HDAC6
HDAC6 (histone deacetylase 6) is a unique class IIb histone deacetylase that localizes predominantly in the cytoplasm and preferentially targets non-histone substrates rather than chromatin-associated proteins[1][2]. HDAC6 regulates fundamental cellular functions through deacetylation of α-tubulin, Hsp90, and ubiquitin-associated protein complexes, thereby controlling microtubule dynamics, protein trafficking, stress responses, and protein quality-control mechanisms[2][3][4]. Mechanistically, HDAC6 functions at the intersection of the ubiquitin-proteasome system and autophagy-related pathways, where its ubiquitin-binding capability facilitates the processing and clearance of misfolded or aggregated proteins[3][4]. Therefore, HDAC6 has emerged as an important regulator of cellular proteostasis and cytoskeletal remodeling in both physiological and pathological contexts[2][3]. In disease models, HDAC6 has been implicated in cancer progression, neurodegenerative disorders, and inflammatory conditions through its effects on cell motility, intracellular transport, protein aggregation, and stress signaling pathways[2][4][5]. Increased HDAC6 activity promotes α-tubulin deacetylation and influences processes associated with tumor cell migration and metastasis, while modulation of HDAC6 activity alters axonal transport and protein aggregate handling in neurodegenerative disease models[4][5]. Compared with related HDAC isoforms, HDAC6 is distinguished by its predominantly cytoplasmic localization, preference for non-histone substrates, dual catalytic domains, and zinc-finger ubiquitin-binding domain, features that confer specialized biological functions not shared by most nuclear HDAC family members[2][5]. For experimental applications, HDAC6-selective inhibitors have become widely used chemical probes because they enable investigation of HDAC6-dependent signaling and protein homeostasis pathways while potentially reducing the off-target effects associated with pan-HDAC inhibition[3][6].
References:
- [1]. Park SY, et al. A short guide to histone deacetylases including recent progress on class II enzymes. Exp Mol Med. 2020 Feb;52(2):204-212. [Content Brief]
- [2]. Simões-Pires C, et al. HDAC6 as a target for neurodegenerative diseases: what makes it different from the other HDACs? Mol Neurodegener. 2013 Jan 29;8:7. doi: 10.1186/1750-1326-8-7. PMID: 23356410; PMCID: PMC3615964. [Content Brief]
- [3]. Brindisi M, et al. Old but Gold: Tracking the New Guise of Histone Deacetylase 6 (HDAC6) Enzyme as a Biomarker and Therapeutic Target in Rare Diseases. J Med Chem. 2020 Jan 9;63(1):23-39. [Content Brief]
- [4]. HDAC6 gene information from NCBI.
- [5]. Li G, et al. HDAC6 α-tubulin deacetylase: a potential therapeutic target in neurodegenerative diseases. J Neurol Sci. 2011 May 15;304(1-2):1-8. [Content Brief]
- [6]. Zhang Y, et al. Tanshinone IIA sodium sulfonate facilitates endocytic HMGB1 uptake. Biochem Pharmacol. 2012 Dec 1;84(11):1492-500. [Content Brief]
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HDAC6 Related Products (326)
Related Products (326)
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Antibodies (2)
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HDAC6-IN-43
0 ImagesCat. No.: HY-161524CAS No.: 3037978-19-8HDAC6-IN-43 (compound 26) is a potent HDAC inhibitor. HDAC6-IN-43 effectively inhibits several HDACs, notably HDAC1, HDAC2, and HDAC6 (IC50 < 150 nM), displaying a particularly high sensitivity towards HDAC6 (IC50 = 11 nM). HDAC6-IN-43 can be used for the research of autosomal dominant polycystic kidney disease (ADPKD).
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HDAC-IN-93
0 ImagesCat. No.: HY-178104HDAC-IN-93 is a HDAC inhibitor with promising total pan-HDAC inhibitory activity. HDAC-IN-93 demonstrates significant broad-spectrum antiproliferative activity across various cancer cell lines. HDAC-IN-93 induces cell apoptosis along with necrosis. HDAC-IN-93 can be used for the studies of prostate cancer and breast cancer.
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HDAC6/ERα ligand-1
0 ImagesCat. No.: HY-187388HDAC6/ERα ligand-1 is a dual-target ligand with inhibitory activity against both estrogen receptor α (ERα) and histone deacetylase 6 (HDAC6). HDAC6/ERα ligand-1 can be used to synthesize PROTACs, such as PROTAC HDAC6/ERα degrader 1 (HY-187387). HDAC6/ERα ligand-1 binds to the ligand-binding pocket of ERα and forms hydrogen bonds with specific residues in helices 10, 11 and 12. HDAC6/ERα ligand-1 binds stably to HDAC6 and forms hydrogen bonds with specific residues of this protein. HDAC6/ERα ligand-1 can be used in breast cancer research.
