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 (337)
Related Products (337)
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Antibodies (2)
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HDAC-IN-37
0 ImagesCat. No.: HY-146750CAS No.: 2766466-56-0
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PARP-1/HDAC-IN-1
0 ImagesCat. No.: HY-146160CAS No.: 3032621-10-3PARP-1/HDAC-IN-1 is a PARP-1/HDAC6 dual targeting inhibitor with IC50s of 68.90 nM and 510 nM, respectively. PARP-1/HDAC-IN-1 displays remarkable anticancer, anti-migration and anti-angiogenesis activities.
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HDAC6-IN-47
0 ImagesCat. No.: HY-163834HDAC6-IN-47 (Compound S-29b) is inhibitor for HDAC, which exhibits high affinities to HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, HDAC10 with Ki of 60, 56, 162, 0.44, 362 and 849 nM, respectively. HDAC6-IN-47 causes tubulin hyperacetylation in MV4-11, inhibits the proliferation of MV4-11 with an EC50 of 0.50 µM. HDAC6-IN-47 can be used in research of leukemia.
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PI3Kδ/HDAC6-IN-1
0 ImagesCat. No.: HY-174396CAS No.: 3075011-99-0PI3Kδ/HDAC6-IN-1 (Compound 22E) is an orally active and dual inhibitor of PI3Kδ and HDAC6 with IC50 values of 2.4 nM and 6.2 nM, respectively. PI3Kδ/HDAC6-IN-1 exhibits potent antiproliferative effects on non-Hodgkin lymphoma (NHL) cells and possesses in vivo antitumor activity without significant toxicity. PI3Kδ/HDAC6-IN-1 arrests the cell cycle at the G0/G1 phase and induces apoptosis. PI3Kδ/HDAC6-IN-1 blocks the PI3K/AKT/mTOR signaling pathway and increases the acetylation levels of α-tubulin and histone H3.
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GSK-3β/HDAC-IN-2
0 ImagesCat. No.: HY-174398GSK-3β/HDAC-IN-2 is a potent inhibitor of GSK-3β (IC50 = 0.04 μM), HDAC2 (IC50 = 1.05 μM, Ki = 0.070 μM) and HDAC6 (IC50 = 1.52 μM, Ki = 0.017 μM). GSK-3β/HDAC-IN-2 inhibits HDAC2 and HDAC6 activities and blocks tau hyperphosphorylation. GSK-3β/HDAC-IN-2 exerts neuroprotective effects and shows no significant toxicity. GSK-3β/HDAC-IN-2 can be used in the research of Alzheimer's disease.
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cGAS/HDAC-IN-1
0 ImagesCat. No.: HY-184398cGAS/HDAC-IN-1 is an orally active dual cGAS/HDAC inhibitor that exhibits potent inhibitory activity against human and mouse cGAS (IC50: 0.17 and 1.80 μM, respectively) and moderate activity against HDAC3 and HDAC6 (IC50: 1.2 and 0.4 μM, respectively). cGAS/HDAC-IN-1 directly suppresses cGAS activity and increases its acetylation levels via HDAC3 inhibition. cGAS/HDAC-IN-1 is effective in murine models of inflammatory bowel disease and Aicardi-Goutières syndrome, and can be used in research on cGAS-dependent disorders.
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SHN7
0 ImagesCat. No.: HY-184706CAS No.: 3126116-06-8SHN7 is a selective HDAC1/HDAC6 inhibitor, NQO1 substrate and ROS inducer, with an IC50 of 30 nM against HDAC1 and an IC50 of 10 nM against HDAC6. SHN7 inhibits STAT3 with a Kd of 8.9 μM. SHN7 arrests the cell cycle at the G2/M phase and induces Apoptosis. SHN7 exhibits anti-tumor effects in triple-negative breast cancer (TNBC) xenograft models. SHN7 can be used for the research of triple-negative breast cancer.
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HDAC ligand-5
0 ImagesCat. No.: HY-168864HDAC ligand-5 is a template for the non-selective HDAC inhibitor Vorinostat (HY-10221). HDAC ligand-5 can serve as a ligand for target protein (Ligands for Target Protein for PROTAC) for the development of PROTAC HDAC degraders with antitumor activity. HDAC ligand-5 can be used for the synthesis of FF2049 (HY-168863).
