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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Rodin-C
0 ImagesCat. No.: HY-176868CAS No.: 2065162-16-3Rodin-C is a selective HDAC inhibitor with IC50s of 0.059, 0.18 and 5.39 μM for HDAC1, HDAC2 and HDAC11, respectively, over HDAC3-10. Rodin-C significantly inhibits the HDAC-CoREST complex with low hematological toxicity. Rodin-C can be used for neurologic disorders such as Alzheimer’s disease research.
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HDAC6-IN-82
0 ImagesCat. No.: HY-183560CAS No.: 1228571-33-2HDAC6-IN-82 is a selective HDAC6 inhibitor with an IC50 of 4.9 nM against HDAC6. HDAC6-IN-82 inhibits HDAC1 (112 nM), HDAC2 (737 nM), HDAC3 (623 nM), HDAC8 (1140 nM), HDAC10 (91.4 nM) and HDAC11 (219 nM). HDAC6-IN-82 reduces cancer cell viability, induces cell cycle arrest, triggers apoptosis, and increases the acetylation levels of H3K9 and α-tubulin. HDAC6-IN-82 can be used in cancer-related research such as leukemia.
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HDAC-IN-51
0 ImagesCat. No.: HY-152173CAS No.: 3026728-28-6HDAC-IN-51 is a potent histone deacetylase (HDAC) inhibitor with IC50 values of 0.32, 0.353, 0.431, 0.515, and 85.4 μM for HDAC10, HDAC1, HDAC2, HDAC3 and HDAC11, respectively. HDAC-IN-51 induces cell cycle arrest and apoptosis, modulating cell cycle-/apoptosis-related miRNAs expression. HDAC-IN-51 can be used in research of cancer.
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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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HDAC-IN-91
0 ImagesCat. No.: HY-175021HDAC-IN-91 is a multiple inhibitor of HDAC (IC50 = 134.22 nM for HDAC1, 66.29 nM for HDAC2), carbonic anhydrase (CA) (Ki = 72.03 nM for CA IX, 50.76 nM for XII), and tubulin polymerization ( IC50 = 2.56 μM). HDAC-IN-91 inhibits PARP1 and increases the Bax/Bcl-2 ratio. HDAC-IN-91 blocks the cell cycle at the G2/M phase and induces apoptosis through a mitochondrial apoptosis activation mechanism. HDAC-IN-91 can exert potent cytotoxic activity through tubulin polymerization inhibition. HDAC-IN-91 can be used in breast, colorectal, cervical and lung cancer research.
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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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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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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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HDAC8-IN-17
0 ImagesCat. No.: HY-187382HDAC8-IN-17 is a histone deacetylase 8 inhibitor with human IC50 values of 0.08 μM, 0.44 μM, and 1.9 μM, and high selectivity over HDAC1, HDAC2, HDAC3, and HDAC6. HDAC8-IN-17 exhibits slow-binding, reversible uncompetitive inhibition via allosteric binding to the enzyme-substrate complex. HDAC8-IN-17 induces selective hyperacetylation of SMC3. HDAC8-IN-17 can be used for the research of cancer.
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PARP-1/HDAC-IN-1
0 ImagesCat. No.: HY-146160CAS No.: 3032621-10-3PARP-1/HDAC-IN-1 is a PARP-1/HDAC6 dual targeting inhibitor with IC50s of 68.90 nM and 510 nM, respectively. PARP-1/HDAC-IN-1 displays remarkable anticancer, anti-migration and anti-angiogenesis activities.
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HDAC6-IN-47
0 ImagesCat. No.: HY-163834HDAC6-IN-47 (Compound S-29b) is inhibitor for HDAC, which exhibits high affinities to HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, HDAC10 with Ki of 60, 56, 162, 0.44, 362 and 849 nM, respectively. HDAC6-IN-47 causes tubulin hyperacetylation in MV4-11, inhibits the proliferation of MV4-11 with an EC50 of 0.50 µM. HDAC6-IN-47 can be used in research of leukemia.
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GSK-3β/HDAC-IN-2
0 ImagesCat. No.: HY-174398GSK-3β/HDAC-IN-2 is a potent inhibitor of GSK-3β (IC50 = 0.04 μM), HDAC2 (IC50 = 1.05 μM, Ki = 0.070 μM) and HDAC6 (IC50 = 1.52 μM, Ki = 0.017 μM). GSK-3β/HDAC-IN-2 inhibits HDAC2 and HDAC6 activities and blocks tau hyperphosphorylation. GSK-3β/HDAC-IN-2 exerts neuroprotective effects and shows no significant toxicity. GSK-3β/HDAC-IN-2 can be used in the research of Alzheimer's disease.
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HDAC-IN-31
0 ImagesCat. No.: HY-144293CAS No.: 1916505-13-9HDAC-IN-31 is a potent, selective and orally active HDAC inhibitor with IC50s of 84.90, 168.0, 442.7, >10000 nM for HDAC1, HDAC2, HDAC3, HDAC8, respectively. HDAC-IN-31 induces apoptosis and cell cycle arrests at G2/M phase. HDAC-IN-31 shows good antitumor efficacy. HDAC-IN-31 has the potential for the research of diffuse large B-cell lymphoma.
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Largazole
0 ImagesCat. No.: HY-13906CAS No.: 1009815-87-5Synonyms: (+)-LargazoleLargazole ((+)-Largazole) is an orally active, blood-brain barrier-permeable class I histone deacetylase (HDAC) inhibitor with in vivo anticancer activity and osteogenic efficacy. As a prodrug, Largazole hydrolyzes to Largazole thiol (HY-170890), which has a Ki value of 0.07 nM against human HDAC2. Largazole regulates the cell cycle, induces apoptosis, upregulates tumor suppressors and osteoblast differentiation markers, inhibits osteoclast formation, and upregulates neuroprotection-related genes. Largazole can be used in the research of various cancers including colorectal cancer, as well as neurodegenerative diseases.
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HDAC ligand-5
0 ImagesCat. No.: HY-168864HDAC ligand-5 is a template for the non-selective HDAC inhibitor Vorinostat (HY-10221). HDAC ligand-5 can serve as a ligand for target protein (Ligands for Target Protein for PROTAC) for the development of PROTAC HDAC degraders with antitumor activity. HDAC ligand-5 can be used for the synthesis of FF2049 (HY-168863).
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HDAC6-IN-44
0 ImagesCat. No.: HY-162630HDAC6-IN-44 (compound H10) is a selective HDAC6 inhibitor with an IC50 value of 8.97 nM. HDAC6-IN-44 can inhibit the idiopathic pulmonary fibrosis (IPF) phenotype and exhibits antifibrotic activity. Additionally, HDAC6-IN-44 reduces fibrogenesis in a bleomycin-induced pulmonary fibrosis mouse model and demonstrates good metabolic stability. HDAC6-IN-44 holds promise for research in the field of idiopathic pulmonary fibrosis.
