HDAC

HDAC2-IN-2 is a selective inhibitor of histone deacetylase 2 (HDAC2), exhibiting a Kd value ranging from 0.1 to 1 μM. This compound is instrumental in studying the role of HDAC2 in various biological processes, including gene expression regulation and cell differentiation. Its inhibitory action makes it a valuable tool for researchers investigating epigenetic modifications and potential therapeutic targets in cancer and neurodegenerative diseases.

LSD1/HDAC6-IN-2 is a potent inhibitor targeting LSD1, HDAC6, and MAO-A, with IC50 values of 5 nM, 11 nM, and 5 nM, respectively. It demonstrates significant inhibitory effects on the growth of multiple myeloma cell lines, including MM.1S, MM.1R, and RPMI-8226. This compound is suitable for research applications focused on acute myeloid leukemia and lymphoma, providing insights into potential therapeutic mechanisms.

PT3 is a selective inhibitor of histone deacetylase 3 (HDAC3), demonstrating an IC50 value of 0.25 μM. This compound shows promising brain penetration capabilities and bioavailability following oral administration. PT3 is valuable for investigating the role of HDAC3 in neurodegenerative disorders, particularly in the context of Alzheimer’s disease research.

Ac-Arg-Gly-Lys(Ac)-AMC is a substrate specifically designed for the study of histone deacetylases (HDACs). It serves as a useful tool for measuring HDAC activity in various biological assays. This compound is instrumental in investigating the role of HDACs in cellular processes, as well as drug development related to cancer and other diseases where HDAC modulation may be therapeutic.

(E,E)-RGFP966 is a selective inhibitor of Histone Deacetylase 3 (HDAC3) that is capable of penetrating the central nervous system. This compound is particularly relevant for the investigation of neurodegenerative disorders, including Huntington's disease. Its specificity for HDAC3 makes it a valuable tool in studying the epigenetic regulation of gene expression and the accompanying mechanistic pathways involved in this condition.

DNMT/HDAC-IN-1 is a dual inhibitor targeting DNA methyltransferases (DNMT) and histone deacetylases (HDACs), demonstrating IC50 values of 56.84 nM for HDAC1 and 17.39 nM for HDAC6. This compound induces apoptosis in tumor cells and is valuable for cancer research applications, providing insights into the mechanisms of epigenetic regulation in malignancies. Its role in modulating both DNMT and HDAC activities makes it a significant tool for investigating therapeutic strategies in oncology.

HDAC1-IN-7 is a potent inhibitor of histone deacetylase 1 (HDAC1), exhibiting an IC50 of 0.957 mM. This compound serves as a valuable tool for investigating the role of HDAC1 in various biological processes, including gene expression regulation and cellular differentiation. Its application is relevant in studies of cancer biology and neurodegenerative disorders, where modulation of HDAC1 activity may provide insights into therapeutic strategies.

HDAC11-IN-2 is a selective inhibitor of Histone Deacetylase 11 (HDAC11), exhibiting an IC50 of 51.1 µM for HDAC11 and 5 µM for HDAC8. This compound effectively inhibits de novo lipogenesis and promotes fatty acid oxidation, addressing hepatic lipid accumulation and its associated pathological features in MASLD mouse models. Additionally, HDAC11-IN-2 enhances the phosphorylation of AMPKα1 at Thr172, further regulating metabolic pathways involved in lipid metabolism within the liver.

Bavarostat is a potent inhibitor of histone deacetylase 6 (HDAC6) with an IC50 of 17 nM, capable of crossing the blood-brain barrier. As a PET radiotracer, it can be labeled with 18F for in vivo mapping of HDAC6 distribution and assessing target occupancy in non-human primate models. Bavarostat selectively enhances tubulin acetylation without affecting histone acetylation, making it a valuable tool for research into neurodegenerative diseases, such as Alzheimer’s, as well as various cancers.

HDAC6 Degrader-3 is a selective inhibitor that promotes the degradation of histone deacetylase 6 (HDAC6) through ternary complex formation and the ubiquitin-proteasome pathway, exhibiting a DC50 value of 19.4 nM. With IC50 values of 4.54 nM for HDAC6 and 0.647 μM for HDAC1, it effectively induces significant hyperacetylation of α-tubulin. This compound is valuable for research applications focused on neurodegenerative diseases and cancer, where modulation of HDAC6 activity may play a critical role.

