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HDAC Inhibitor
BRD4097 is a potent inhibitor of histone deacetylases (HDACs), particularly targeting HDAC1, 2, and 3. By employing metal chelation and spatial rejection mechanisms, BRD4097 effectively modulates HDAC activity, leading to alterations in gene expression and chromatin structure. This compound is valuable for investigating the role of HDACs in cholesterol metabolism and Niemann-Pick C1 (NPC1) disease models. -
HDAC Inhibitor x
(Rac)-Nanatinostat is a potent histone deacetylase (HDAC) inhibitor, exhibiting an IC50 of <330 nM. This compound demonstrates significant anticancer activity, effectively inhibiting cell growth in various cancer cell lines, including HeLa, U937, and HUT cells. It serves as a valuable tool for researching the role of HDACs in cancer biology and potential therapeutic applications in oncology. -
HDAC Inhibitor
MD 85 is a potent histone deacetylase (HDAC) inhibitor with an EC50 of 5 μM. It effectively modulates epigenetic regulation by inhibiting HDAC activity, which can lead to altered gene expression. MD 85 is primarily utilized in cancer research to explore mechanisms of tumorigenesis and potential therapeutic strategies. -
HDAC8 Inhibitor
J1075 is a selective inhibitor of the histone deacetylase 8 (HDAC8) enzyme in Schistosoma mansoni, exhibiting reduced affinity for human HDAC8. This compound has been shown to induce apoptosis and cell death in schistosome cells. J1075 serves as a valuable tool in the investigation of anti-parasitic agents, contributing to the understanding of therapeutic strategies against schistosomiasis. -
BET/HDAC Inhibitor
TW9 is a potent dual inhibitor that targets bromodomain and extraterminal (BET) proteins and histone deacetylases (HDAC) with KDs of 0.069 μM and 0.231 μM for BRD4(1) and BRD4(2), respectively, and an IC50 of 0.29 μM for HDAC1. This compound is a novel derivative of the BET inhibitor (+)-JQ1 and the class I HDAC inhibitor CI994. TW9 demonstrates significant anti-tumor activity in pancreatic ductal adenocarcinoma (PDAC) and enhances the efficacy of the chemotherapeutic agent Gemcitabine, making it a valuable tool for cancer research applications. -
JAK/HDAC Inhibitor
JAK/HDAC-IN-3 is a dual inhibitor targeting Janus kinase (JAK) and histone deacetylases (HDAC). It exhibits potent inhibitory activity with IC50 values of 25.36 nM for JAK2, and 0.2 μM and 0.43 μM for HDAC and HDAC1, respectively. This compound is valuable for investigating the roles of JAK and HDAC pathways in cellular processes and disease models, particularly in cancer and inflammatory research. -
HDAC Inhibitor
J27644 is a potent inhibitor of histone deacetylases (HDACs), demonstrating efficacy in mitigating TGF-β-induced pulmonary fibrosis. This compound not only modulates histone acetylation but also influences cellular pathways associated with fibrosis, making it a valuable tool for studying mechanisms underlying fibrotic diseases. Its unique profile supports research applications aimed at elucidating the role of HDACs in various pathological conditions. -
HDAC Inhibitor
HDAC/BET-IN-1 is a potent inhibitor of histone deacetylases HDAC1 and HDAC6, with IC50 values of 0.163 μM and 0.067 μM, respectively. Additionally, it targets BRD4 with a Ki of 0.076 μM. This compound demonstrates significant antileukemia activity, making it a valuable tool for studying epigenetic regulation and potential therapeutic applications in leukemia research. -
HDAC8/PGNGdacs Inhibitor
NHNB is a selective inhibitor of histone deacetylase 8 (HDAC8) and Peptidoglycan N-acetylglucosamine deacetylases (PGNGdacs), with an IC50 value of 66.0 μM. This compound exhibits significant antibacterial and bactericidal activity against Bacillus anthracis and Bacillus cereus. NHNB is particularly useful in research related to acute myeloid leukemia and infections caused by these pathogenic bacteria. -
HDAC6 Inhibitor
