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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IHCH-3064
0 ImagesCat. No.: HY-145406CAS No.: 2420562-65-6IHCH-3064 is a dual-acting compounds targeting Adenosine A2A Receptor and HDAC. IHCH-3064 exhibits potent binding to A2AR (Ki=2.2 nM) and selective inhibition of HDAC1 (IC50=80.2 nM), with good antiproliferative activity against tumor cell lines in vitro. IHCH-3064 is a tumor immunotherapeutic agent.
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NT376
0 ImagesCat. No.: HY-163806CAS No.: 2820208-97-5NT376 is a high potency and selectivity inhibitor of class-IIa Histone deacetylases (HDAC) with an IC50 value of 32 nM, similar to NT160 (HY-149285) (IC50= 46 nM) in HT-29 cells. NT376 is proming for research of various cancers and in the diseases of the central nervous system (CNS) such as Alzheimer’s and Huntington’s diseases.
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WMJ-J-09
0 ImagesWMJ-J-09 is an HDAC inhibitor with IC50 values of 7.5 nM (HDAC1), 21.3 nM (HDAC2), 18.4 nM (HDAC3), 90.9 nM (HDAC8), 3.9 nM (HDAC6) and 8715.7 nM (HDAC4). WMJ-J-09 blocks the cell cycle and induces apoptosis in cancer cells. WMJ-J-09 induces cancer cell death through the LKB1-AMPK-p38MAPK-p63-survivin signaling cascade.WMJ-J-09 inhibits HDAC enzyme activity, leading to acetylation of key proteins and thereby regulating cancer cell death. WMJ-J-09 can be used in HCT116 cells and FaDu cells research[1][2].
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HDAC-IN-62
0 ImagesCat. No.: HY-155182HDAC-IN-62 (Compound 5) a HDAC inhibitor, with IC50s of 0.78, 1.0, 1.2? μM for HDAC6/8/11 respectively. HDAC-IN-62 inhibits-induced microglial activation by the initiation of autophagy, and inhibits nitric oxide production. HDAC-IN-62 has anti-inflammatory and anti-depressant effects. HDAC-IN-62 inhibits microglial activation in mouse brain.
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4-Iodo-SAHA
0 ImagesSynonyms: ISAHA
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HDAC-IN-26
0 ImagesCat. No.: HY-145350CAS No.: 2410542-97-9HDAC-IN-26 is a highly selective class I HDAC inhibitor with an EC50 value of 4.7 nM.
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BChE/HDAC6-IN-1
0 ImagesCat. No.: HY-149417CAS No.: 2925457-27-6BChE/HDAC6-IN-1 is a potent and selective dual BChE/HDAC6 inhibitor with IC50 values of 4 and 8.9 nM, respectively. BChE/HDAC6-IN-1 ameliorates the cognitive impairment in an Aβ1–42-induced mouse model and has the potental for AD research.
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JMJD3/HDAC-IN-1
0 ImagesCat. No.: HY-156094CAS No.: 2883046-06-6JMJD3/HDAC-IN-1 (compound A5b) is a dual inhibitor targeting Jumonji domain-containing protein demethylase 3 (JMJD3) and histone deacetylase (HDAC1, IC50=16 nM). JMJD3/HDAC-IN-1 promotes hypermethylation of histone H3K27 and hyperacetylation of H3K9, and also cleaves caspase-7 and PARP to induce apoptosis. JMJD3/HDAC-IN-1 effectively inhibits cancer cell cloning, migration, and invasion.
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Top/HDAC-IN-3
0 ImagesCat. No.: HY-159966CAS No.: 3059615-90-3Top/HDAC-IN-3 (Compound 31) is an orally active dual inhibitor of Topoisomerase and HDAC. Top/HDAC-IN-3 increases reactive oxygen species (ROS) levels, leading to DNA damage, thereby inhibiting cancer cell colony formation and migration, inducing cancer cell Apoptosis, and causing cell cycle arrest. In the NSCLC model, Top/HDAC-IN-3 exhibited significant antitumor effects, with a tumor growth inhibition (TGI) of 77.5% at 100 mg/kg, surpassing the efficacy of the HDAC inhibitor SAHA (HY-10221) and the combination of SAHA (HY-10221) with the topoisomerase inhibitor Irinotecan (HY-16562).
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HDAC-IN-20
0 ImagesCat. No.: HY-116465CAS No.: 1238944-56-3
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ZMF-23
0 ImagesCat. No.: HY-155179Purity: 99.83%ZMF-23 is a PAK1/HDAC6 dual inhibitor. ZMF-23 inhibits PAK1 and HDAC6 regulated aerobic glycolysis and migration. ZMF-23 induces TNF-α-regulated necroptosis, and further enhances apoptosis. ZMF-23 inhibits the Warburg effect and cell migration. ZMF-23 can be used for research of triple-negative breast cancer (TNBC).
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2-Propylpent-4-ynoic acid
0 ImagesCat. No.: HY-W787758CAS No.: 24102-11-2Synonyms: 4-yn-VPA2-Propylpent-4-ynoic acid (4-yn-VPA) is a HDAC inhibitor (with an IC50 of 0.5 mM against human HDAC). 2-Propylpent-4-ynoic acid also induces P-glycoprotein function, and exhibits teratogenicity, fetal growth inhibition and neurotoxicity. 2-Propylpent-4-ynoic acid shows significant stereospecific teratogenic effects, with the S-enantiomer being more teratogenic than the R-enantiomer and other analogs. The neurotoxicity of 2-Propylpent-4-ynoic acid is independent of its stereochemical structure. 2-Propylpent-4-ynoic acid has been used in studies related to the pathogenesis of colon cancer and neural tube defects such as exencephaly.
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HDAC6-IN-22
0 ImagesCat. No.: HY-156279HDAC6-IN-22 (compound 30) is a inhibitor of HDAC6, with the IC50 of 4.63 nM. HDAC6-IN-22 has antiproliferative effects in vitro and in vivo towards multiple myeloma. HDAC6-IN-22 induces cell cycle arrest in the G2 phase and promotes apoptosis through the mitochondrial pathway.
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YF479
0 ImagesCat. No.: HY-120046CAS No.: 1803281-22-2YF479 is a potent inhibitor of histone deacetylase. YF479 abates cell viability, suppresses colony formation and tumor cell motility. YF479 significantly inhibits breast tumor growth and metastasis. YF479 has the potential for the research of clinical trials for breast cancer.