HD-TAC7 is a highly effective PROTAC HDAC degrader, specifically targeting histone deacetylases HDAC1, HDAC2, and HDAC3 with IC50 values of 3.6 μM, 4.2 μM, and 1.1 μM, respectively. This compound has demonstrated the ability to reduce NF-κB p65 levels in RAW 264.7 macrophages. HD-TAC7 is suitable for research applications focused on inflammatory diseases, including asthma and chronic obstructive pulmonary disease (COPD).

TD034 is a selective, reversible, and noncovalent inhibitor of HDAC11, exhibiting an IC50 value of 5.1 nM and a Ki of 1.5 nM. This compound specifically targets HDAC11 without affecting other histone deacetylases or sirtuins, and it inhibits the defatty acylation of the substrate SHMT2. Additionally, TD034 reduces the levels of YAP1 through its action on HDAC11. This reagent is suitable for investigating the role of HDAC11 in lung cancer research.

HDAC6-IN-3 is a potent inhibitor of histone deacetylase 6 (HDAC6), with an IC50 ranging from 0.02 to 1.54 μM for various HDAC isoforms, including HDAC1, HDAC2, HDAC3, and HDAC8. Additionally, it exhibits significant inhibitory activity against monoamine oxidase A (MAO-A) with an IC50 of 0.79 μM and lysine-specific demethylase 1 (LSD1). This compound serves as a valuable tool for research applications in cancer biology and epigenetics and is equipped with an alkyne functionality, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc).

HDAC6-IN-23 is a potent inhibitor of the histone deacetylase HDAC6, exhibiting oral bioavailability. This compound demonstrates significant biological activity by modulating histone acetylation, which plays a crucial role in gene regulation and cellular processes. It is primarily utilized in research focused on neurodegenerative disorders, cancer therapy, and the study of protein homeostasis.

HDAC Ligand-1 is a selective histone deacetylase (HDAC) ligand that serves as a valuable building block for the synthesis of PROTAC HDAC degraders. This compound can facilitate the development of innovative therapeutic agents targeting HDAC enzymes, enhancing the understanding of their role in various biological processes. Its applications extend to cancer research and epigenetic studies, providing insights into the modulation of gene expression and cellular behavior.

HDAC-IN-4 is a selective inhibitor of HDAC6 and HDAC10, demonstrating pIC50 values of 7.2 and 6.8 in BRET assays, respectively. This compound exhibits antitumoral activity, making it a significant tool for the investigation of cancer biology and the modulation of gene expression. Its selective inhibition of these histone deacetylases positions HDAC-IN-4 as a valuable reagent for research focusing on epigenetic regulation and potential therapeutic applications in cancer treatment.

BG48 is a potent histone deacetylase (HDAC) inhibitor that selectively targets HDAC1 and HDAC2. By inhibiting the enzymatic activity of these enzymes, BG48 modulates gene expression and can influence cellular processes such as differentiation, proliferation, and apoptosis. This compound is valuable for research applications in cancer biology, neurodegenerative diseases, and epigenetic studies.

Purinostat is a selective inhibitor of histone deacetylases (HDAC) I and IIb, exhibiting potent anti-leukemic activity. It effectively reduces the survival of Philadelphia chromosome-positive leukemic cells and CD34+ leukemic progenitors from chronic myeloid leukemia patients. By targeting HDAC I/IIb, Purinostat disrupts critical pathways for leukemic stem cell survival, influencing factors such as c-Myc, β-Catenin, E2F, Ezh2, Alox5, and mTOR. Additionally, Purinostat enhances glutamate metabolism in leukemic stem cells by upregulating GLS1.

HNHA is a potent histone deacetylase (HDAC) inhibitor with an IC50 of 100 nM. The compound effectively induces cell cycle arrest at the G1/S phase through the upregulation of p21. HNHA has demonstrated the ability to inhibit tumor growth and neovascularization, suggesting potential applications in cancer research, particularly in the context of breast cancer therapeutics.

JPS036 is a benzamide-based HDAC degrader that operates through the Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimera (PROTAC) mechanism. This compound selectively degrades class I histone deacetylases (HDAC1 and HDAC2), demonstrating significant biological activity by promoting the expression of differentially expressed genes and enhancing apoptosis in HCT116 cells. JPS036 serves as a valuable research tool for studying the roles of HDACs in cellular processes and disease models.