HDAC6-IN-71 is a selective inhibitor of histone deacetylase 6 (HDAC6), exhibiting an IC50 of 13.68 nM for HDAC6 and 443.12 nM for HDAC1. This compound effectively reduces nitric oxide production in mouse macrophages, with an IC50 of 2.31 μM. By inhibiting the HDAC6-NF-κB signaling pathway, HDAC6-IN-71 leads to decreased phosphorylation of IκB-α and IKK-α/β, and downregulates the expression of key inflammatory mediators such as COX-2 and iNOS. Its efficacy has been demonstrated in models of ulcerative colitis, highlighting its potential for therapeutic applications in inflammatory diseases. -
HDAC6 Inhibitor
HDAC6-IN-14 is a selective inhibitor of histone deacetylase 6 (HDAC6), exhibiting an IC50 of 42 nM. This compound demonstrates over 100-fold selectivity against HDAC1, HDAC2, HDAC3, and HDAC4. HDAC6-IN-14 is utilized in research focused on cellular processes related to neurodegenerative diseases, cancer, and immunological responses, making it a valuable tool for studying histone acetylation and its effects on gene expression. -
HDAC Inhibitor
(R)-Dihydrolipoic acid is a selective inhibitor of histone deacetylase 6 (HDAC6). It demonstrates the ability to modulate HDAC6 activity through specific interactions, thereby contributing to the regulation of gene expression and cellular functions. This compound is valuable for research into the interplay between HDAC function and oxidative stress, offering insights into potential therapeutic strategies for conditions linked to epigenetic modifications. -
HDAC Inhibitor
ZG-126 is a potent histone deacetylase (HDAC) inhibitor with an IC50 range of 0.63-67.6 μM, also functioning as an agonist for the vitamin D receptor (VDR). This compound demonstrates significant cytotoxicity against cancer cell lines, including MDA-MB-231 and 4T1. In murine models, ZG-126 exhibits robust antitumor and anti-metastatic effects, particularly in melanoma and triple-negative breast cancer (TNBC). Additionally, it displays anti-inflammatory properties by reducing macrophage infiltration and promoting a shift away from immunosuppressive M2 polarization. -
PD-L1/HDAC6 Inhibitor
PD-L1/HDAC6-IN-1 is a dual inhibitor targeting PD-L1 and HDAC6, effectively disrupting the PD-L1/PD-1 interaction with IC50 values of 26.8 nM and 69 nM, respectively. This compound significantly enhances the cytotoxicity of Jurkat T cells against HepG2 cells with an IC50 of 3.4 μM. Additionally, PD-L1/HDAC6-IN-1 demonstrates favorable pharmacokinetics in rat models, achieving a drug exposure level of 871.62 ng·h/mL, and shows promising antitumor efficacy in B16-F10 xenograft models in mice. -
HDAC6 Inhibitor
HDAC6-IN-64 is a selective inhibitor of histone deacetylase 6 (HDAC6) with an IC50 of 11.9 nM. It demonstrates potent antitumor activity and is particularly relevant in the context of chemotherapy for non-small cell lung cancer (NSCLC) research. Despite its poor cell permeability, HDAC6-IN-64 can provide valuable insights into the role of HDAC6 in cancer biology and potential therapeutic interventions. -
HDAC Inhibitor
HDAC-IN-30 is a potent multi-target histone deacetylase (HDAC) inhibitor, demonstrating strong inhibition of HDAC1 (IC50 = 13.4 nM), HDAC2 (IC50 = 28.0 nM), HDAC3 (IC50 = 9.18 nM), HDAC6 (IC50 = 42.7 nM), and HDAC8 (IC50 = 131 nM). This compound exhibits significant antitumor activity, making it a valuable tool for cancer research and potential therapeutic applications in oncology. Its ability to modulate gene expression through HDAC inhibition positions HDAC-IN-30 as an important reagent in epigenetic studies and cancer treatment research. -
HDAC/CK2 Inhibitor
HDAC/CK2-IN-1 is an inhibitor targeting histone deacetylases HDAC1 and HDAC6, with IC50 values of 1.46 μM and 0.66 μM, respectively, as well as casein kinase 2 (CK2) with an IC50 of 3.67 μM. This compound demonstrates significant antiproliferative effects on various cancer cell lines, including Jurkat, MCF-7, HCT-116, and HL-60. It serves as an important research tool for studying the roles of histone modifications and CK2 in tumor biology and could have potential implications in the development of cancer therapeutics. -
