Catalog No.
Product Name
Application
Product Information
Citations
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HDAC Inhibitor
CHDI-00484077 is a class IIa HDAC inhibitor that demonstrates potent inhibitory activity against HDAC4 (IC50 = 0.01 μM), HDAC5 (IC50 = 0.02 μM), HDAC7 (IC50 = 0.02 μM), and HDAC9 (IC50 = 0.03 μM). This compound is capable of penetrating the central nervous system, making it a valuable tool for research applications related to Huntington's disease. Its selective activity on histone deacetylases offers insights into epigenetic regulation and therapeutic strategies in neurodegenerative disorders. -
HDACs/NF-κB Dual Inhibitor
Homobutein is a natural chalcone that functions as a potent dual inhibitor of histone deacetylases (HDACs) and nuclear factor kappa B (NF-κB), exhibiting IC50 values of 190 μM and 38 μM, respectively. This compound also acts as a chelator for iron (II and III) cations and demonstrates a range of biological activities, including anticancer, anti-inflammatory, antiparasitic, and antioxidant effects. Homobutein is valuable for research applications involving cellular signaling pathways and the investigation of potential therapeutic strategies in cancer and inflammatory diseases. -
HDAC Inhibitor
MPT0G211 mesylate is a selective inhibitor of histone deacetylase 6 (HDAC6) with a potency characterized by an IC50 of 0.291 nM. It exhibits over 1000-fold selectivity for HDAC6 compared to other HDAC isoforms and is capable of penetrating the blood-brain barrier. MPT0G211 mesylate has demonstrated significant effects in ameliorating tau phosphorylation and cognitive deficits in models of Alzheimer’s disease, along with possessing anti-metastatic and neuroprotective properties. Its potential applications extend to various cancer research settings, highlighting its utility in both neurodegenerative and oncological studies. -
HDAC6 Inhibitor
HDAC6-IN-5 is a potent inhibitor of histone deacetylase 6 (HDAC6), demonstrating an IC50 of 0.025 μM. This compound effectively inhibits the self-aggregation of amyloid-beta 1-42 and acetylcholinesterase (AChE), with IC50 values of 3.0 μM and 0.72 μM, respectively. HDAC6-IN-5 has been shown to promote neurite outgrowth while exhibiting minimal neurotoxicity, making it a valuable tool for research in neurodegenerative disease and neuronal regeneration studies. -
SHP2/HDAC Inhibitor
SHP2/HDAC-IN-1 is a dual allosteric inhibitor targeting SHP2 and HDAC with IC50 values of 20.4 nM and 25.3 nM, respectively. This compound enhances antitumor immunity through the activation of T cells, improving antigen presentation and cytokine secretion. SHP2/HDAC-IN-1 is valuable for investigations in cancer immunotherapy and associated research applications. -
HDAC6 Inhibitor
KA2507 monohydrochloride is a potent and highly selective inhibitor of the histone deacetylase enzyme HDAC6, exhibiting an IC50 value of 2.5 nM. This compound demonstrates significant antitumor efficacy and has been found to modulate immune responses, making it valuable for research into cancer therapies and immunological studies. Researchers may utilize KA2507 monohydrochloride to explore novel treatment strategies in oncology and immune regulation. -
LSD1/HDAC6 Inhibitor
LSD1/HDAC6-IN-1 is a dual inhibitor targeting lysine-specific demethylase 1 (LSD1) and histone deacetylase 6 (HDAC6), demonstrating significant anti-tumor activity. This compound is particularly relevant for research into multiple myeloma (MM), providing insights into epigenetic regulation and potential therapeutic strategies. Its oral bioavailability makes it suitable for in vivo studies in cancer research. -
Anti-malarial HDAC Inhibitor
FNDR-20123 free base is a potent, orally active anti-malarial agent that functions as a histone deacetylase (HDAC) inhibitor. It demonstrates significant inhibitory activity against Plasmodium falciparum, achieving IC50 values of 41 nM during the asexual stage and 190 nM for male gametocytes. In addition, FNDR-20123 free base selectively inhibits various HDAC isoforms, including HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, with respective IC50 values of 25 nM, 29 nM, 2 nM, 11 nM, and 282 nM. This compound is a valuable tool for research into the treatment of malaria and the role of HDACs in cellular regulation. -