HDAC-IN-40 is a potent alkoxyamide-based inhibitor of histone deacetylases (HDACs), specifically targeting HDAC2 and HDAC6 with Ki values of 60 nM and 30 nM, respectively. This compound exhibits significant antitumor activity, making it a valuable tool for cancer research. HDAC-IN-40 can be utilized to explore the role of histone deacetylation in tumor development and progression, as well as to investigate potential therapeutic interventions in various cancers.

BG47 is a selective inhibitor of histone deacetylases HDAC1 and HDAC2, functioning as an optoepigenetic probe. Upon light-induced trans-to-cis isomerization, BG47 competitively inhibits the deacetylase activity of its targets, resulting in increased acetylation of Histone H3K9. This compound is relevant for research applications in neurological diseases, providing insights into epigenetic regulation and its implications in various disorders.

HDAC6-IN-65 is a selective inhibitor of histone deacetylase 6 (HDAC6) with an IC50 of 0.9 nM, demonstrating additional inhibitory effects on HDAC3 with an IC50 of 39.4 nM. This compound induces the accumulation of acetylated α-tubulin and acetylated histone H3 in Neuro-2a cells, serving as a marker for class I HDAC inhibition. HDAC6-IN-65 provides valuable insights in the study of melanoma and related cancer research applications.

HDAC-IN-48 is a potent inhibitor of histone deacetylases (HDACs) that exhibits significant cytotoxicity, with a GI50 of approximately 20 nM. This hybrid molecule incorporates pharmacophores from SAHA and CETZOLE, effectively inducing ferroptosis while inhibiting HDAC activity. Additionally, HDAC-IN-48 features an alkyne group, allowing it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions, making it a valuable tool for click chemistry applications in chemical biology and therapeutic research.

HDAC11-IN-3 is a selective inhibitor of HDAC11, exhibiting an IC50 of 4.1 nM. This compound demonstrates potent anti-acute myeloid leukemia (AML) activity against U937 and OCI-AML2 cell lines with an IC50 of 10 μM. It effectively induces apoptosis, cell cycle arrest, and differentiation while upregulating iron transporters transferrin (TF) and transferrin receptor (TFRC). Additionally, HDAC11-IN-3 activates the p62-Keap1-Nrf2-HMOX1 pathway, resulting in elevated intracellular iron levels and subsequent ferroptosis in AML cells. This reagent is suited for studies investigating the molecular mechanisms of AML and can be utilized alone or in combination with other therapeutic agents like Cytarabine.

HDAC-IN-54 is a potent histone deacetylase (HDAC) inhibitor, exhibiting IC50 values of 25 nM for human HDAC1, 66 nM for HDAC2, 6.5 nM for HDAC3, and 281 nM for HDAC6. This compound effectively induces acetylation of α-tubulin and histone H3, promoting cancer cell apoptosis, particularly in synergy with cisplatin. HDAC-IN-54 is relevant for research applications in head and neck cancer, ovarian cancer, and tongue squamous cell carcinoma.

Nicoxamat, also known as N-Hydroxynicotinamide, functions as an inhibitor of hepatitis C virus (HCV) and selectively targets HDAC6. This compound exhibits antiviral activity against HCV, making it a useful tool in research on hepatitis C infection. Its role as an HDAC6 inhibitor further supports investigations into epigenetic regulation and potential therapeutic strategies.

CARM1/HDAC2-IN-1 is a dual inhibitor targeting both CARM1 and HDAC2, exhibiting IC50 values of 3.71 nM and 4.07 nM, respectively. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. CARM1/HDAC2-IN-1 is suitable for studies investigating the role of these epigenetic regulators in tumor biology and therapeutic strategies.

HDAC6 degrader-5 functions as an HDAC6 degrader, demonstrating potent inhibitory and degradation capabilities with an IC50 of 4.95 nM and a DC50 of 0.96 nM. This compound effectively inhibits the release of pro-inflammatory cytokines, including TNF-α, IL-1β, and IL-6, while also preventing hepatocyte apoptosis. Additionally, HDAC6 degrader-5 shows anti-inflammatory effects in mouse models of acetaminophen-induced liver injury, making it a valuable tool for research on inflammatory diseases and liver pathologies.

