HDAC3
HDAC3 (histone deacetylase 3) is a class I histone deacetylase that functions as a central epigenetic regulator of chromatin structure and transcriptional repression through its association with nuclear receptor corepressor complexes containing NCOR and SMRT[1][2]. Mechanistically, HDAC3 forms an enzymatically active complex with NCOR/SMRT and associated cofactors, enabling histone deacetylation and coordinated control of gene expression programs involved in metabolism, circadian regulation, and cellular homeostasis[2][3][4]. HDAC3 also participates in signal-responsive transcriptional regulation, including repression of the JNK pathway and modulation of inflammatory gene expression, linking epigenetic regulation to cellular stress and immune responses[5][6]. In disease models, dysregulation of HDAC3-dependent transcriptional networks has been associated with metabolic disorders, cardiovascular pathology, inflammatory diseases, and cancer-related transcriptional abnormalities[4][6]. HDAC3 is additionally required for normal embryonic development, organ function, and maintenance of metabolic processes, highlighting its broad physiological significance[4]. Compared with related class I HDAC isoforms, HDAC3 is distinguished by its obligate functional interaction with the NCOR/SMRT corepressor complex and its dependence on corepressor-mediated activation for full biological activity[1][2][7]. Structural and genetic studies further demonstrate that disruption of HDAC3-corepressor interactions compromises HDAC3 function in vivo, emphasizing a unique regulatory mechanism not shared to the same extent by other HDAC family members[7][3]. For experimental applications, selective HDAC3 inhibitors are widely used to investigate epigenetic control of inflammation, metabolism, and disease-associated transcriptional programs, while offering greater isoform specificity than pan-HDAC inhibition strategies[6][4].
References:
- [1]. Wen YD, et al. The histone deacetylase-3 complex contains nuclear receptor corepressors. Proc Natl Acad Sci U S A. 2000 Jun 20;97(13):7202-7. [Content Brief]
- [2]. Fischle W, et al. Enzymatic activity associated with class II HDACs is dependent on a multiprotein complex containing HDAC3 and SMRT/N-CoR. Mol Cell. 2002 Jan;9(1):45-57. [Content Brief]
- [3]. Watson PJ, et al. Structure of HDAC3 bound to co-repressor and inositol tetraphosphate. Nature. 2012 Jan 9;481(7381):335-40. [Content Brief]
- [4]. He R, et al. The role of HDAC3 and its inhibitors in regulation of oxidative stress and chronic diseases. Cell Death Discov. 2023 Apr 18;9(1):131. [Content Brief]
- [5]. Zhang J, et al. The N-CoR-HDAC3 nuclear receptor corepressor complex inhibits the JNK pathway through the integral subunit GPS2. Mol Cell. 2002 Mar;9(3):611-23. [Content Brief]
- [6]. Watson N, et al. The role of HDAC3 in inflammation: mechanisms and therapeutic implications. Front Immunol. 2024 Jul 10;15:1419685. [Content Brief]
- [7]. Rabezanahary H, et al. Live virus neutralizing antibodies against pre and post Omicron strains in food and retail workers in Québec, Canada. Heliyon. 2024 May 21;10(10):e31026. [Content Brief]
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HDAC3 Related Products (204)
Related Products (204)
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Antibodies (1)
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PIM-1/HDAC-IN-1
0 ImagesCat. No.: HY-143233CAS No.: 2897622-19-2PIM-1/HDAC-IN-1 (compound 4d) is a PIM-1 inhibitor, with an IC50 of 343.87 nM. PIM-1/HDAC-IN-1 has strong inhibitory activity and selectivity against HDAC 1 and HDAC 6, with IC50 values of 63.65 and 62.39 nM, respectively. PIM-1/HDAC-IN-1 exhibits apoptosis inducing potential in MCF-7 cell lines. PIM-1/HDAC-IN-1 shows pre-G1 apoptosis and cell cycle arrest at G2/M phase.
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HDAC6-IN-14
0 ImagesCat. No.: HY-151896CAS No.: 3023019-97-5
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ZG-126
0 ImagesCat. No.: HY-161778CAS No.: 3049802-32-3ZG-126 is an agonist for vitamin D receptor (VDR) and an inhibitor for histone deacetylase (HDAC) (IC50=0.63-67.6 μM). ZG-126 exhibits cytotoxicity in cancer cells MDA-MB-231 and 4T1. ZG-126 exhibits antitumor and anti-metastatic efficacy against melanoma and triple-negative breast cancer (TNBC) in mouse models. ZG-126 also exhibits anti-inflammatory activity, through the reduction of macrophage infiltration and immunosuppressive M2-polarization.
