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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PD-L1/HDAC-IN-1
0 ImagesCat. No.: HY-172167CAS No.: 2923313-69-1PD-L1/HDAC-IN-1 (Compound 14) is the inhibitor for PD-L1 and HDAC that inhibits PD-1/PD-L1 interaction, HDAC2 and HDAC3 with IC50 of 88.10, 27.98 and 14.47 nM, respectively. PD-L1/HDAC-IN-1 exhibits slight cytotoxicity in MCF-7 (IC50=19.34 μM). PD-L1/HDAC-IN-1 upregulates the expression of PD-L1 and CXCL10, promoting anti-tumour immune response by recruiting T-cell infiltration into TME.
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β-Hydroxymethyl chalcone
0 ImagesCat. No.: HY-118394CAS No.: 1613310-15-8β-Hydroxymethyl chalcone is a time-dependent selective HDAC2 inhibitor, with IC50 values of 0.17 μM (24 h) and 9.19 μM (1 h). After binding to the catalytic zinc ion in the active pocket of HDAC2, β-Hydroxymethyl chalcone undergoes an intramolecular nucleophilic attack to form a cyclic product, resulting in time-dependent tight binding. β-Hydroxymethyl chalcone can be used for the study of HDAC2 selective inhibition and related epigenetic targets[1].
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CRA-026440
0 ImagesCat. No.: HY-19754CAS No.: 847460-34-8CRA-026440 is a potent, broad-spectrum HDAC inhibitor. The Ki values against recombinant HDAC isoenzymes HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 are 4, 14, 11, 15, 7, and 20 nM respectively. CRA-026440 shows antitumor and antiangiogenic activities. CRA-026440 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