HDAC3 Degrader-2 is a selective degrader of histone deacetylase 3 (HDAC3), functioning through targeted degradation to inhibit the activation of the NLRP3 inflammasome. By facilitating the reduction of IL-1β maturation and caspase-1 activity, HDAC3 Degrader-2 demonstrates significant anti-inflammatory effects. This reagent is applicable in researching conditions such as endotoxin shock, colitis, and gouty arthritis, providing valuable insights into mechanisms of inflammation and therapeutic interventions.

CM-444 is a potent inhibitor of histone deacetylases (HDACs) with an IC50 range of 6 nM to 0.6 μM, and demonstrates inhibition of DNA methyltransferases (DNMT) with IC50 values between 1.8 and 2.3 μM. This compound facilitates the differentiation of acute myeloid leukemia cells and exhibits significant anti-leukemic activity, enhancing survival rates in mouse models. CM-444 serves as a valuable tool for research into cancer epigenetics and the development of targeted therapies for leukemia.

HDAC-IN-101 is a selective inhibitor of HDAC1, exhibiting an IC50 of 65 nM against human HDAC1. This compound effectively inhibits cancer cell proliferation by targeting HDAC1 activity. In addition, HDAC-IN-101 is metabolically activated by overexpressed nitroreductase to produce H6AQ, which displays fluorescence under low pH conditions. Its unique properties make it valuable for applications in cancer research and cellular imaging studies.

2-Propylpent-4-ynoic acid, a histone deacetylase (HDAC) inhibitor, exhibits an IC50 of 0.5 mM against human HDAC. This compound induces P-glycoprotein function and has been associated with teratogenicity, fetal growth inhibition, and neurotoxicity. Notably, the S-enantiomer demonstrates more significant teratogenic effects compared to its R-enantiomer and other analogs. 2-Propylpent-4-ynoic acid is relevant in research focused on the mechanisms underlying colon cancer and neural tube defects, including exencephaly.

LG190119 is a selective modulator of HDAC8, primarily targeting Schistosoma mansoni with reduced affinity for human HDAC8. This compound has been shown to induce apoptosis in schistosome cells, making it a valuable tool for research in anti-parasitic agents. Its ability to selectively affect parasitic cells underscores its potential in developing effective treatments against schistosomiasis.

HDAC2-IN-3 is a selective HDAC2 inhibitor with an IC50 of 14 nM, capable of crossing the blood-brain barrier. This compound effectively upregulates histone acetylation levels both in cultured cells and in vivo, and has been shown to enhance long-term potentiation (LTP) in the hippocampus. HDAC2-IN-3 is valuable for research applications focused on neurodegenerative disorders, particularly Alzheimer's disease.

HDAC8-IN-16 is a selective inhibitor of histone deacetylase 8 (HDAC8), exhibiting an IC50 of 0.16 μM. It has been shown to induce apoptosis in various cell lines, trigger G2/M phase cell cycle arrest, and moderately inhibit cancer cell proliferation. This compound is particularly relevant for research applications related to colorectal cancer, providing valuable insights into the therapeutic potential of HDAC8 modulation.

HDAC6-IN-78 is a highly selective inhibitor of histone deacetylase 6 (HDAC6), exhibiting an IC50 of 24 nM. This compound demonstrates specificity by showing no significant activity against other HDAC isoforms. HDAC6-IN-78 is valuable for research applications focused on studying the role of HDAC6 in cellular processes, including neurodegenerative diseases and cancer.

NCT-10b is a selective inhibitor of HDAC6, primarily targeting this enzyme to influence cellular processes. It facilitates α-tubulin acetylation while having minimal effect on histone H4 acetylation. NCT-10b is applicable in research focused on multiple myeloma, providing insights into the mechanisms of this hematological malignancy and potential therapeutic strategies.

4-Phenylcinnamic acid is a weak inhibitor of HDAC2, exhibiting an IC50 value greater than 5 μM. This compound has demonstrated moderate activity in inhibiting cell growth in various tumor cell lines. Its role as an HDAC2 inhibitor makes it a useful tool for exploring the effects of histone deacetylation in cancer research and related fields.