093 can be used in research on bone diseases.
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PySAHA
0 ImagesCat. No.: HY-174854PySAHA is a multifunctional HDAC inhibitor. PySAHA can degrade intracellular HDAC via a hydrophobic tagging mechanism. PySAHA also possesses photodynamic therapeutic activity and can generate reactive oxygen species under light irradiation. PySAHA can inhibit the proliferation, migration and induce cell apoptosis of breast cancer cells. PySAHA has antitumor activity and can be used in breast cancer research.
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HDAC6-IN-30
0 ImagesCat. No.: HY-157436HDAC6-IN-30 (compound 8g) is a selective HDAC6 inhibitor with the IC50 21 nM, and increase cell protein acetylation levels.
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LTK-14A
0 ImagesCat. No.: HY-160461CAS No.: 71118-00-8LTK-14A, a derivative of Garcinol (HY-107569), is an orally effective selective inhibitor of histone butyrylation. LTK-14A selectively inhibits butyrylation without affecting acetylation by interacting with the C1438 residue in the catalytic domain of p300. LTK-14A significantly inhibits H4K5 butyrylation in vitro and downregulates the expression of adipogenic genes, thereby blocking adipogenesis. LTK-14A inhibits body weight gain and reduces body weight in obese mice. LTK-14A can be used in obesity-related research.
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HDAC-IN-32
0 ImagesCat. No.: HY-145687CAS No.: 2766688-17-7
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HDAC/NAMPT-IN-1
0 ImagesCat. No.: HY-162124CAS No.: 2898381-63-8
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HDAC-IN-77
0 ImagesCat. No.: HY-169014HDAC-IN-77 (HL-5s) is an HDAC inhibitor. HDAC-IN-77 can induce ferroptosis and inhibit the Nrf2/HO-1 signaling pathway. HDAC-IN-77 can be used in cancer research.
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HDAC-IN-85
0 ImagesCat. No.: HY-170907HDAC-IN-85 (Compound 1) is a BBB-permeable HDAC inhibitor. HDAC-IN-85 has an inhibitory effect on brain tumor cell lines. HDAC-IN-85 can induce acetylation, leading to DNA double-strand breaks, and induce the ubiquitination of RAD51, disrupting the DNA repair process. HDAC-IN-85 can be used in the research of glioblastoma.
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Theophylline-d3
0 ImagesCat. No.: HY-B0809S1CAS No.: 65566-68-9Synonyms: 1,3-Dimethylxanthine-d3; Theo-24-d3Theophylline-d3 is deuterated 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.