MAO A/HDAC Inhibitor
MAO A/HDAC-IN-1 is a dual inhibitor targeting monoamine oxidase A (MAO A) and histone deacetylases (HDAC). This compound exhibits significant biological activity in glioma research, facilitating studies on tumor biology and epigenetic modifications. Additionally, MAO A/HDAC-IN-1 features an alkyne group that enables copper-catalyzed azide-alkyne cycloaddition (CuAAc), making it a valuable tool for click chemistry applications in investigating cellular processes. -
HDAC Inhibitor
OKI-006 is a potent, orally active inhibitor of histone deacetylase (HDAC). As a unique congener of the natural product HDAC inhibitor largazole, it modulates epigenomic regulation by targeting HDACs, enzymes integral to histone acetylation, which is often dysregulated in various cancers. This compound demonstrates significant potential for research applications in cancer biology and the study of epigenetic alterations in tumorigenesis. -
HDAC6 Inhibitor
HDAC6-IN-6 is a potent inhibitor of histone deacetylase 6 (HDAC6), exhibiting an IC50 of 0.025 μM. This compound is capable of crossing the blood-brain barrier and demonstrates strong inhibitory activity against amyloid-beta peptide (Aβ1-42) self-aggregation and acetylcholinesterase (AChE) with IC50 values of 3.0 μM and 0.72 μM, respectively. Additionally, HDAC6-IN-6 enhances neurite outgrowth while maintaining a favorable safety profile, making it a valuable tool for research in neurodegenerative diseases and related fields. -
HDAC6 Inhibitor
SP-2-225 is a selective inhibitor of Histone Deacetylase 6 (HDAC6). This compound enhances the production of cancer-associated antigens and promotes macrophage antigen cross-presentation to T cells, thereby facilitating immune response. Additionally, SP-2-225 has demonstrated efficacy in reducing tumor volume in a syngeneic SM1 melanoma model, making it a valuable tool for cancer immunotherapy research. -
HDAC Inhibitor
Bocodepsin hydrochloride is a selective histone deacetylase (HDAC) inhibitor that demonstrates notable antitumor activity. It is effective in the suppression of solid tumors as well as hematologic malignancies, making it a valuable tool for cancer research. Bocodepsin hydrochloride is suitable for studies aimed at elucidating the role of HDAC in tumor biology and therapeutic response. -
PROTAC HDAC Degrader
JPS035 is a benzamide-derived HDAC degrader that utilizes the Von Hippel-Lindau (VHL) E3 ligase-mediated PROTAC technology. It specifically targets and degrades class I histone deacetylases (HDAC1 and HDAC2), leading to significant alterations in gene expression and promoting apoptosis in HCT116 colorectal cancer cells. This compound serves as a valuable tool for studies focused on epigenetic modulation and therapeutic strategies against HDAC-related diseases. -
HDAC6 Inhibitor
(S)-Trichostatin A is a selective inhibitor of HDAC6, demonstrating IC50 values of 9.88 nM and 11.1 nM for Zebrafish and Human HDAC6, respectively. It exhibits weak inhibition of other human HDACs, making it a valuable tool for studying HDAC6's role in cellular processes. This compound is useful in research applications related to cancer, neurodegenerative diseases, and epigenetic regulation. -
HDAC Inhibitor
HDAC-IN-72 is a potent inhibitor of histone deacetylases 1 (HDAC1), 2 (HDAC2), and 3 (IC50 values of 0.65 μM, 0.78 μM, and 1.70 μM, respectively). This compound exhibits significant antiproliferative activity, making it a valuable tool for studying epigenetic regulation in cancer. HDAC-IN-72 is particularly relevant for breast cancer research, facilitating investigations into the role of histone deacetylation in tumor biology and potential therapeutic strategies. -
HDAC6/8/BRPF1 Inhibitor
HDAC6/8/BRPF1-IN-1 is a selective dual inhibitor targeting HDAC6, HDAC8, and the bromodomain and PHD finger-containing protein 1 (BRPF1). It demonstrates inhibitory activity against HDAC1, HDAC6, and HDAC8 with IC50 values of 797 nM, 344 nM, and 908 nM, respectively, while also inhibiting BRPF1 with a Kd value of 175.2 nM. This compound is valuable for research in cancer biology, providing insights into the role of histone deacetylases and bromodomain proteins in tumorigenesis and cellular processes. -
