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-46
0 ImagesCat. No.: HY-150597CAS No.: 2562386-85-8HDAC-IN-46 (compound 12c) is a potent HDAC inhibitor with an IC50 value of 0.21 μM and 0.021 μM for HDAC1 and HDAC6, respectively. HDAC-IN-46 upregulates p-p38, and downregulates Bcl-xL and cyclin D1 in MDA-MB-231 cells. HDAC-IN-46 induces significant G2 phase arrest and apoptosis. HDAC-IN-46 can be used for researching triple-negative breast cancer (TNBC).
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GRK2 modulator 1
0 ImagesCat. No.: HY-183057CAS No.: 2234900-83-3GRK2 modulator 1 is an orally active, brain-penetrant and selective GRK2 modulator. GRK2 modulator 1 enhances the active, non-phosphorylated GRK2 and prevents mitochondrial GRK2 and TOMM6 aggregation. GRK2 modulator 1 enhances the non-amyloidogenic processing of APP and prevent PHF-tau, neurodegeneration, and neuronal loss. GRK2 modulator 1 decreases the senescence marker, UPAR, reduces the Alzheimer disease (AD)-related mortality, and prolongs survival. GRK2 modulator 1 exerts neuroprotection by inhibiting HDAC6, and counteracts age-related cardiac dysfunction. GRK2 modulator 1 can be used for research on AD.
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PROTAC HDAC6 degrader 10
0 ImagesCat. No.: HY-184389PROTAC HDAC6 degrader 10 is a highly efficient, safe and selective HDAC6 PROTAC degrader with a pIC50 of 8.75 and a pDC50 of 9.2 in BEAS-2B cells. PROTAC HDAC6 degrader 10 recruits cereblon to form a ternary complex with HDAC6, thereby achieving the degradation of HDAC6. PROTAC HDAC6 degrader 10 significantly induces hyperacetylation of α-tubulin without affecting the acetylation of H3, and achieves sustained HDAC6 knockdown in mouse lung tissues. PROTAC HDAC6 degrader 10 exhibits high bioavailability after subcutaneous administration in mice. PROTAC HDAC6 degrader 10 enables the study of HDAC6 pharmacology via chemical knockdown of HDAC6 in vitro and in vivo, and can be used for research on pulmonary diseases.
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HDAC6-IN-75
0 ImagesHDAC6-IN-75 is a selective HDAC6 inhibitor with an IC50 of 0.17 nM against HDAC6. HDAC6-IN-75 induces the accumulation of acetylated α-tubulin in glioma cells. HDAC6-IN-75 triggers cell cycle changes, increases the SubG1 cell population, and promotes apoptosis in glioma cells and glioblastoma stem cells. HDAC6-IN-75 is applicable for glioma-related research.
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HDAC6-IN-61
0 ImagesCat. No.: HY-176733HDAC6-IN-61 (Compound 4e) is a HDAC6 inhibitor (IC50: 73 nM) with selectivity over other HDAC isoforms. HDAC6-IN-61 is also a GPR40 activator. HDAC6-IN-61 increases acetylated tubulin and ERK phosphorylation levels. HDAC6-IN-61 can be used for research of neuroinflammation such as Alzheimer's disease.
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FF2039
0 ImagesCat. No.: HY-172159FF2039 is a pan-HDAC PROTAC degrader that binds to DCAF11, acting on HDAC6, HDAC1, HDAC2 and HDAC4. FF2039 recruits the DCAF11 E3 ligase and mediates the polyubiquitination and degradation of HDACs via the ubiquitin-proteasome system. FF2039 induces cell cycle arrest, apoptosis, cytotoxicity and antiproliferative activity in cancer cells, and reduces the clonogenic capacity of cancer cells. FF2039 is applicable to research related to multiple myeloma, triple-negative breast cancer and glioblastoma.
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HDAC-IN-98
0 ImagesHDAC-IN-98 is a HDAC1, HDAC2, HDAC3 inhibitor (one of the most selective class I HDAC inhibitors) with human IC50 values of 41.2 nM, 52.5 nM, and 74.3 nM respectively. HDAC-IN-98 induces H3K9 acetylation, p21 upregulation, G2/M arrest, cell apoptosis, has strong antiproliferative effects in colorectal cancer cells, low toxicity in healthy colon epithelium, modulates short-term in vitro effects via autophagy, and shows strong antitumor efficacy in vivo in the chorioallantoic membrane model (CAM) assay. HDAC-IN-98 can be used for the research of colorectal cancer.
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HDAC6-IN-42
0 ImagesCat. No.: HY-161516HDAC6-IN-42 (compound 2b) is an HDAC6 inhibitor (IC50=0.009 μM). HDAC6-IN-42 shows significant anti-leukemia activity and synergistic effect with Decitabine (HY-A0004). HDAC6-IN-42 can be used for the AML research.
