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 (210)
Related Products (210)
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Antibodies (2)
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FNDR-20123
0 ImagesFNDR-20123 is a safe, first-in-class, and orally active anti-malarial HDAC inhibitor with IC50s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively. FNDR-20123 exerts anti-malarial activity against Plasmodium falciparum asexual stage (IC50=41 nM) and sexual blood stage (IC50=190 nM for male gametocytes). FNDR-20123 inhibits HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 (IC50=25/29/2/11/282 nM, respectively.) and inhibits Class III HDAC isoforms at nanomolar concentrations.
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HDAC4-IN-1
0 ImagesHDAC4-IN-1 (compound 1a) is a class IIa HDACI inhibitor (IC50=0.077 μM). HDAC4-IN-1 can enhance Caspase-induced Apoptosis. HDAC4-IN-1 has anticancer activity. HDAC4-IN-1 can be used in the research of drug combination against cancer.
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CARM1/HDAC2-IN-1
0 ImagesCat. No.: HY-157388CAS No.: 3074558-69-0CARM1/HDAC2-IN-1 (compound CH-1) is a dual inhibitor against CARM1 and HDAC2, with IC50 values of 3.71 nM and 4.07 nM, respectively. CARM1/HDAC2-IN-1 possesses antitumor activity.
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HDAC-IN-53
0 ImagesCat. No.: HY-149208CAS No.: 2921948-27-6HDAC-IN-53 is an orally active, and selective HDAC1-3 inhibitor with IC50 values of 47 nM, 125 nM, and 450 nM, respectively. HDAC-IN-53 does not inhibit class II HDACs (HDAC4, 5, 6, 7, 9; IC50>10 μM). HDAC-IN-53 induces caspase-dependent apoptosis. HDAC-IN-53 significantly inhibits the growth of human tumor xenografts in nude mice and murine tumor growth in immune-competent mice bearing MC38 colon cancer.
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LSD1/HDAC-IN-2
0 ImagesLSD1/HDAC-IN-2 (Compound 20c) is the inhibitor for LSD and HDAC, that inhibits LSD1, HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, with IC50s of 39.0, 1.4, 1.0, 1.3, 2.9 and 16.0 nM, respectively. LSD1/HDAC-IN-2 inhibits the proliferation of cancer cells, especially the colorectal cancer cells. LSD1/HDAC-IN-2 arrests the cell cycle at G2/M phase, inhibits cell migration, and induces apoptosis in HCT-116 and HT-29 cells. LSD1/HDAC-IN-2 exhibits antitumor efficacy in mouse model without significant toxicity.
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Tucidinostat-d4
0 ImagesSynonyms: Chidamide-d4; HBI-8000-d4; CS 055-d4
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cis-BG47
0 ImagesCat. No.: HY-117583Purity: 98.02%cis-BG47 is an cis-isomer of BG47, BG47 is a prototypical histone deacetylases HDAC1 and HDAC2 selective, optoepigenetic probe. BG47 can bind to and competitively inhibits the deacetylase activity of HDAC targets upon a light-induced trans-to-cis isomerization, and increases Histone Methyltransferase H3K9 acetylation. cis-BG47 can be used for neurological disease research.
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CRA-026440 hydrochloride
0 ImagesCRA-026440 hydrochloride is a potent, broad-spectrum HDAC (HDAC) inhibitor. The Ki values against recombinant HDAC isoenzymes HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 are 4 nM, 14 nM, 11 nM, 15 nM, 7 nM, and 20 nM respectively. CRA-026440 hydrochloride shows antitumor and antiangiogenic activities. CRA-026440 (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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XSJ-10
0 ImagesCat. No.: HY-157740XSJ-10 is a HDAC inhibitor containing a RAS/RAF protein interfering unit, with IC50s of 0.05 and 0.04 μM in PANC-1 cells and HT-29 cells. XSJ-10 can effectively induce the apoptosis of cancer cells and suppress the tumor by strongly inhibiting the RAS-RAF-MEK-ERK signaling pathway and the acetylation level of HDAC3.
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4-Phenylcinnamic acid
0 ImagesCat. No.: HY-W103792CAS No.: 13026-23-84-Phenylcinnamic acid is a weak HDAC2 inhiibitor (IC50 > 5 μM). 4-Phenylcinnamic acid has weak cell growth inhibition against tumor cells.
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FF2049
0 ImagesCat. No.: HY-168863FF2049 is a selective HDAC1-3 PROTAC degrader (with a DC50 of 257 nM against HDAC1). FF2049 recruits the E3 ligase FEM1B to mediate ubiquitination and proteasomal degradation of HDAC1-3. FF2049 induces cell cycle arrest and Apoptosis in cells. FF2049 can be used in research related to multiple myeloma, acute monocytic leukemia, triple-negative breast cancer and glioblastoma.
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HDAC6-IN-5
0 ImagesCat. No.: HY-146678CAS No.: 2413603-15-1HDAC6-IN-5 (compound 11b) is a potent and BBB-penetrated HDAC6 inhibitor, with an IC50 of 0.025 μM. HDAC6-IN-5 exhibits strong inhibitory activity against Aβ1-42 self-aggregation and AChE, with IC50 values of 3.0 and 0.72 μM. HDAC6-IN-5 can enhance neurite outgrowth without significant neurotoxicity.