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HDAC6-IN-44
0 ImagesCat. No.: HY-162630HDAC6-IN-44 (compound H10) is a selective HDAC6 inhibitor with an IC50 value of 8.97 nM. HDAC6-IN-44 can inhibit the idiopathic pulmonary fibrosis (IPF) phenotype and exhibits antifibrotic activity. Additionally, HDAC6-IN-44 reduces fibrogenesis in a bleomycin-induced pulmonary fibrosis mouse model and demonstrates good metabolic stability. HDAC6-IN-44 holds promise for research in the field of idiopathic pulmonary fibrosis.
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HDAC6-IN-34
0 ImagesCat. No.: HY-163368CAS No.: 1432508-73-0HDAC6-IN-34 (compound 21) is an oral active and selective HDAC6 inhibitor with the IC50 of 18 nM. HDAC6-IN-34 increases the acetylation level of tubulin without affecting histone acetylation in cutaneous T-cell lymphoma cells and inhibits TNF-α secretion in LPS (HY-D1056)-stimulated macrophage cells. HDAC6-IN-34 shows excellent anti-arthritic efficacy in rat.
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mTOR/HDAC6-IN-1
0 ImagesCat. No.: HY-144449CAS No.: 2986747-52-6
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HDAC6-IN-86
0 ImagesCat. No.: HY-187210CAS No.: 2271229-98-0HDAC6-IN-86 is a histone deacetylase 6 (HDAC6) inhibitor with an IC50 of 74 nM, and it exhibits high selectivity for HDAC1. HDAC6-IN-86 induces cell apoptosis, triggers G2/M phase cell cycle arrest, and inhibits the proliferation of glioma cells. HDAC6-IN-86 can be used for the research of glioblastoma multiforme (GBM).
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HDAC-IN-76
0 ImagesCat. No.: HY-161984HDAC-IN-76 (compound 6i) is a histone deacetylase (HDAC) inhibitor. HDAC-IN-76 IC50 values of 30 nM and 98 nM for Pf3D7 (chloroquine (HY-17589A) drug-susceptible strain) and PfDd2 (chloroquine (HY-17589A) drug-resistant strain), has a highly potent antimalarial activity against asexual blood-stage Plasmodium, respectively, and exhibits selective inhibition against parasites, with IC50 values of 7 nM and 9 nM for human HDAC1 and HDAC6, respectively, while inhibiting PfHDAC1.
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NN-429
0 ImagesCat. No.: HY-182649CAS No.: 2490284-32-5NN-429 is a selective HDAC6 inhibitor. NN-429 induces apoptosis, increases the acetylation level of α-tubulin, and exhibits cytotoxicity against cancer cells. NN-429 is applicable to research related to acute myeloid leukemia, multiple myeloma and lymphoma.
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JAK/HDAC-IN-2
0 ImagesCat. No.: HY-149283CAS No.: 3029138-43-7JAK/HDAC-IN-2 is a potent 2-amino-4-phenylaminopyrimidine JAK/HDAC dual-target inhibitor. JAK/HDAC-IN-2 potently inhibits HDAC3/6 and JAK1/2 at nanomolar levels. JAK/HDAC-IN-2 has proapoptotic activity and inhibits histone deacetylation and STAT3 phosphorylation. JAK/HDAC-IN-2 presents remarkable antiproliferative activity in both hematological malignancies and solid cancers.
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PROTAC HDAC6 degrader 4
0 ImagesCat. No.: HY-172359PROTAC HDAC6 degrader 4 is a potent and selective HDAC6 PROTAC degrader with an IC50 of 0.295 μM. PROTAC HDAC6 degrader 4 bridges HDAC6 and the CRBN E3 ubiquitin ligase to form a ternary complex, thereby inducing the specific degradation of HDAC6 via the ubiquitin-proteasome system. PROTAC HDAC6 degrader 4 can be used in studies related to multiple myeloma.