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NS06
0 ImagesCat. No.: HY-187511CAS No.: 3133892-41-5NS06 is a dual-target inhibitor of STAT3 and HDAC, with a Kd of 5.82 μM for human STAT3, an IC50 of 129.1 nM for human HDAC1, an IC50 of 451.2 nM for human HDAC3, and an IC50 of 230.4 nM for human HDAC6. NS06 binds to STAT3 to inhibit its phosphorylation without altering the total STAT3 level; it inhibits the enzymatic activity of HDAC via coordination with Zn2+ at the catalytic center of HDAC1 and increases the acetylation level of histone H3. NS06 induces cell apoptosis, inhibits cancer cell migration and colony formation, and exhibits antiproliferative activity against solid tumor cells and 3D tumor spheroid models. NS06 is applicable to solid tumor-related research.
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HDAC-IN-54
0 ImagesCat. No.: HY-153514CAS No.: 2098896-13-8HDAC-IN-54 is a HDAC inhibitor with an IC50 of 25 nM against human HDAC1, 66 nM against HDAC2, 6.5 nM against HDAC3, and 281 nM against HDAC6. HDAC-IN-54 induces acetylation of α-tubulin and histone H3. HDAC-IN-54 acts synergistically with cisplatin to induce cancer cell apoptosis. HDAC-IN-54 can be used in research related to head and neck cancer, ovarian cancer, and tongue squamous cell carcinoma.
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JN210
0 ImagesCat. No.: HY-189074JN210 is a dual inhibitor of DCN1 and HDAC, with an IC50 of 94.26 nM against human DCN1. JN210 disrupts the UBE2M-DCN1 protein-protein interaction, blocks the neddylation modification of cullin-RING ligases, inhibits HDAC activity and induces histone hyperacetylation. JN210 impairs DNA damage repair function, induces cell apoptosis, exerts cytotoxicity and inhibits tumor growth. JN210 can be used for the research of non-small cell lung cancer.
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HDAC-IN-49
0 ImagesCat. No.: HY-151897CAS No.: 3035173-63-5
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PI3K/HDAC-IN-4
0 ImagesCat. No.: HY-172889CAS No.: 3085191-45-0PI3K/HDAC-IN-4 (Compound 31f) is a PI3K/HDAC dual inhibitor (IC50: 0.2μM). PI3K/HDAC-IN-4 shows high selectivity for HDAC1-3 (IC50 values of 75.5 nM, 70.9 nM, and 1.9 nM, respectively). PI3K/HDAC-IN-4 is a potent PIK3 inhibitor with IC50 values of 2.5 nM, 80.5 nM, 10.0 nM, and 57.2 nM for PI3Kα, β, δ, and γ, respectively. PI3K/HDAC-IN-4 significantly induces tumor cell apoptosis by simultaneously inhibiting the PI3K/AKT/mTOR signaling pathway and HDAC1-3. PI3K/HDAC-IN-4 exhibits potent antiproliferative activity in a variety of tumor cell lines (e.g., MV4-11, Jeko-1, HL60, and MCF-7, with IC50 values of 0.2, 0.9, 0.8, and 1.5 μM, respectively). PI3K/HDAC-IN-4 can be used in the study of lymphoma and leukemia.
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HDAC1/3-IN-1
0 ImagesHDAC1/3-IN-1 is a selective HDAC1/3 inhibitor, with IC50 values of 256 nM and 340.3 nM against HDAC1 and HDAC3, respectively. HDAC1/3-IN-1 increases the SubG1 cell population and promotes apoptosis of glioma cells and glioblastoma stem cells. HDAC1/3-IN-1 can be used in studies related to glioblastoma.
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Quisinostat hydrochloride
0 ImagesCat. No.: HY-15433BCAS No.: 1083078-98-1Synonyms: JNJ26481585 hydrochlorideQuisinostat (JNJ-26481585) hydrochloride is a potent and orally active pan-HDAC inhibitor (HDACi), with IC50 values ranging from 0.11 nM to 0.64 nM for HDAC1, HDAC2, HDAC4, HDAC10 and HDAC11. Quisinostat hydrochloride has a broad spectrum antitumoral activity. Quisinostat hydrochloride can induce autophagy in neuroblastoma cells.