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KH-259
0 ImagesCat. No.: HY-150503CAS No.: 3023019-93-1
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PIM-1/HDAC-IN-2
0 ImagesCat. No.: HY-174302CAS No.: 3103925-33-0PIM-1/HDAC-IN-2 is a robust PIM/HDAC inhibitor (IC50 = 0.11 μM in MV4-11cells), which exerts a synergistic antiproliferative effect through a dual mechanism of inhibiting PIM1 kinase and selectively inhibiting HDAC6. PIM-1/HDAC-IN-2 induces cell apoptosis. PIM-1/HDAC-IN-2 remarkably induces the cleavage of PARP, thereby initiating the arrest of the cell cycle in G1 phase and a reduction in S phase. PIM-1/HDAC-IN-2 demonstrates significant anticancer efficacyin the MV4-11 xenograft model without notable toxicity[1].
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HDAC6-IN-83
0 ImagesCat. No.: HY-184304CAS No.: 3053098-60-2HDAC6-IN-83 is a selective histone deacetylase 6 (HDAC6) inhibitor with an IC50 value of 11.49 nM. HDAC6-IN-83 selectively increases the acetylation level of α-tubulin without affecting histone H3. HDAC6-IN-83 induces cell apoptosis, induces cell cycle arrest, inhibits cancer cell proliferation, suppresses cancer cell invasion and inhibits angiogenesis. HDAC6-IN-83 can be used in non-small cell lung cancer research.
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NN-390
0 ImagesCat. No.: HY-143877CAS No.: 2490284-25-6NN-390 is a potent and selective HDAC6 inhibitor, with an IC50 of 9.8 nM. NN-390 penetrates the blood-brain barrier (BBB). NN-390 shows study potential in metastatic Group 3 MB (medulloblastoma).
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HDAC-IN-104
0 ImagesCat. No.: HY-184574HDAC-IN-104 is a potent and selective class I Histone deacetylases (HDAC) inhibitor with an IC50 of 25 nM. HDAC-IN-104 exerts potent antiproliferative and antitumor effects by inhibiting glycolysis and OXPHOS via blockade of the PI3K/AKT signaling pathway, and these effects are synergistically enhanced when combined with the FMS-like tyrosine kinase 3 (FLT3) inhibitor Quizartinib (AC220) (HY-13001). HDAC-IN-104 induces significant early and late apoptosis. HDAC-IN-104 can be used for acute myeloid leukemia (AML) research.
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G4/HDAC-IN-1
0 ImagesCat. No.: HY-151263CAS No.: 3031784-60-5G4/HDAC-IN-1 (compound a6) is a G4/HDAC dual-targeting compound. G4/HDAC-IN-1 inhibits intracellular HDAC activity with an IC50 value of 1.1 μM, and induces G4 formation. G4/HDAC-IN-1 inhibits TNBC proliferation and tumor growth in TNBC xenograft model. G4/HDAC-IN-1 can be used for the research of cancer.
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HDAC6/HSP90-IN-1
0 ImagesCat. No.: HY-146293CAS No.: 2411955-43-4HDAC6/HSP90-IN-1 (compound 17) is a potent and selective dual inhibitor of HDAC6 and HSP90, with IC50 values of 4.3 and 46.8 nM, respectively. HDAC6/HSP90-IN-1 down-regulates PD-L1 expression in INF-γ treated H1975 lung cancer cells. HDAC6/HSP90-IN-1 inhibits tumor growth in human H1975 xenograft mice.
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HDAC6-IN-63
0 ImagesCat. No.: HY-178022HDAC6-IN-63 (Compound 7) is an orally active HDAC6 inhibitor with an IC50 of 145 nM. HDAC6-IN-63 inhibits the expression of Sp1 and RAD51, thereby inducing Caspase-dependent apoptosis. HDAC6-IN-63 has antitumor activity and sensitizes Etoposide (HY-13629) and Gemcitabine (HY-17026), promoting synergistic death of NSCLC cells through the inhibition of homologous recombination and non-homologous end joining (NHEJ) pathways involved in DNA DSB repair. HDAC6-IN-63 can be used for chemotherapy of cancers like NSCLC research.
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HDAC6/HSP90-IN-3
0 ImagesCat. No.: HY-175467HDAC6/HSP90-IN-3 (Compound 17) is an orally active dual histone deacetylase 6 (HDAC6) and heat shock protein 90 (HSP90) inhibitor with IC50 values of 28 nM and 0.88 μM, respectively. HDAC6/HSP90-IN-3 is promising for research of malignant tumors such as prostate cancer.
