trichostatin A (VTR-297) / Vanda - LARVOL DELTA

Increasing global chromatin accessibility alone is insufficient to enhance global transcription during mouse zygotic gene activation. (PubMed, J Reprod Dev) - "Therefore, global chromatin accessibility was increased at each developmental stage using two mechanistically distinct perturbations, KDM4D-mediated removal of H3K9me3 and trichostatin A (TSA)-mediated histone hyperacetylation, and the resulting accessibility and transcription were evaluated by DNase-TUNEL and 5-ethynyl uridine incorporation, respectively...The transcriptional response depended on the mechanism of chromatin perturbation. Furthermore, maternally enriched H3K9me3 did not account for the lower transcriptional activity in the maternal pronucleus."

Journal • Preclinical • KDM4D

PPARGC1A as an Epigenetic Biomarker of Differentiation in Differentiated Thyroid Cancer (ETA 2026) - "Similarly, thyroid cancer redifferentiation models, including treatments with LY294002 (PI3K inhibitor), PD325901 (ERK/MAPK inhibitor), Trichostatin A (histone deacetylase inhibitor) and 5-azacytidine (DNA methyltransferase inhibitor), also resulted in an increased PPARGC1A expression alongside the TDS, reinforcing the link between PPARGC1A and differentiation state. In conclusion, we have identified PPARGC1A as an epigenetic factor with a great potential as a biomarker of differentiation in DTC. Understanding its role may provide new insights into tumour dedifferentiation and open new avenues for therapeutic strategies in advanced thyroid carcinomas."

Biomarker • Oncology • Solid Tumor • Thyroid Gland Carcinoma • PPARGC1A

Beyond bioactivity: Chitosan macromolecular coatings on titanium surfaces drive osseointegration and immune suppression through targeted epigenetic regulation. (PubMed, Iran J Basic Med Sci) - "This coating utilizes a chitosan (CH) matrix to deliver epigenetic pharmaceuticals, 5-azacytidine (AZ) and trichostatin A (TR), onto Ti surfaces (AZ/TR-CH@TI). This macromolecular epigenetic drug-loaded CH coating effectively mitigates inflammation while simultaneously stimulating bone formation. The AZ/TR-CH@TI system presents a highly promising therapeutic approach to improve Ti osseointegration for clinical orthopaedic and dental applications."

Journal • Inflammation • Orthopedics • BMP2 • IL6 • RUNX2 • TNFA

Identification and Validation of Candidate Biomarkers Co-expressed with Creatine Metabolism-Related Genes in Ischemic Stroke Based on Transcriptomics Data. (PubMed, Mol Neurobiol) - "Further screening highlighted cyclosporin A and trichostatin A as drugs that could simultaneously target both candidate biomarkers. This study identified F12 and PLXDC2 as candidate biomarkers co-expressed with CMRGs, offering preliminary insights that warrant further investigation in larger cohorts."

Biomarker • Journal • Cardiovascular • Ischemic stroke

The upper airway microbiome related to asthma exacerbations is associated with leukocyte methylation markers linked to immunity, inflammation, and asthma comorbidities (ERS 2026) - "We observed an enrichment of CpGs related to asthma, atopy, air pollution, and smoking, and genes implicated in asthma-associated pathways (Wnt, TGF-β), comorbidities (type 2 diabetes and rheumatoid arthritis), and regulated by trichostatin A, a potential asthma drug. We revealed novel associations between blood DNAm and the upper airway microbiome linked to asthma exacerbations, implicating immunoinflammatory pathways and asthma comorbidities, and supporting a role for microbiome–epigenome interactions in asthma. Funding: Fundación DISA (009/2024), MICIU/AEI/10.13039/501100011033, FEDER, UE (PID2024-160302OB-I00), Catalina Ruiz (ACIISI)."