HDAC6 Inhibitor
HDAC6-IN-76 is a selective inhibitor of histone deacetylase 6 (HDAC6) with an IC50 of 12 nM. This compound promotes autophagy and apoptosis in a p53-dependent manner, demonstrating potential therapeutic implications in cancer research. HDAC6-IN-76 exhibits significant anticancer activity, particularly against hematologic malignancies such as acute myeloid leukemia, making it a valuable tool for investigating the role of HDAC6 in cancer biology and treatment strategies. -
A2AAR/HDAC Dual Inhibitor
A2AAR/HDAC-IN-2 is a potent dual inhibitor targeting the adenosine A2A receptor (A2AAR) and histone deacetylase 1 (HDAC1). It demonstrates a strong binding affinity for A2AAR with a Ki value of 10.3 nM and exhibits significant inhibitory activity against HDAC1 with an IC50 of 18.5 nM. This compound is applicable in cancer research, particularly in studies exploring antitumor mechanisms and therapeutic efficacy. -
HDAC6 Inhibitor
HDAC6-IN-60 is a selective inhibitor of histone deacetylase 6 (HDAC6) that is orally active. By inhibiting the enzymatic activity of HDAC6, this compound regulates pathways associated with protein homeostasis and modulates tumor cell proliferation. HDAC6-IN-60 is valuable for investigating the role of HDAC6 in various cancer types and therapeutic applications related to HDAC6-associated malignancies. -
HDAC6/HDAC1 Inhibitor
HDAC6-IN-59 is a selective inhibitor of histone deacetylase 6 (HDAC6) with an IC50 of 3.12 nM and a remarkable 352-fold selectivity over HDAC1. This compound is valuable for investigating the role of HDAC6 in various biological processes and is particularly relevant in esophageal cancer research. Its potency and specificity make HDAC6-IN-59 an important tool for exploring therapeutic strategies targeting HDAC6-related pathways. -
HDAC Inhibitor
HDAC-IN-33 is a potent inhibitor of histone deacetylases (HDACs), exhibiting IC50 values of 24 nM, 46 nM, and 47 nM for HDAC1, HDAC2, and HDAC6, respectively. This compound demonstrates significant antiproliferative activity against various tumor cell lines, contributing to its potential as an anticancer agent. Furthermore, HDAC-IN-33 has shown promising antitumor efficacy in vivo, promoting antitumor immune responses that may enhance its therapeutic potential in cancer research applications. -
HDAC6 Inhibitor
HDAC6-IN-43 is a selective inhibitor of histone deacetylase 6 (HDAC6) with an IC50 value of 11 nM, demonstrating potent activity against other HDACs, including HDAC1 and HDAC2 (IC50 < 150 nM). By inhibiting HDAC6, this compound contributes to the modulation of acetylation processes, which are critical for cellular functions. HDAC6-IN-43 is relevant for research applications in autosomal dominant polycystic kidney disease (ADPKD) and other conditions involving dysregulated histone modification. -
HDAC1/3 Inhibitor
HDAC1/3-IN-1 is a selective inhibitor targeting histone deacetylases HDAC1 and HDAC3, exhibiting IC50 values of 256 nM and 340.3 nM, respectively. This compound has been shown to increase the SubG1 cell population and promote apoptosis in glioma cells and glioblastoma stem cells. HDAC1/3-IN-1 is ideal for research applications focused on investigating glioblastoma and exploring therapeutic strategies for glioma-related disorders. -
pan-HDAC Inhibitor
Quisinostat hydrochloride is a potent pan-HDAC inhibitor, exhibiting IC50 values between 0.11 nM and 0.64 nM for multiple HDAC targets including HDAC1, HDAC2, HDAC4, HDAC10, and HDAC11. This compound demonstrates significant antitumoral activity across various cancer models. Additionally, Quisinostat hydrochloride has been shown to induce autophagy in neuroblastoma cells, making it a valuable tool for research in cancer biology and therapeutic development. -
