HDAC11
HDAC11 is the sole member of class IV histone deacetylases and represents the smallest zinc-dependent HDAC isoform, with distinctive catalytic properties that differentiate it from other HDAC family members[1][2]. Mechanistically, HDAC11 functions as an epigenetic regulator that controls gene expression through deacylation and deacetylation reactions, and accumulating evidence indicates that its long-chain fatty acid defatty-acylase activity is substantially more efficient than its intrinsic deacetylase activity[3][1]. Therefore, HDAC11 influences multiple biological pathways involved in immune regulation, metabolism, and cellular homeostasis[1][4]. In immune signaling, HDAC11 regulates interleukin-10 expression, immune tolerance, and type I interferon signaling, highlighting its role as a key modulator of inflammatory responses[5][6][7]. In metabolic systems, HDAC11 participates in adipogenesis, lipid metabolism, energy expenditure, and insulin-related processes, linking the enzyme to obesity and metabolic syndrome models[4][8]. Disease-associated studies further demonstrate involvement of HDAC11 in cancer, neuroinflammation, and immune-mediated disorders, supporting its relevance as a therapeutic target across diverse experimental settings[1][9]. Compared with related HDAC isoforms, HDAC11 exhibits unique substrate specificity and prominent defatty-acylase activity, providing a functional distinction that has stimulated intensive drug-discovery efforts[1][3]. For experimental applications, several selective HDAC11 inhibitors have been developed and are widely used as chemical probes to investigate HDAC11-dependent pathways and evaluate therapeutic potential in disease models[1][10].
References:
- [1]. Jia G, et al. Biological function and small molecule inhibitors of histone deacetylase 11. Eur J Med Chem. 2024 Oct 5;276:116634. [Content Brief]
- [2]. Ujlaky-Nagy L, et al. Disrupting EGFR-HER2 Transactivation by Pertuzumab in HER2-Positive Cancer: Quantitative Analysis Reveals EGFR Signal Input as Potential Predictor of Therapeutic Outcome. Int J Mol Sci. 2024 May 29;25(11):5978. [Content Brief]
- [3]. Núñez-Álvarez Y, et al. HDAC11: a multifaceted histone deacetylase with proficient fatty deacylase activity and its roles in physiological processes. FEBS J. 2022 May;289(10):2771-2792. [Content Brief]
- [4]. Chen H, et al. HDAC11, an emerging therapeutic target for metabolic disorders. Front Endocrinol (Lausanne). 2022 Oct 20;13:989305. [Content Brief]
- [5]. Villagra A, et al. The histone deacetylase HDAC11 regulates the expression of interleukin 10 and immune tolerance. Nat Immunol. 2009 Jan;10(1):92-100. [Content Brief]
- [6]. Cao J, et al. HDAC11 regulates type I interferon signaling through defatty-acylation of SHMT2. Proc Natl Acad Sci U S A. 2019 Mar 19;116(12):5487-5492. [Content Brief]
- [7]. Jung E, et al. Global analysis of AGO2-bound RNAs reveals that miRNAs induce cleavage of target RNAs with limited complementarity. Biochim Biophys Acta Gene Regul Mech. 2017 Nov;1860(11):1148-1158. [Content Brief]
- [8]. Skubisz MM, et al. Gefitinib and Methotrexate to Treat Ectopic Pregnancies with a Pre-Treatment Serum hCG 1000-10,000 IU/L: Phase II Open Label, Single Arm Multi-Centre Trial. EBioMedicine. 2018 Jul;33:276-281. [Content Brief]
- [9]. Liu Y, et al. HDAC11: A novel target for improved cancer therapy. Biomed Pharmacother. 2023 Oct;166:115418. [Content Brief]
- [10]. Ho TT, et al. Trapoxin A Analogue as a Selective Nanomolar Inhibitor of HDAC11. ACS Chem Biol. 2023 Apr 21;18(4):803-809. [Content Brief]
All Product Categories
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HDAC11 Related Products (71)
Related Products (71)
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HDAC6-IN-10
0 ImagesCat. No.: HY-150595CAS No.: 2408286-73-5HDAC6-IN-10 is a highly selective HDAC6 inhibitor with the IC50 of 0.73 nM. HDAC6-IN-10 has 144~10941-fold selectivity over other HDAC isoforms. HDAC6-IN-10 shows anti-proliferative activities against multiple myeloma cells.
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ALK/HDAC-IN-2
0 ImagesCat. No.: HY-180811ALK/HDAC-IN-2 (Compound 19b) is an ALK/HDAC inhibitor with IC₅₀ values for ALK WT and total HDACs of 8 nM and 1.18 μM, respectively. ALK/HDAC-IN-2 exhibits inhibitory activity against ALK mutants G1202R, F1174L, and L1196M, with IC₅₀ values of 2.74, 9.23, and 34.28 nM, respectively. ALK/HDAC-IN-2 shows potent and selective inhibition against HDAC1 (IC₅₀ = 0.24 μM), while its inhibitory activity against HDAC7, HDAC6, and HDAC11 is weak (IC₅₀ > 10 μM). ALK/HDAC-IN-2 has broad-spectrum anti-proliferative activity against various cancer cells, inducing cell cycle arrest and apoptosis. ALK/HDAC-IN-2 can be used for the study of neuroblastoma.
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HDAC-IN-43
0 ImagesCat. No.: HY-147966CAS No.: 1809163-24-3HDAC-IN-43 is a potent HDAC 1/3/6 inhibitor with IC50 values of 82, 45, and 24 nM, respectively. HDAC-IN-43 is a weak PI3K/mTOR inhibitors with IC50 values of 3.6 and 3.7 μM, respectively. HDAC-IN-43 shows broad anti-proliferative activity .
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MC2590
0 ImagesMC2590 is a potent pyridine-containing histone deacetylase (HDAC) inhibitor. MC2590 is a inhibitor of HDAC1-3, -6, -8, and -10 (class I/IIb-selective inhibitor) with IC50s of 0.015 μM-0.156 μM. MC2590 also inhibits HDAC isoforms HDAC4, HDAC5, HDAC7, HDAC9, HDAC11 with IC50s of 1.35 μM-3.98 μM. MC2625 induces G2/M cell cycle arrest and modulates pro- and anti-apoptotic microRNAs towards apoptosis induction.
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HDAC-IN-94
0 ImagesCat. No.: HY-179019HDAC-IN-94 is a potent, selective HDAC6 inhibitor (IC50 = 4.5 nM). HDAC-IN-94 shows >1000-fold selectivity over HDAC8 and shows minimal activity against other isoforms (HDAC1-3/10). HDAC-IN-94 induces α-tubulin hyperacetylation, apoptosis, and G2/M cell cycle arrest, exhibiting potent anti-tumor efficacy with low cytotoxicity. HDAC-IN-94 can be used for neuroblastoma and glioblastoma research.
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sEH/HDAC6-IN-1
0 ImagesCat. No.: HY-163207CAS No.: 2847838-67-7
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ZINC000028464438
0 ImagesCat. No.: HY-157889CAS No.: 866123-66-2
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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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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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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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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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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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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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G4/HDAC-IN-1
0 ImagesCat. No.: HY-151263CAS No.: 3031784-60-5G4/HDAC-IN-1 (compound a6) is a G4/HDAC dual-targeting compound. G4/HDAC-IN-1 inhibits intracellular HDAC activity with an IC50 value of 1.1 μM, and induces G4 formation. G4/HDAC-IN-1 inhibits TNBC proliferation and tumor growth in TNBC xenograft model. G4/HDAC-IN-1 can be used for the research of cancer.
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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.