Asthma • Diabetes • Immunology • Inflammation • Inflammatory Arthritis • Metabolic Disorders • Respiratory Diseases • Rheumatoid Arthritis • Type 2 Diabetes Mellitus • FOXA2 • TGFB1

Transient histone deacetylase inhibition reveals cell type invariant and specific effects of chromatin decondensation on irradiation response. (PubMed, Front Cell Dev Biol) - "Here, we show that transient (2 h) trichostatin A (TSA) treatment of cancerous and non-tumorigenic breast epithelial cell lines increases immediate DNA damage and decreases long term cell viability in both cell types at high radiation doses...This suggests that chromatin decompaction acts to increase cellular vulnerability to initial DNA damage from high doses of radiation in a cell type independent manner that does not rely on changes to DNA repair pathways caused by longer TSA treatment. However, responses to lower doses of radiation and long term survival are more cell type specific: only MCF7 cells experience an effect of TSA on DNA damage after 1 Gy X-ray radiation while MCF10a cells experience somewhat more evident cell viability effects of combined TSA and radiation treatment long term."

Journal • Breast Cancer • Melanoma • Oncology • Solid Tumor

Trichostatin A ameliorates ulcerative colitis via the SERPINB5-mediated MMP9/RLN2 signaling pathway. (PubMed, Pathol Res Pract) - "TSA improves ulcerative colitis by targeting the SERPINB5-MMP9-RLN2 signaling axis, thereby suppressing inflammation, oxidative stress, and apoptosis while preserving intestinal barrier integrity."

Journal • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Bowel Disease • Targeted Protein Degradation • Ulcerative Colitis • CDH1 • IL17A • IL1B • IL6 • MMP9 • OCLN • RLN2 • SERPINB5 • TJP1 • TNFA

Trichostatin A Inhibits Cytokines Released in LPS-Induced THP-1 Cells via Downregulating Deacetylated-Syntaxin 17 and Promoting Autophagosome-Lysosome Fusion. (PubMed, Physiol Res) - "Furthermore, network pharmacology analysis revealed an inner relationship concerning HDAC2 between TSA and sepsis. Therefore, TSA can be considered a potential drug to cure sepsis-related diseases."

Journal • Infectious Disease • Septic Shock • HDAC2 • IL6

The HDAC Inhibitor Butyrate Reduces SOD1 Aggregation and Improves Motor Function in C. elegans and Cellular Models of ALS. (PubMed, Int J Cell Biol) - "Mechanistically, NaB recapitulated the effects of the pan-HDAC inhibitor trichostatin A, suggesting HDAC inhibition as key to reducing Sod1 aggregation and its downstream effects...These findings support a conserved neuroprotective role for NaB and HDAC inhibitors via their antiaggregation activity. Our findings also verify C. elegans and neuroblastoma cell lines as excellent research tools to explore the mechanisms underlying the antiaggregation action of NaB and HDAC inhibitors, as well as their potential for future therapeutic development."

Journal • Amyotrophic Lateral Sclerosis • CNS Disorders • Neuroblastoma • Oncology • Solid Tumor • SOD1

Inhibition of HOX/PBX Dimers as a Potential Therapeutic Strategy in Breast Cancer Subtypes Including Triple Negative Breast Cancer. (PubMed, Curr Issues Mol Biol) - "Combination studies were performed with epigenetic modifiers (5-azacytidine (5-aza), Trichostatin A (TSA)) and standard-of-care chemotherapeutic drugs including Paclitaxel. We further demonstrate that HTL-001 can significantly reduce tumour growth in a mouse model of TNBC. Our findings indicate that HOX/PBX dimers are a potential therapeutic target in this cancer."

Journal • Breast Cancer • Hematological Malignancies • Leukemia • Oncology • Solid Tumor • Triple Negative Breast Cancer

INO80E Suppresses Oxidized LDL-Induced Endothelial Apoptosis Through HDAC1-Mediated Stabilization of YY1. (PubMed, Biomolecules) - "These findings suggest that INO80E protects endothelial cells from ox-LDL-induced apoptosis, at least in part by promoting HDAC-associated YY1 deacetylation and stabilization. The INO80E-HDAC1-YY1 pathway may represent a candidate protective mechanism in AS that requires further validation."

