HDAC2
HDAC2 (histone deacetylase 2) is a class I histone deacetylase that removes acetyl groups from histone lysine residues and functions within multiprotein transcriptional repressor complexes to regulate gene expression, cell-cycle progression, and developmental processes[1][2]. Mechanistically, HDAC2 promotes chromatin condensation and transcriptional repression through histone deacetylation, thereby influencing cellular homeostasis and epigenetic regulation of gene activity[3][4]. Because histone acetylation and deacetylation dynamically control chromatin accessibility, HDAC2 participates in biological pathways linked to cell growth, cell death, and signal transduction[2][3]. In disease contexts, altered HDAC2 expression has been associated with multiple pathological conditions, particularly cancer and neurodegenerative disorders, where dysregulated epigenetic control contributes to disease progression[2]. Therefore, HDAC2 has emerged as an important experimental target for investigating epigenetic mechanisms underlying tumor biology and neurological dysfunction[2]. Compared with closely related class I isoforms, especially HDAC1, HDAC2 exhibits both overlapping and unique biological functions, with evidence supporting distinct as well as redundant roles in the regulation of proliferation and tumorigenesis[5]. This distinction has increased interest in isoform-selective approaches that can dissect HDAC2-specific functions while minimizing the limitations associated with broad-spectrum HDAC inhibition[2]. For experimental applications, selective HDAC2 inhibitors are widely investigated as chemical tools for studying transcriptional regulation and disease-associated epigenetic networks, and isoform-selective inhibition is considered advantageous because it may provide improved specificity and reduced adverse effects relative to pan-HDAC inhibitors[2].
References:
- [1]. HDAC2 gene information from NCBI.
- [2]. Marinović M, et al. Further investigation of harmicines as novel antiplasmodial agents: Synthesis, structure-activity relationship and insight into the mechanism of action. Eur J Med Chem. 2021 Nov 15;224:113687. [Content Brief]
- [3]. 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]
- [4]. Milazzo G, et al. Histone Deacetylases (HDACs): Evolution, Specificity, Role in Transcriptional Complexes, and Pharmacological Actionability. Genes (Basel). 2020 May 15;11(5):556. [Content Brief]
- [5]. Ogiwara H, et al. Histone acetylation by CBP and p300 at double-strand break sites facilitates SWI/SNF chromatin remodeling and the recruitment of non-homologous end joining factors. Oncogene. 2011 May 5;30(18):2135-46. [Content Brief]
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HDAC2 Related Products (211)
Related Products (211)
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Antibodies (2)
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C1A
0 ImagesCat. No.: HY-124946CAS No.: 1021463-02-4
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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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KTT-1
0 ImagesCat. No.: HY-179216CAS No.: 2397562-26-2KTT-1 is a kinetically selective and orally active HDAC2 inhibitor. KTT-1 exhibits high HDAC2-selectivity over HDAC1. KTT-1 inhibits osteoclast differentiation at an early stage by downregulating c-Fos expression. KTT-1 effectively suppresses arthritis symptoms in the collagen-induced arthritis (CIA) mouse model. KTT-1 can be used for the research of rheumatoid arthritis and neurodegenerative diseases.
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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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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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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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AC-340
0 ImagesCat. No.: HY-178336CAS No.: 3109965-54-7AC-340 is a potent hybrid VDR agonist/HDAC inhibitor. AC-340 superinduces VDR target genes (e.g., CYP24A1) and inhibits HDAC6 (IC50 = 0.37 μM) with ~10-fold selectivity over HDAC2. AC-340 induces VDR hyperagonism by causing widespread protein hyperacetylation (e.g., tubulin and H3K9/K27), which leads to elevated H3K27 acetylation on VDR target genes. AC-340 can be used for melanoma cancer 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.
