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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. -
PROTAC HDAC Degrader
JPS014 is a benzamide-based HDAC degrader designed to engage the Von Hippel-Lindau (VHL) E3 ligase for targeted proteolysis. It effectively degrades class I histone deacetylases (HDAC1 and HDAC2), leading to significant alterations in gene expression profiles and promoting apoptotic pathways in HCT116 cancer cells. This compound is particularly useful for studying the role of HDAC inhibition in cancer biology and elucidating mechanisms of resistance to therapies. -
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. -
HDACi
ZYJ-34c is a potent histone deacetylase inhibitor (HDACi) that effectively targets HDAC6 and HDAC8, exhibiting IC50 values of 0.056 μM and 0.146 μM, respectively. At low concentrations, ZYJ-34c induces G1 phase cell cycle arrest and demonstrates significant antiproliferative activity. In preclinical studies, it shows substantial antitumor effects in MDA-MB-231 and HCT116 xenograft models and reveals antimetastatic potential in a mouse hepatoma-22 (H22) pulmonary metastasis model, highlighting its applicability in cancer research. -
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. -
HDAC Substrate
Z-MAL is a potent HDAC substrate that efficiently targets class I and II histone deacetylases, as well as class III SIRT1. This compound demonstrates significant conversion activity, making it suitable for studies focused on structure-activity relationships, subtype selectivity, and inhibitor screening of histone deacetylases. Z-MAL is an essential tool for advancing research in epigenetics and related biological pathways. -
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. -
HDAC6 Degrader
HDAC6 degrader-4 is a PROTAC that selectively targets and degrades HDAC6. By combining a non-selective HDAC inhibitor with a thalidomide-type E3 ligase ligand, it effectively modulates histone deacetylation. This reagent is primarily utilized in cancer research to investigate the role of HDAC6 in tumor progression and to evaluate potential therapeutic strategies. -
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. -
PI3Kα/HDAC6 Inhibitor
PI3Kα/HDAC6-IN-1 is a dual inhibitor targeting PI3Kα and HDAC6, exhibiting IC50 values of 2.9 nM and 26 nM, respectively. This compound effectively inhibits AKT (Ser473) phosphorylation and promotes the accumulation of acetylated α-tubulin, while not influencing acetylated histones H3 and H4. Its potent anti-cancer activity is demonstrated in the L-363 cell line with an IC50 of 0.17 μM, highlighting its potential for therapeutic applications in cancer research. -
HDAC Inhibitor
LB-205 is a pan-histone deacetylase inhibitor (HDACi) that modulates histone acetylation, impacting gene expression. This compound demonstrates significant potential in the study of acute traumatic brain injury, providing insights into cellular responses and neuroprotection mechanisms. Its application in research may facilitate the understanding of therapeutic strategies for neurodegenerative conditions. -
HDAC Inhibitor
HDAC-IN-58 is a selective inhibitor of histone deacetylase 6 (HDAC6) with an IC50 value of 2.06 nM. It exhibits important biological activity in modulating protein acetylation, which is crucial for cellular processes linked to chronic diseases. This compound is particularly useful for research applications focused on neurodegenerative disorders and psychiatric conditions, providing insights into potential therapeutic strategies. -
HDAC6 Inhibitor
HDAC6-IN-11 is a selective inhibitor of histone deacetylase 6 (HDAC6), displaying an IC50 value of 20.7 nM and over 300-fold selectivity against other HDAC isoforms. This compound exhibits significant anti-proliferative activity in cancer cell lines, making it a valuable tool for research in oncology and epigenetics. Its specificity and robust biological effects position HDAC6-IN-11 as a potent reagent for investigating HDAC6-related pathways in cancer development and treatment. -
CYP51/HDAC Inhibitor
CYP51/HDAC-IN-1 is a potent dual inhibitor of CYP51 and HDAC, demonstrating significant biological activity in combating virulence factors as well as down-regulating resistance-associated genes. This compound shows promising therapeutic potential for treating tropical candidiasis and cryptococcal meningitis, making it a valuable tool for research in antifungal therapies. -
HDAC1/MAO-B Inhibitor
HDAC1/MAO-B-IN-1 is a selective inhibitor targeting both HDAC1 and MAO-B, exhibiting IC50 values of 21.4 nM and 99.0 nM, respectively. This compound effectively crosses the blood-brain barrier, making it a valuable tool for studying neurological disorders. Its potential applications include research into Alzheimer's disease and related pathologies, facilitating the exploration of epigenetic modifications and monoamine metabolism in the brain. -