IO biomarker • Journal • Atherosclerosis • Cardiovascular • APOE • BAX • BCL2 • HDAC1 • INO80 • YY1

Trichostatin A Modulates Ethanol Consumption and Reveals Dose- and Sex-Specific Transcriptomic Signatures in the Nucleus Accumbens Shell. (PubMed, Cells) - "GSEA analysis has identified additional gene sets, hallmark genes and microRNAs, and functions including immune response, metabolism, and estrogen response significantly associated with TSA treatment. This study successfully identified gene expression evidence that TSA treatment is sex- and dose-specific, underscoring the importance of considering both variables in the development of HDAC-targeted therapies for alcohol use disorders."

Journal • Addiction (Opioid and Alcohol) • CNS Disorders • Psychiatry • BDNF • ER • FKBP5 • IL1B

Identification and Validation of Mannose Metabolism-Related Biomarkers in COPD Through Integrated Bioinformatics and Machine Learning Analysis: A Pilot Study. (PubMed, Int J Chron Obstruct Pulmon Dis) - "Finally, drug prediction revealed 12 and 3 potential drugs for MAN1C1 and MAN2B2, respectively, with trichostatin A showing a potential binding conformation. This study revealed the potential roles of MMRGs in COPD and identified novel biomarkers. These findings provided new insights and research foundations for the early diagnosis, personalized treatment, and drug development of COPD."

Biomarker • Journal • Chronic Obstructive Pulmonary Disease • Immunology • Pulmonary Disease • Respiratory Diseases

Epigenetic Activation of Silent Pathways in Endophytic Aspergillus sp. EGP214 Reveals Porphyrin-Derived Antimicrobial Metabolites Targeting DNA Gyrase: In Vitro and In Silico Evaluation. (PubMed, Microb Pathog) - "The expression of cryptic genes needed stimulation through the use of two epigenetic modifiers, which included trichostatin A as a histone deacetylase inhibitor and 5-aza-2'-deoxycytidine as a DNA methyltransferase inhibitor, during fermentation...The evaluation of ADMET characteristics and toxicity levels showed moderate lipophilicity, together with minimal systemic toxicity but restricted oral bioavailability. The research shows that epigenetic modulation serves as an effective method to activate dormant fungal biosynthetic pathways, which produce valuable secondary compounds with antimicrobial and antioxidant properties."

Journal • Preclinical

Identification and validation of glycosaminoglycan metabolism-associated immune biomarkers in patients with ischemic stroke based on weighted gene co-expression network analysis and machine learning. (PubMed, Front Neurol) - "Drug-gene interaction analysis identified trichostatin A as a shared molecular target...MCEMP1, PRRG4, and VSIG4 constitute reliable molecular indicators that link systemic GAG metabolic dysregulation to IS-associated immune reorganization. These findings advance our mechanistic understanding of GAG-mediated inflammatory networks in stroke and establish actionable targets for both clinical risk stratification and therapeutic development."

Biomarker • Journal • Cardiovascular • Inflammation • Ischemic stroke • Metabolic Disorders • CD8

COPZ2 and KDELR3 are Linked to Stromal Inflammation and Metabolic Reprogramming in Osteoarthritis. (PubMed, Curr Med Chem) - "Our findings suggest that COPZ2 and KDELR3 may serve as potential regulators of the pathogenic fibroblast phenotype in OA. KDELR3 warrants further investigation as a potential drug-related target, and Trichostatin A should be regarded as a computationally predicted candidate compound rather than a validated inhibitor."

Journal • Immunology • Inflammation • Osteoarthritis • Pain • Rheumatology • KDELR3 • TNFA

Discovery and validation of programmed cell death-associated key biomarker genes in ischemic stroke via ssGSEA/WGCNA and LASSO-SVM-RFE. (PubMed, Front Mol Biosci) - "Enrichr/DSigDB prioritization and docking highlighted papaverine (CREBBP) and trichostatin A (ANTXR2) as plausible leads. An integrative network-ML framework delineated a peripheral-blood pan-PCD-related transcriptional pattern in IS and prioritized three biomarkers with consistent diagnostic performance and a neutrophil-skewed immune context. The exploratory pathway-gene-drug framework proposed here nominates testable compounds and provides a basis for prospective multi-cohort validation and mechanistic studies."

