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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Bavarostat
0 ImagesSynonyms: EKZ-001Bavarostat (EKZ-001) is a blood-brain barrier-permeable, potent HDAC6 inhibitor and PET radiotracer, with an IC50 as low as 17 nM against human HDAC6. Bavarostat can be labeled with 18F and used as a probe to map HDAC6 distribution and measure target occupancy in the brains of non-human primates. Bavarostat also selectively modulates tubulin acetylation, but not histone acetylation. Bavarostat is applicable for research on Alzheimer's disease, other neurodegenerative disorders, and cancers.
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TD034
0 ImagesTD034 is a selective, reversible and noncovalent HDAC11 inhibitor with an IC50 of 5.1 nM and a Ki of 1.5 nM. TD034 does not inhibit other HDACs or sirtuins. TD034 inhibits the defatty acylation of SHMT2 (HDAC11 substrate). TD034 decreases the YAP1 level via HDAC11 inhibition. TD034 can be used for the study of lung cancer.
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MIR002
0 ImagesMIR002 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. MIR002 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. MIR002 shows significant antitumor activity in vivo.
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HDAC11-IN-2
0 ImagesHDAC11-IN-2 (compound B6) is a high selective Histone Deacetylase 11 (HDAC11) inhibitor. HDAC11-IN-2 inhibits HDAC11 and HDAC8 with IC50s of 51.1 ×10-3 μM and 5 μM, respectively. HDAC11-IN-2 inhibits denovolipogenesis (DNL) and promotes fatty acid oxidation, thus mitigating hepaticlipid accumulation and pathological symptoms in MASLD mice. HDAC11-IN-2 enhances the phosphorylation of AMPKα1 at Thr172 through the inhibition of HDAC11, consequently modulating DNL and fatty acid oxidation in the liver.
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GEM144
0 ImagesCat. No.: HY-143411CAS No.: 2487526-28-1GEM144 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. GEM144 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. GEM144 has significant antitumor activity in human orthotopic malignant pleural mesothelioma xenografts.
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Domatinostat tosylate
0 ImagesSynonyms: 4SC-202
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MC1742
0 ImagesMC1742 is a potent HDAC inhibitor, with IC50s of 0.1 μM, 0.11 μM, 0.02 μM, 0.007 μM, 0.61 μM, 0.04 μM and 0.1 μM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, HDAC10 and HDAC11, respectively. MC1742 can increase acetyl-H3 and acetyl-tubulin levels and inhibits cancer stem cells growth. MC1742 can induce growth arrest, apoptosis, and differentiation in sarcoma CSC.
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HDAC11-IN-3
0 ImagesHDAC11-IN-3 (Compound A9) is a selective HDAC11 inhibitor (IC50: 4.1 nM). HDAC11-IN-3 has inhibitory effects on U937 and OCI-AML2 acute myeloid leukemia (AML) cell lines (IC50: 10 μM). HDAC11-IN-3 has significant anti-AML activity, inducing apoptosis, cell cycle arrest, and differentiation. HDAC11-IN-3 upregulates the iron transporters transferrin (TF) and transferrin receptor (TFRC), and activates the p62-Keap1-Nrf2-HMOX1 pathway, which together lead to increased intracellular iron levels and induce ferroptosis in AML cells. HDAC11-IN-3 can be used alone or in combination with Cytarabine (HY-13605) for AML research.
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AES-350
0 ImagesAES-350 is a potent and orally active HDAC6 inhibitor with an IC50 and a Ki of 0.0244 μM and 0.035 μM, respectively. AES-350 is also against HDAC3, HDAC8 in an enzymatic activity assay with IC50 values of 0.187 μM and 0.245 μM, respectively. AES-350 triggers apoptosis in AML cells through HDAC inhibition and can be used for acute myeloid leukemia (AML) research.
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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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HDAC-IN-36
0 ImagesCat. No.: HY-146684CAS No.: 2482992-54-9
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TNI-97
0 ImagesCat. No.: HY-175030CAS No.: 2790425-52-2TNI-97 is a selective and orally active HDAC6 inhibitor, with an IC50 of 0.2 nM. TNI-97 potently inhibited TNBC cell MDA-MB-453 growth and clonogenicity. TNI-97 induces PANoptosis including apoptosis, necroptosis and pyroptosis in MDA-MB-453 cells. TNI-97 shows antitumor activity in the mice carrying the MDA-MB-453 xenograft or carrying murine-derived TNBC cell allografts. TNI-97 can be used for the study of triple-negative breast cancer.
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HDACs/EZH2-IN-1
0 ImagesCat. No.: HY-169400HDACs/EZH2-IN-1 (Compound 22a) is a HDACs/EZH2 inhibitor (EZH2 Y641N inhibition rate at 50 nM: 98%), with selective inhibition against HDAC1 and HDAC6 (IC50: 0.23 μM and 0.07 μM, respectively). HDACs/EZH2-IN-1 exerts a antiproliferative effect on diffuse large B-cell lymphoma cells harboring an EZH2 mutation and on various acute myeloid leukemia cells. HDACs/EZH2-IN-1 has the ability to induce cell differentiation and Apoptosis.
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Wee1/HDAC-IN-1
0 ImagesCat. No.: HY-179272CAS No.: 3037071-29-4Wee1/HDAC-IN-1 is a dual Wee1/HDAC inhibitor with an IC50 of 1.2 nM for Wee1 and IC50 values of 196 nM for HDAC1, 156 nM for HDAC3, and 55 nM for HDAC6. Wee1/HDAC-IN-1 exhibits strong antiproliferative activity against MV4-11 cells with an IC50 of 0.076 μM. Wee1/HDAC-IN-1 selectively binds to Wee1 and HDACs. Wee1/HDAC-IN-1 interferes with DNA damage repair pathways and induces apoptosis in MV4-11 cells. Wee1/HDAC-IN-1 Wee1/HDAC-IN-1 can be used for the research of acute myeloid leukemia (AML).