HDAC8 Inhibitor
HDAC8-IN-4 is a selective inhibitor of histone deacetylase 8 (HDAC8), demonstrating an IC50 of 0.15 μM for HDAC8 and 12 μM for HDAC3. This compound is crucial for studies focusing on epigenetic regulation and cancer biology, as it modulates histone acetylation and affects gene expression. HDAC8-IN-4 provides a valuable tool for exploring the therapeutic potential of HDAC inhibition in various diseases. -
HDAC Inhibitor
HDAC-IN-41 is a selective class I histone deacetylase (HDAC) inhibitor, exhibiting IC50 values of 0.62 µM for HDAC1, 1.46 µM for HDAC2, and 0.62 µM for HDAC3. This compound is orally active and demonstrates potential in modulating gene expression through HDAC inhibition. Applications in research include studies on cancer, neurodegenerative diseases, and epigenetic regulation. Notably, HDAC-IN-41 does not exhibit NO releasing activity. -
HDAC Inhibitor
2-Hexyl-4-pentynoic acid serves as an HDAC inhibitor, demonstrating an IC50 value of 13 μM. This compound induces HSP70 expression and promotes histone hyperacetylation, providing neuroprotection against glutamate-induced excitotoxicity in cultured neurons. Additionally, it is utilized in breast carcinoma research and acts as a click chemistry reagent, featuring an alkyne group that allows for copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. -
HDAC3 Inhibitor
HDAC3-IN-3 is a potent inhibitor of histone deacetylase 3 (HDAC3) that plays a critical role in the regulation of gene expression and chromatin remodeling. By inhibiting HDAC3, this compound exhibits significant biological activity in modulating cell proliferation and apoptosis, making it a valuable tool for cancer research. Its application extends to studying the mechanisms underlying tumorigenesis and developing potential therapeutic strategies for HDAC3-related malignancies. -
HDAC1/3 Inhibitor
GK718 is a potent inhibitor of histone deacetylases 1 and 3 (HDAC1/3), exhibiting IC50 values of 259 nM and 139 nM, respectively. This compound effectively increases the levels of acetylated histone H3 in cells, indicating its potential for altering epigenetic regulation. Additionally, GK718 has demonstrated efficacy in inhibiting Bleomycin-induced pulmonary fibrosis in murine models, making it relevant for research into fibrotic diseases and epigenetic modifications. -
Dual HDAC/HSP90 Inhibitor
HDAC/HSP90-IN-1 is a potent dual inhibitor targeting both histone deacetylases (HDAC) with an IC50 of 194 nM and heat shock protein 90 (HSP90), specifically HSP90α with an IC50 of 153 nM. This compound induces the expression of HSP70, downregulates HSP90 client proteins, and facilitates the acetylation of α-tubulin and histone H3 in cancer cells. Additionally, HDAC/HSP90-IN-1 effectively reduces PD-L1 expression in interferon-gamma treated H1975 cells, making it a valuable tool for cancer research, particularly in lung and colon malignancies. -
HDAC Inhibitor
HDAC-IN-95 is a potent histone deacetylase (HDAC) inhibitor that plays a crucial role in epigenetic regulation. This compound has demonstrated significant biological activity in the context of non-small cell lung cancer (NSCLC), making it a valuable tool for cancer research. Its inhibition of HDAC activity can lead to altered gene expression patterns, facilitating the study of tumor biology and potential therapeutic strategies in NSCLC. -
HDAC8/BRPF1 Inhibitor
HDAC8/BRPF1-IN-1 is a dual inhibitor targeting HDAC8 and BRPF1, demonstrating an IC50 of 443 nM for HDAC8 and a Kd of 67 nM for BRPF1 in human cells. This compound exhibits minimal activity against HDAC1 and HDAC6, making it a selective tool for probing histone deacetylation pathways. It is valuable for investigating the roles of HDAC8 and BRPF1 in gene regulation and potential therapeutic strategies in cancer research. -
HDAC Inhibitor
HDAC-IN-66 is a selective histone deacetylase (HDAC) inhibitor that demonstrates potent activity against hematological tumor cells. As a derivative of Pomalidomide, this compound functions by modulating gene expression through HDAC inhibition, leading to a decrease in tumor cell proliferation and survival. HDAC-IN-66 is primarily utilized in research applications focused on studying the epigenetic regulation of cancer and developing novel therapeutic strategies for hematological malignancies. -
HDAC3 Inhibitor
HDAC3-IN-8 is a selective inhibitor targeting histone deacetylase 3 (HDAC3) with an IC50 of 0.38 nM, along with notable inhibition of HDAC1 and HDAC2 at 3.52 nM and 15.14 nM, respectively. This compound demonstrates high selectivity for HDAC3 and modulates histone deacetylase activity, making it a valuable tool for epigenetic research. HDAC3-IN-8 is particularly applicable in studies focused on acute myeloid leukemia (AML) and can be utilized in the development of HDAC3-targeted PROTAC degraders.