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Quisinostat hydrochloride
0 ImagesCat. No.: HY-15433BCAS No.: 1083078-98-1Synonyms: JNJ26481585 hydrochlorideQuisinostat (JNJ-26481585) hydrochloride is a potent and orally active pan-HDAC inhibitor (HDACi), with IC50 values ranging from 0.11 nM to 0.64 nM for HDAC1, HDAC2, HDAC4, HDAC10 and HDAC11. Quisinostat hydrochloride has a broad spectrum antitumoral activity. Quisinostat hydrochloride can induce autophagy in neuroblastoma cells.
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HDAC-IN-47
0 ImagesCat. No.: HY-151443CAS No.: 3033608-94-2HDAC-IN-47 is an orally active inhibitor of histone deacetylase (HDAC), with IC50s of 19.75 nM (HDAC1), 5.63 nM (HDAC2), 40.27 nM (HDAC3), 57.8 nM (HDAC2), 302.73 nM (HDAC8), respectively. HDAC-IN-47 inhibits autophagy and induces apoptosis via the Bax/Bcl-2 and caspase-3 pathways. HDAC-IN-47 arrests cell cycle at G2/M phase, and shows anti-tumor efficacy in vivo.
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CM-444
0 ImagesCat. No.: HY-163803CAS No.: 2256079-52-2CM-444 is inhibitor for HDAC (IC50 is 6 nM-0.6 μM) and DNA methyltransferases (DNMT, IC50 is 1.8-2.3 μM). CM-444 is an inducer for the differentiation of acute myeloid leukemia cells. CM-444 exhibits anti-leukemic activity and improves the survival rate in mouse models.
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HDAC1/6-IN-1
0 ImagesCat. No.: HY-144725CAS No.: 2630989-02-3HDAC1/6-IN-1 (compound D7) is a potent multitarget inhibitor of GLP, HDAC6 and HDAC1, with IC50 values of 1.3, 13, and 89 nM, respectively. HDAC1/6-IN-1 can inhibit the methylation and deacetylation of H3K9 on protein level. HDAC1/6-IN-1 induces cancer cell apoptosis, G0/G1 cell cycle arrest, and blocks migration and invasion.
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HDAC6-IN-80
0 ImagesCat. No.: HY-182777CAS No.: 3118852-74-4HDAC6-IN-80 is an orally active, selective HDAC6 inhibitor with an IC50 of 8.5 nM. HDAC6-IN-80 inhibits lipopolysaccharide-induced microglial activation, reduces the levels of iNOS, COX-2, TNF-α and IL-6, and alleviates sensory hypersensitivity behaviors. HDAC6-IN-80 can be used for the research of inflammatory pain and chemotherapy-induced peripheral neuropathy.
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HDAC6-IN-49
0 ImagesCat. No.: HY-169156HDAC6-IN-49 (Compound 3) is an inhibitor for HDAC with IC50 of 0.012 and 0.735 μM for HDAC6 and HDAC1. HDAC6-IN-49 also exhibits inhibitory activities against MAO-B, cholinesterase (ChE), histamine receptor (H3R) and serotonin 6 receptor (5-HT6R). HDAC6-IN-49 exhibits neuroprotective efficacy on SH-SY5Y cell. HDAC6-IN-49 improves cognitive function and locomotor ability in Drosophila Parkinson's disease models and in C. elegans Alzheimer's disease models.
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HDAC6-IN-74
0 ImagesCat. No.: HY-181579HDAC6-IN-74 is an orally active, selective histone deacetylase 6 (HDAC6) inhibitor with an IC50 of 0.036 μM. HDAC6-IN-74 induces tumor cell apoptosis, arrests cells at the S phase of the cell cycle, and impairs cell migration, invasion and colony-forming abilities. HDAC6-IN-74 exerts anticancer effects with no obvious toxicity. HDAC6-IN-74 can be used in the research of cancers such as liver cancer.
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ZYJ-34c
0 ImagesCat. No.: HY-139815CAS No.: 1314556-93-8ZYJ-34c is an orally active and potent histone deacetylase inhibitor (HDACi) with IC50s of 0.056 μM and 0.146 μM for HDAC6 and HDAC8, respectively. ZYJ-34c causes G1 phase arrest in low concentration. ZYJ-34c has antiproliferative activities. ZYJ-34c exhibits antitumor potency in MDA-MB-231 and HCT116 xenograft models and possesses antimetastatic potential in a mouse hepatoma-22 (H22) pulmonary metastasis model.
