HDAC3
HDAC3 (histone deacetylase 3) is a class I histone deacetylase that functions as a central epigenetic regulator of chromatin structure and transcriptional repression through its association with nuclear receptor corepressor complexes containing NCOR and SMRT[1][2]. Mechanistically, HDAC3 forms an enzymatically active complex with NCOR/SMRT and associated cofactors, enabling histone deacetylation and coordinated control of gene expression programs involved in metabolism, circadian regulation, and cellular homeostasis[2][3][4]. HDAC3 also participates in signal-responsive transcriptional regulation, including repression of the JNK pathway and modulation of inflammatory gene expression, linking epigenetic regulation to cellular stress and immune responses[5][6]. In disease models, dysregulation of HDAC3-dependent transcriptional networks has been associated with metabolic disorders, cardiovascular pathology, inflammatory diseases, and cancer-related transcriptional abnormalities[4][6]. HDAC3 is additionally required for normal embryonic development, organ function, and maintenance of metabolic processes, highlighting its broad physiological significance[4]. Compared with related class I HDAC isoforms, HDAC3 is distinguished by its obligate functional interaction with the NCOR/SMRT corepressor complex and its dependence on corepressor-mediated activation for full biological activity[1][2][7]. Structural and genetic studies further demonstrate that disruption of HDAC3-corepressor interactions compromises HDAC3 function in vivo, emphasizing a unique regulatory mechanism not shared to the same extent by other HDAC family members[7][3]. For experimental applications, selective HDAC3 inhibitors are widely used to investigate epigenetic control of inflammation, metabolism, and disease-associated transcriptional programs, while offering greater isoform specificity than pan-HDAC inhibition strategies[6][4].
References:
- [1]. Wen YD, et al. The histone deacetylase-3 complex contains nuclear receptor corepressors. Proc Natl Acad Sci U S A. 2000 Jun 20;97(13):7202-7. [Content Brief]
- [2]. 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]
- [3]. Watson PJ, et al. Structure of HDAC3 bound to co-repressor and inositol tetraphosphate. Nature. 2012 Jan 9;481(7381):335-40. [Content Brief]
- [4]. He R, et al. The role of HDAC3 and its inhibitors in regulation of oxidative stress and chronic diseases. Cell Death Discov. 2023 Apr 18;9(1):131. [Content Brief]
- [5]. Zhang J, et al. The N-CoR-HDAC3 nuclear receptor corepressor complex inhibits the JNK pathway through the integral subunit GPS2. Mol Cell. 2002 Mar;9(3):611-23. [Content Brief]
- [6]. Watson N, et al. The role of HDAC3 in inflammation: mechanisms and therapeutic implications. Front Immunol. 2024 Jul 10;15:1419685. [Content Brief]
- [7]. Rabezanahary H, et al. Live virus neutralizing antibodies against pre and post Omicron strains in food and retail workers in Québec, Canada. Heliyon. 2024 May 21;10(10):e31026. [Content Brief]
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HDAC3 Related Products (204)
Related Products (204)
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Antibodies (1)
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HDAC3-IN-3
0 ImagesCat. No.: HY-161154CAS No.: 2170996-03-7
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HDAC6-IN-87
0 ImagesCat. No.: HY-189296CAS No.: 3122437-17-3HDAC6-IN-87 is a selective HDAC6 inhibitor (IC50 = 4.29 nM). HDAC6-IN-87 weakly inhibits HDAC1 (IC50 = 749.59 nM), HDAC3 (IC50 = 813.09 nM), and HDAC10 (IC50 = 679.25 nM). HDAC6-IN-87 exhibits broad-spectrum antitumor activity, elevates α-tubulin acetylation levels without affecting histone H3 acetylation, and induces cell cycle arrest and apoptosis. HDAC6-IN-87 can be used for cancer-related research.
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Top/HDAC-IN-2
0 ImagesCat. No.: HY-145852CAS No.: 2775446-64-3
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HDAC3-IN-8
0 ImagesCat. No.: HY-181768CAS No.: 2763368-90-5HDAC3-IN-8 is a selective inhibitor targeting HDAC1, HDAC2 and HDAC3, with IC50 values of 3.52 nM for HDAC1, 15.14 nM for HDAC2 and 0.38 nM for HDAC3. HDAC3-IN-8 shows high selectivity for HDAC3 and exerts its effect by inhibiting histone deacetylase activity. HDAC3-IN-8 can be used to construct HDAC3-targeted PROTAC degrader (HY-181767) and is suitable for the research of acute myeloid leukemia (AML).
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HDAC6-IN-45
0 ImagesCat. No.: HY-161783CAS No.: 3048532-05-1HDAC6-IN-45 (Compound 15) is a selective inhibitor for HDAC6 with IC50 of 15.2 nM. HDAC6-IN-45 exhibits neurotrophic through the upregulation of GAP43 and Beta-3 tubulin markers. HDAC6-IN-45 activates the Nrf2 signaling pathway, reduces H2O2-induced ROS production, inhibits apoptosis in PC12, and exhibits neuroprotective efficacy in SCOP-induced zebrafish Alzheimer's Disease models. HDAC6-IN-45 exhibits antioxidant activity and good blood-brain barrier (BBB) permeability.
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sEH/HDAC6-IN-1
0 ImagesCat. No.: HY-163207CAS No.: 2847838-67-7
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HDAC/Top-IN-1
0 ImagesCat. No.: HY-144654CAS No.: 2411379-14-9HDAC/Top-IN-1 is an orally active and pan HDAC/Top dual inhibitor with IC50s of 0.036 μM, 0.14 μM, 0.059 μM, 0.089 μM and 9.8 μM for HDAC1, HDAC2, HDAC3, HDAC6 and HDAC8. HDAC/Top-IN-1 efficiently induces apoptosis with S cell-cycle arrest in HEL cells. HDAC/Top-IN-1 has exhibits excellent in vivo antitumor efficacy.