HDAC/CoREST Inhibitor
Rodin-A is a selective histone deacetylase (HDAC) and CoREST complex inhibitor, demonstrating an IC50 of 1.80 μM for the CoREST complex, 0.15 μM for HDAC1, and 0.43 μM for HDAC2. This orally active compound enhances histone H3K9 acetylation and upregulates neuron-related gene expression, which promotes dendritic spine density and the colocalization of synaptic proteins such as SV2A and PSD95. Additionally, Rodin-A improves hippocampal long-term potentiation, indicating its potential for neuroprotective and restorative applications in research on neurodegenerative diseases, particularly Alzheimer’s disease. -
HDAC Inhibitor
YPX-C-05 is a hydroxamic acid-derived inhibitor of histone deacetylases (HDACs). It demonstrates notable vasodilatory effects while promoting acetylation of histone H4 in endothelial cells. This compound is applicable in hypertension research, providing insights into the mechanisms underlying vascular regulation and potential therapeutic strategies. -
HDAC inhibitor
HDAC-IN-28 is a potent inhibitor of histone deacetylases (HDACs), which play a crucial role in regulating gene expression and cellular function. This compound exhibits significant anti-tumor activity, effectively inhibiting tumor growth and metastasis. HDAC-IN-28 is valuable for research applications focused on cancer biology, epigenetic regulation, and potential therapeutic strategies for malignancies. -
LSD1/HDAC Inhibitor
LSD1/HDAC-IN-1 is a potent inhibitor of histone deacetylases (HDACs) and lysine-specific demethylase 1 (LSD1), demonstrating impressive inhibitory activity with IC50 values of 0.125 nM for HDAC1, 0.373 nM for HDAC2, 0.0118 nM for HDAC6, 0.103 nM for HDAC8, and 0.571 μM for LSD1. This compound is significant in cancer research, as it influences gene expression and histone modification, making it a valuable tool for studies addressing epigenetic regulation and potential therapeutic interventions. -
HDAC1/2 Inhibitor
M122 is a selective inhibitor of histone deacetylases HDAC1 and HDAC2, demonstrating IC50 values of 0.48 μM and 0.47 μM, respectively. This compound exhibits significant antitumor activity, making it a valuable tool for cancer research. Its ability to modulate gene expression through epigenetic mechanisms positions M122 as a potential candidate for studies in cancer therapeutics and epigenetic regulation. -
HDAC6 Inhibitor
HDAC6-IN-40 is a selective inhibitor of histone deacetylase 6 (HDAC6), demonstrating an IC50 of 0.029 μM. This compound plays a significant role in the regulation of protein acetylation, impacting cellular processes such as stress response and neurodegeneration. It is particularly relevant for research applications focused on cancer, neurodegenerative diseases, and the modulation of immune responses. -
HDAC6 Inhibitor
KT-531 is a potent and selective inhibitor of histone deacetylase 6 (HDAC6), exhibiting an IC50 of 8.5 nM. This compound demonstrates significant cytotoxic activity in SUP-T11 cells, with an IC50 of 0.42 μM. KT-531 is suitable for research applications focused on hematological cancers, enabling the investigation of HDAC6's role in tumor progression and potential therapeutic strategies. -
HDAC Inhibitor
M133 is a selective inhibitor of HDAC1 and HDAC2, demonstrating potent antiproliferative activity against various human tumor cell lines with IC50 values ranging from 0.75 to 1.94 μM. This compound serves as a valuable tool for cancer research, facilitating the investigation of histone deacetylase activity and its implications in tumor biology. -
HDAC Inhibitor
Dihydrochlamydocin analog-1 is a potent histone deacetylase (HDAC) inhibitor that demonstrates significant activity by inhibiting histone H4 peptide deacetylation with an IC50 of 30 nM. This compound is useful for studying the role of HDACs in gene regulation, cellular differentiation, and cancer therapy. It may also serve as a valuable tool in epigenetic research and therapeutic development targeting HDAC-related disorders. -