Biomarker • Journal • Cardiovascular • Inflammation • Ischemic stroke • CREBBP

Histone deacetylase inhibition alters mRNA expression of cell cycle- and senescence-associated genes in primary equine chondrocytes. (PubMed, Res Vet Sci) - "We have inspected transcriptomic data of equine primary chondrocytes of the 4th passage expanded in a 2D culture system, stimulated with a low dose of trichostatin A (TSA) - a common histone deacetylase inhibitor (HDACi), to identify senescence-associated transcriptional response...Selective upregulation of immune-related genes in TSA-stimulated chondrocytes may reflect TSA-mediated modulation of the senescence-associated transcriptional response. The obtained results contribute to ongoing discussions regarding the use of HDACi as a therapeutic agent for the treatment of damaged articular cartilage."

Journal • Inflammation • CDK4 • CDKN2A

Histone Acetylation Differentially Modulates CTCF-CTCF Loops and Intra-TAD Interactions. (PubMed, Nat Commun) - "Here, we show that histone hyperacetylation induced by trichostatin A (TSA) selectively disrupts short-range intra-TAD interactions while largely preserving CTCF-anchored loops...We further identify a TSA-sensitive cohesin fraction at CTCF sites, suggesting transient, non-encircling intermediates. Together, our results reveal that cohesin exists in distinct biochemical states that differentially regulate chromatin loop stability and responsiveness to epigenomic perturbation."

Journal • RAD21

WGCNA combined with machine learning identifies histone deacetylation-related diagnostic features for pediatric septic shock. (PubMed, Korean J Physiol Pharmacol) - "Immunoprecipitation preliminarily evaluated protein acetylation changes after trichostatin A treatment...Multiple potentially interacting transcription factors and miRNAs were also identified. C9orf84, ASAP1-IT1, and CREB5 may serve as diagnostic biomarkers and therapeutic targets for pediatric septic shock."

Journal • Infectious Disease • Pediatrics • Septic Shock • ASAP1 • CREB5

Epigenetic Signatures of Frailty: A Systematic Review, Meta-Analysis, and Network Analysis of the Chemical Exposome. (PubMed, Int J Mol Sci) - "Indeed, these genes are significantly enriched in pathways including thrombin signaling, G protein-coupled receptor signaling, and immune cell differentiation signaling. Finally, our system toxicology analysis demonstrated that arsenite, bisphenol A, benzamide, dorsomorphin, and trichostatin A directly interact with the four shared genes, suggesting that the chemical exposome contributes to the observed epigenetic heterogeneity of frailty and the concomitant clinical manifestations."

Clinical • Journal • Retrospective data • Review • Geriatric Disorders • CDC42BPB • RXRB • SLC1A5

Trichostatin A Improves Impaired Autophagic Flux Associated with ERK/FoxO3a Signaling to Alleviate Acute Pancreatitis. (PubMed, Eur J Pharmacol) - "In conclusion, TSA alleviates AP-associated injury by improving impaired autophagic flux, which may be associated with inhibition of ERK phosphorylation and modulation of FoxO3a-related signaling. These findings highlight the ERK/FoxO3a axis as a potential regulatory pathway involved in AP pathology and a possible therapeutic target."

Journal • Inflammation • Pancreatitis • IL6 • TNFA

Profile of lysine acetylation in Eimeria tenella and its potential implications for anticoccidial research. (PubMed, Parasit Vectors) - "This study is the first to investigate the anticoccidial effect of deacetylase inhibitors, providing a new strategy for the prevention and control of coccidiosis."

Journal

Activatable fluorescent nanosensor for real-time detection and intracellular imaging of histone deacetylase 1. (PubMed, Anal Bioanal Chem) - "Meanwhile, the sensing system was effectively utilized to precisely detect HDAC1 in the serum of humans, quantitatively assess the inhibitory effect of trichostatin A (TSA), and achieve intracellular fluorescence imaging of endogenous HDAC1 in living cells. Featuring high sensitivity, favorable specificity, and simple operation, this fluorescent sensing strategy provides a promising and universal tool for clinical HDAC1 analysis, disease-related research and inhibitor screening."

Journal • HDAC1

Transcriptomic Analysis Of Trichostatin A Treatment Reveals Candidate Genes And Drug Repurposing Potential In Alzheimer's Disease (AAIC 2026) - No abstract available

Omic analysis • Alzheimer's Disease • CNS Disorders