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HDAC-IN-47
0 ImagesCat. No.: HY-151443CAS No.: 3033608-94-2HDAC-IN-47 is an orally active inhibitor of histone deacetylase (HDAC), with IC50s of 19.75 nM (HDAC1), 5.63 nM (HDAC2), 40.27 nM (HDAC3), 57.8 nM (HDAC2), 302.73 nM (HDAC8), respectively. HDAC-IN-47 inhibits autophagy and induces apoptosis via the Bax/Bcl-2 and caspase-3 pathways. HDAC-IN-47 arrests cell cycle at G2/M phase, and shows anti-tumor efficacy in vivo.
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HDAC-IN-27
0 ImagesHDAC-IN-27 (Compound 11h) is a potent, orally active class I HDAC-selective inhibitor with IC50 values ranging from 0.43 to 3.01 nM against HDAC1-3. HDAC-IN-27 exhibits both in vivo and in vitro antitumor activity. HDAC-IN-27 demonstrates significant anti-proliferative activity against acute myeloid leukemia (AML) cell lines by inducing apoptosis and histone acetylation (AcHH3 and AcHH4). HDAC-IN-27 can be used for research in acute myeloid leukemia (AML).
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JPS014
0 ImagesCat. No.: HY-145815CAS No.: 2669785-76-4JPS014 is a PROTAC degrader targeting HDAC1, HDAC2 and HDAC3, with DC50 values of 0.91 μM, 4.19 μM and 0.64 μM, respectively. JPS014 recruits the VHL E3 ligase to mediate the ubiquitination and proteasomal degradation of HDAC1, HDAC2 and HDAC3. JPS014 acts as a submicromolar inhibitor of the HDAC1-CoREST, HDAC2-CoREST and HDAC3-SMRT complexes in vitro. JPS014 increases the level of H3K56ac, reduces the stability of LSD1 and SIN3A, and induces cell apoptosis (apoptosis). JPS014 can be used for the research of colon cancer.
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CM-444
0 ImagesCat. No.: HY-163803CAS No.: 2256079-52-2CM-444 is inhibitor for HDAC (IC50 is 6 nM-0.6 μM) and DNA methyltransferases (DNMT, IC50 is 1.8-2.3 μM). CM-444 is an inducer for the differentiation of acute myeloid leukemia cells. CM-444 exhibits anti-leukemic activity and improves the survival rate in mouse models.
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EGFR/HDAC-IN-2
0 ImagesCat. No.: HY-175805EGFR/HDAC-IN-2 (Compound 38) is dual-functional inhibitor of EGFR and HDAC3 with IC50s of 20.34 and 1.09 nM for CDK9 and HDAC3, respectively. EGFR/HDAC-IN-2 has superior anti-proliferative activity against cancer cells, inhibits cell migration and induces late-stage cell apoptosis. EGFR/HDAC-IN-2 significantly inhibits triple-negative breast cancer (TNBC) tumor growth in xenograft mouse models. EGFR/HDAC-IN-2 can be used for cancers like TNBC research.
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HDAC3-IN-7
0 ImagesCat. No.: HY-172601CAS No.: 3104610-92-3HDAC3-IN-7 (Compound 8ae) is a selective HDAC3 inhibitor with an IC50 value of 311 nM. HDAC3-IN-7 degrades PD-L1 through the lysosome pathway mediated by Cathepsin B, exerting activities such as inhibiting tumor cell proliferation, migration, and invasion. HDAC3-IN-7 is promising for research of cancers.
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HDAC6-IN-74
0 ImagesCat. No.: HY-181579HDAC6-IN-74 is an orally active, selective histone deacetylase 6 (HDAC6) inhibitor with an IC50 of 0.036 μM. HDAC6-IN-74 induces tumor cell apoptosis, arrests cells at the S phase of the cell cycle, and impairs cell migration, invasion and colony-forming abilities. HDAC6-IN-74 exerts anticancer effects with no obvious toxicity. HDAC6-IN-74 can be used in the research of cancers such as liver cancer.