PD-L1/HDAC Inhibitor
PD-L1/HDAC-IN-1 is a dual inhibitor targeting PD-L1, HDAC2, and HDAC3, with IC50 values of 88.10 nM, 27.98 nM, and 14.47 nM, respectively. This compound effectively disrupts the PD-1/PD-L1 interaction and demonstrates minimal cytotoxicity in MCF-7 cells (IC50=19.34 μM). PD-L1/HDAC-IN-1 enhances the expression of PD-L1 and CXCL10, thereby facilitating an anti-tumor immune response through increased T-cell recruitment into the tumor microenvironment (TME). Its unique mechanism positions it as a valuable tool for research in cancer immunotherapy. -
HDAC Inhibitor
BATCP is an inhibitor of histone deacetylases (HDACs), which play a crucial role in the regulation of gene expression through the removal of acetyl groups from histone proteins. This compound exhibits potent HDAC inhibitory activity, potentially leading to increased acetylation of histones and altered transcriptional outcomes. BATCP is suitable for research applications focusing on epigenetic regulation, cancer biology, and related therapeutic strategies. -
HDAC Inhibitor
Butyrylhydroxamic acid is a selective inhibitor of histone deacetylase (HDAC), modulating gene expression by preventing histone deacetylation. Its biological activity has been shown to enhance cognitive functions in rodent models, suggesting potential applications in memory enhancement and mood stabilization. Additionally, it is being explored in research related to β-chain hemoglobinopathies, providing valuable insights into therapeutic strategies for related disorders. -
HDAC8 Inhibitor
J1038 is a selective inhibitor of histone deacetylase 8 (HDAC8), targeting the catalytic zinc ion of Schistosoma mansoni HDAC8 (smHDAC8). This compound demonstrates significant inhibition of HDAC8 activity, making it a valuable tool for studying epigenetic regulation and potential therapeutic applications in cancer and neurodegenerative diseases. Researchers can utilize J1038 to explore the biological effects of HDAC8 inhibition in various cellular contexts. -
HDAC Inhibitor
FFK29 is a potent synthetic inhibitor of class II histone deacetylases (HDACs). It effectively impedes the growth and encystation of Acanthamoeba, making it a valuable tool in the study of protozoan and parasitic diseases. Research applications for FFK29 include investigations into the molecular mechanisms of HDAC inhibition and its potential therapeutic effects against parasitic infections. -
HDAC Inhibitor
Diheteropeptin is a potent histone deacetylase (HDAC) inhibitor that modulates various cellular processes. This compound exhibits biological activities similar to those of Transforming Growth Factor-β (TGF-β) and may influence gene expression and cellular differentiation. Diheteropeptin is useful in the study of epigenetic regulation and has potential applications in cancer research and therapeutic development. -
HDAC/NAMPT Inhibitor
HDAC/NAMPT-IN-1 is a potent dual inhibitor of histone deacetylases (HDAC) and nicotinamide adenine dinucleotide (NAD+) biosynthesis enzyme NAMPT, exhibiting IC50 values ranging from 0.72 to 37081 nM for HDAC and 1618 nM for NAMPT. This compound demonstrates significant potential in modulating cellular acetylation levels and metabolic processes associated with cancer and neurodegenerative diseases. Its application in research can facilitate studies on epigenetic regulation and NAD+ metabolism, contributing to a deeper understanding of cellular mechanisms and therapeutic strategies. -
HDAC Inhibitor
HDAC6-IN-10 is a potent and selective inhibitor of histone deacetylase 6 (HDAC6) with an IC50 of 0.73 nM, demonstrating a remarkable 144 to 10,941-fold selectivity over other HDAC isoforms. This compound exhibits significant anti-proliferative activity against multiple myeloma cells, making it a valuable tool for cancer research. Its selectivity and effectiveness support its use in studies exploring the therapeutic potential of HDAC6 inhibition in various malignancies. -
