HDAC5
HDAC5 (histone deacetylase 5) is a member of the class IIa histone deacetylase family and functions as a signal-responsive transcriptional regulator through its conserved N-terminal transcription factor-binding domain and C-terminal catalytic domain[1][2]. HDAC5 interacts with transcription factors such as myocyte enhancer factor 2 (MEF2), and phosphorylation-dependent binding to 14-3-3 proteins promotes its nuclear export, thereby relieving transcriptional repression of target genes[1][2]. Mechanistically, HDAC5 participates in chromatin-dependent gene regulation and integrates extracellular signaling pathways that control cellular differentiation, survival, and tissue-specific transcriptional programs[2][3]. These properties place HDAC5 within a broader class IIa HDAC regulatory network that functions primarily through transcriptional repression complexes rather than strong intrinsic deacetylase activity[2]. In disease-related settings, aberrant HDAC5 expression has been reported across multiple cancer types, where it is associated with regulation of cell proliferation, invasion, stemness maintenance, immune-related processes, and cell-cycle progression[1]. Experimental studies summarized in cancer models further indicate that HDAC5 can influence oncogenic pathways including DLL4, Notch1, c-Met, and Six1 signaling, supporting its relevance as a molecular regulator of tumor biology[1]. Compared with related HDAC isoforms, HDAC5 shares the characteristic class IIa adaptor architecture and signal-dependent nucleocytoplasmic shuttling mechanism, yet retains distinct tissue distribution patterns and target-gene regulatory functions that contribute to biological specificity[1][2]. For experimental applications, HDAC5 is widely investigated as a candidate therapeutic target, and ongoing efforts to develop class IIa-selective HDAC modulators aim to improve isoform selectivity while minimizing off-target effects associated with pan-HDAC inhibition[2][3].
References:
- [1]. Yang J, et al. Insights Into the Function and Clinical Application of HDAC5 in Cancer Management. Front Oncol. 2021 Jun 10;11:661620. [Content Brief]
- [2]. 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]
- [3]. 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]
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HDAC5 Related Products (56)
Related Products (56)
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Nanatinostat
0 ImagesSynonyms: CHR-3996Nanatinostat (CHR-3996) is a potent, class I selective and orally active HDAC inhibitor with IC50s of 3 nM, 4 nM, and 7 nM for HDAC1, HDAC2, and HDAC3, respectively. Nanatinostat has low activity against HDAC5 (IC50 of 200 nM) and HDAC6 (IC50 of 2100 nM). Nanatinostat induces apoptosis in myeloma cells. Nanatinostat has potent anticancer effects, such as myeloma, advanced solid tumours and colorectal cancer.
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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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KR-39038
0 ImagesKR-39038 is an orally active and potent GRK5 (G protein-coupled receptor kinase 5) inhibitor, with an IC50 of 0.02 μM. KR-39038 significantly inhibits angiotensin II-induced cellular hypertrophy through suppression of HDAC5 pathway in neonatal cardiomyocytes. KR-39038 shows profound anti-hypertrophic effects and improved cardiac function. KR-39038 can be used for heart failure research.
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Domatinostat tosylate
0 ImagesSynonyms: 4SC-202
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G194-0712
0 ImagesG194-0712 is a selective histone deacetylase 5 (HDAC5) activator with an EC50 of 7.96 μM and a Kd of 2.53 μM. G194-0712 restores ACTN4-K417 deacetylation and nuclear import, and increases CSTA expression. G194-0712 accelerates wound closure in chronic wound models, reducing wound area and epithelial gap. G194-0712 can be used for the research of chronic skin wounds, such as diabetic wounds, ischemic wounds, radiation injury wounds.
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BRD 4354 ditrifluoroacetate
0 ImagesCat. No.: HY-112719BCAS No.: 2444837-63-0
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SAP15 acetate
0 ImagesCat. No.: HY-P10462APurity: 98.04%Synonyms: Synthetic anti-inflammatory peptide 15 acetateSAP15 (Synthetic anti-inflammatory peptide 15) acetate is a synthetic anti-inflammatory peptide consisting of 15 amino acids designed from human beta-defensin 3. SAP15 acetate has the ability to penetrate cells and is able to induce downregulation of intracellular inflammation. SAP15 acetate inhibits inflammation by inhibiting the phosphorylation of HDAC5 and thereby reducing the phosphorylation of NF-κB p65. SAP15 acetate inhibits HDAC5 and NF-κB p65 phosphorylation in LPS (HY-D1056)-induced macrophages. SAP15 acetate increases the expression of aggrecan and type II collagen and decreases the expression of osteocalcin in LPS-induced chondrocytes. SAP15 acetate can be used in the study of inflammation regulation and anti-inflammatory therapy of biomaterials.
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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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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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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.
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HDAC6-IN-6
0 ImagesCat. No.: HY-146679CAS No.: 2413603-10-6HDAC6-IN-6 (compound 6a) is a potent and BBB-penetrated HDAC6 inhibitor, with an IC50 of 0.025 μM. HDAC6-IN-6 exhibits strong inhibitory activity against Aβ1-42 self-aggregation and AChE, with IC50 values of 3.0 and 0.72 μM. HDAC6-IN-6 can enhance neurite outgrowth without significant neurotoxicity.
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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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SAP15
0 ImagesCat. No.: HY-P10462CAS No.: 1403753-45-6Synonyms: Synthetic anti-inflammatory peptide 15SAP15 (Synthetic anti-inflammatory peptide 15) is a synthetic anti-inflammatory peptide consisting of 15 amino acids designed from human beta-defensin 3. SAP15 has the ability to penetrate cells and is able to induce downregulation of intracellular inflammation. SAP15 inhibits inflammation by inhibiting the phosphorylation of HDAC5 and thereby reducing the phosphorylation of NF-κB p65. SAP15 inhibits HDAC5 and NF-κB p65 phosphorylation in LPS (HY-D1056)-induced macrophages. SAP15 increases the expression of aggrecan and type II collagen and decreases the expression of osteocalcin in LPS-induced chondrocytes. SAP15 can be used in the study of inflammation regulation and anti-inflammatory therapy of biomaterials.