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HDAC6-IN-51
0 ImagesCat. No.: HY-169226CAS No.: 2994634-78-3HDAC6-IN-51 (Compound 7e) is a selective HDAC6 inhibitor with an IC50 value of 42.9 nM. HDAC6-IN-51 exhibits good anti-lung fibrosis activity.
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Andrographidine E
0 ImagesCat. No.: HY-N16881CAS No.: 113963-41-0Andrographidine E is a COX-2 (IC50 = 19 μM) and HDAC inhibitor, with high affinity for HDAC1 and HDAC3. Andrographidine E can specifically bind to macrophages and has potential immunotargeting properties. Andrographidine E can be used for studying inflammation.
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sEH/HDAC6-IN-2
0 ImagesCat. No.: HY-159171CAS No.: 3009011-58-6sEH/HDAC6-IN-2 is a potent dual soluble epoxide hydrolase (sEH) and HDAC6 inhibitor with IC50s of 0.9 nM, 46.8 nM, and 8 nM for human sEH, mouse sEH, and HDAC6, respectively. sEH/HDAC6-IN-2 can be used for the study of inflammatory pain.
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Leuxinostat
0 ImagesCat. No.: HY-162658Leuxinostat is an inhibitor for HDAC with IC50 of 30 nM for hHDAC6. Leuxinostat inhibits the proliferation of cells THP1, K562, U937 and MEK1, induces apoptosis in leukemia cells NB4 and MOLT-4. Leuxinostat inhibits the expansion of hematopoietic stem cells and exhibits antileukemic activity in zebrafish models.
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Nanatinostat TFA
0 ImagesCat. No.: HY-13432ACAS No.: 1256448-48-2Synonyms: CHR-3996 TFANanatinostat (CHR-3996) TFA is a potent, class I selective and orally active HDAC inhibitor with IC50s of 3 nM, 4 nM, and 7 nM for HDAC1, HDAC2, and HDAC3, respectively. Nanatinostat TFA has low activity against HDAC5 (IC50 of 200 nM) and HDAC6 (IC50 of 2100 nM). Nanatinostat TFA induces apoptosis in myeloma cells. Nanatinostat TFA has potent anticancer effects, such as myeloma, advanced solid tumours and colorectal cancer.
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CM-414
0 ImagesCat. No.: HY-119316CAS No.: 2007971-51-7CM-414 is a brain-penetrant phosphodiesterase 5 (PDE5) and HDAC inhibitor with IC50s of 60 nM, 91 nM, 310 nM, 322 nM and 490 nM for PDE5, HDAC6, HDAC1, HDAC3 and HDAC2, respectively. CM-414 diminishes brain Aβ and tau phosphorylation (pTau) level in Tg2576 mice. CM-414 can be used for the study of Alzheimer's disease (AD).
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PROTAC HDAC3 degrader-1
0 ImagesCat. No.: HY-181767CAS No.: 3133883-15-2PROTAC HDAC3 degrader-1 is a selective PROTAC degrader targeting HDAC3 with a DC50 of 30.73 nM. PROTAC HDAC3 degrader-1 induces degradation of HDAC3 via the ubiquitin-proteasome system. PROTAC HDAC3 degrader-1 promotes apoptosis, induces DNA damage, and downregulates anti-apoptotic proteins Mcl-1 and Bcl-xL. PROTAC HDAC3 degrader-1 can be used for the research of acute myeloid leukemia.
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MC2625
0 ImagesCat. No.: HY-152225CAS No.: 1776116-75-6MC2625 is a potent pyridine-containing histone deacetylase (HDAC) inhibitor. MC2625 show selective HDAC3 and HDAC6 inhibition with IC50s of 80 nM and 11 nM. MC2625 increases acetyl-H3 and acetyl-tubulin levels and inhibits cancer stem cells (CSCs) growth by apoptosis induction.
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IOR-160
0 ImagesCat. No.: HY-176561CAS No.: 2421119-78-8IOR-160 is a dual inhibitor of casein kinase 2 (CK2) and HDACs. IOR-160 exhibits high selectivity for CK2 (IC50 = 1.7 nM) and broad inhibitory activity against HDAC (HDAC 1, 2, 3, and 6 with IC50s of 3.3 nM, 24.0 nM, 3.9 nM, and 13.0 nM, respectively, with low activity for HDAC8). IOR-160 modulates key cellular signaling pathways by inhibiting AKT phosphorylation and increasing acetylated α-tubulin. IOR-160 inhibits tumor growth and reduces tumor burden through dual CK2/HDAC inhibition. IOR-160 is indicated for use in triple-negative breast cancer research.
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HDAC6-IN-69
0 ImagesCat. No.: HY-180214HDAC6-IN-69 is a brain-penetrant and highly selective HDAC6 inhibitor with an IC50 of 4.0 nM. HDAC6-IN-69 shows >176-fold against other HDAC isoforms. HDAC6-IN-69 engages the target in neuronal cells by dose-dependently upregulating acetylated α-tubulin in virto. HDAC6-IN-69 has neuroprotective effect and can be used for ischemic stroke research .
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NL-103
0 ImagesCat. No.: HY-12487CAS No.: 1788896-33-2
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A2AAR/HDAC-IN-1
0 ImagesCat. No.: HY-143324CAS No.: 2767560-51-8A2AAR/HDAC-IN-1 (compound 14c) is an orally active, potent and balanced A2AAR/HDAC dual inhibitor, with a Ki of 163.5 nM for A2AAR and an IC50 of 145.3 nM for HDAC1. A2AAR/HDAC-IN-1 shows anticancer activity.