HDAC Inhibitor
HDAC-IN-38 is a potent inhibitor of histone deacetylases (HDACs), targeting HDAC1, 2, 3, 5, 6, and 8 with micromolar inhibitory activity. This compound has been shown to enhance cerebral blood flow, mitigate cognitive impairment, and reduce hippocampal atrophy. Additionally, HDAC-IN-38 increases histone acetylation levels, specifically H3K14 and H4K5, making it a valuable tool for studying the epigenetic regulation of gene expression and its implications in neurodegenerative disorders. -
HDAC6 Inhibitor
HDAC6-IN-35 is a potent inhibitor of HDAC6, exhibiting an IC50 of 4.7 μM, which allows for effective modulation of histone acetylation. This compound is capable of penetrating the blood-brain barrier (BBB) and demonstrates cytotoxic effects on MDA-MB-231 breast cancer cells, with an EC50 of 40.6 μM. HDAC6-IN-35 is ideal for investigating the role of histone deacetylation in cancer biology and may contribute to therapeutic strategies targeting HDAC-related pathways. -
HDAC1/2 Inhibitor
GK444 is an inhibitor of histone deacetylases HDAC1 and HDAC2, with IC50 values of 100 nM and 92 nM, respectively. This compound demonstrates significant biological activity by inhibiting Caco-2 cell proliferation, showcasing an IC50 of 4.1 μM. Additionally, GK444 effectively reduces TGF-β1 induced COL1A1 mRNA levels in primary normal human lung fibroblasts and has been shown to inhibit Bleomycin-induced lung fibrosis in murine models. Its applications extend to research in cancer, fibrosis, and other HDAC-related pathways. -
HDAC Inhibitor
HDAC-IN-43 is a potent inhibitor of histone deacetylases HDAC1, HDAC3, and HDAC6, exhibiting IC50 values of 82 nM, 45 nM, and 24 nM, respectively. Additionally, it acts as a weak inhibitor of PI3K and mTOR, with IC50 values of 3.6 μM and 3.7 μM. This compound demonstrates significant anti-proliferative activity, making it a valuable tool for research on cancer and epigenetic regulation. -
HDAC Inhibitor
HDAC-IN-44 is a potent histone deacetylase (HDAC) inhibitor with an IC50 value of 61.2 nM. This compound demonstrates significant anticancer activity across various cancer cell lines, making it a valuable tool for research in cancer biology and epigenetic regulation. HDAC-IN-44 can be utilized in studies exploring the role of HDACs in tumor progression and the development of novel therapeutic strategies. -
HDAC Inhibitor
HDAC6-IN-27 is a selective inhibitor of histone deacetylase 6 (HDAC6) with an IC50 of 15.9 nM, exhibiting weaker activity against HDAC8 and HDAC1 with IC50 values of 136.5 nM and 6180.2 nM, respectively. This compound demonstrates significant antiparasitic efficacy, making it a valuable tool for exploring the role of HDAC6 in various biological pathways. It is suitable for research applications focused on epigenetic modulation and potential therapeutic strategies against parasitic infections. -
PI3K/HDAC Inhibitor
PI3K/HDAC-IN-3 is a dual inhibitor targeting PI3K and HDAC, with IC50 values of 0.23 nM for PI3Kα and 172 nM for HDAC1. It effectively suppresses AKT phosphorylation while enhancing H3 acetylation in MV4-11 cells. Additionally, PI3K/HDAC-IN-3 demonstrates notable anticancer efficacy in a dose-dependent manner within an MV4-11 xenograft model, making it a valuable tool for studying cancer biology and potential therapeutic interventions. -
DNMT/HDAC Inhibitor
DNMT/HDAC-IN-2 is a dual inhibitor of DNA methyltransferase (DNMT) and histone deacetylases (HDAC), exhibiting IC50 values of 365 nM for DNMT1, 0.2 nM for HDAC1, and 8.91 nM for HDAC6. This compound effectively inhibits the proliferation of breast cancer cells and demonstrates significant anti-tumor activity in xenograft and transgenic mouse models of breast cancer. DNMT/HDAC-IN-2 serves as a valuable tool for investigating epigenetic modification in breast cancer research.