HDAC6 Inhibitor
HDAC6-IN-53 is a potent inhibitor of histone deacetylase 6 (HDAC6) with an IC50 of 19.65 nM. This compound effectively suppresses collagen expression induced by TGF-β1, demonstrating therapeutic potential in the treatment of idiopathic pulmonary fibrosis (IPF). Additionally, HDAC6-IN-53 has shown efficacy in a mouse model of pulmonary fibrosis induced by Bleomycin. It is a valuable reagent for studying the molecular mechanisms underlying idiopathic pulmonary fibrosis and related pulmonary diseases. -
HDAC PROTAC Inhibitor
JPS016 is a class I histone deacetylase (HDAC) PROTAC inhibitor that targets HDAC1, HDAC2, and HDAC3 for ubiquitination and proteasomal degradation via VHL E3 ligase recruitment. This compound demonstrates significant anticancer activity by reducing the viability of colon cancer cells and inducing apoptosis. Additionally, JPS016 activates the PINK1/Parkin-mediated mitochondrial autophagy pathway, enhancing cardiomyocyte viability, alleviating mitochondrial damage, and decreasing mitochondrial ROS production. It is valuable for research into colon cancer and sepsis-related cardiac dysfunction. -
HDAC Inhibitor
STR-V-53 is a histone deacetylase (HDAC) inhibitor with a low nanomolar IC50. By inhibiting HDAC activity, STR-V-53 increases histone acetylation, leading to altered gene expression. This compound exhibits significant anti-tumor properties, inhibiting proliferation and promoting apoptosis in cancer cells. It serves as a valuable research tool for studying epigenetic regulation and potential therapeutic strategies in oncology. -
HDAC Inhibitor
HDAC-IN-56 is a potent, orally active inhibitor of class I histone deacetylases (HDACs), demonstrating IC50 values of 56.0 ± 6.0 nM for HDAC1, 90.0 ± 5.9 nM for HDAC2, and 422.2 ± 105.1 nM for HDAC3, with minimal activity against HDAC4-11. This compound effectively increases intracellular levels of acetylated histone H3 and P21, leading to G1 cell cycle arrest and apoptosis in tumor cells. HDAC-IN-56 is utilized in cancer research to investigate its therapeutic potential and mechanisms involving HDAC inhibition. -
A2A Receptor/HDAC Inhibitor
IHCH-3064 is a dual-target compound that inhibits the Adenosine A2A Receptor and histone deacetylase (HDAC). It demonstrates potent binding affinity for the A2A receptor (Ki = 2.2 nM) and selectively inhibits HDAC1 with an IC50 of 80.2 nM. This compound exhibits significant antiproliferative activity against various tumor cell lines in vitro, making it a valuable tool for tumor immunotherapy research applications. -
HDAC6 Inhibitor
HDAC6-IN-50 is a potent HDAC6 inhibitor with an IC50 of 35 nM. This compound is valuable in the investigation of neurodegenerative disorders, particularly in the context of Parkinson's disease (PD) and Alzheimer's disease (AD). HDAC6-IN-50 facilitates research on the epigenetic regulation involved in these diseases, contributing to the understanding of their pathogenesis and potential therapeutic strategies. -
HDAC6 Inhibitor
ITF5924 is a potent and highly selective inhibitor of HDAC6, exhibiting an IC50 of 7.7 nM. This compound demonstrates over 104-fold selectivity for HDAC6 compared to other HDAC subtypes. The unique difluoromethyl-1,3,4-oxadiazole (DFMO) moiety allows ITF5924 to function as a slow-binding substrate analog, undergoing an enzyme-catalyzed ring-opening reaction that forms a stable and long-lasting enzyme-inhibitor complex. ITF5924 is valuable for studies exploring the role of HDAC6 in various cellular processes and disease states, making it an essential tool for epigenetic research. -
HDAC1 Inhibitor
HDAC1-IN-8 is a selective inhibitor of histone deacetylase 1 (HDAC1) with an IC50 of 11.94 µM. It exhibits significant antiproliferative activity and has been shown to induce cell cycle arrest at both G1 and G2/M phases. Additionally, HDAC1-IN-8 promotes autophagy and demonstrates anticancer potential, making it a valuable tool for research in lung cancer and other malignancies. -
HDAC1 Activator
HDAC1 activator-1 is a selective activator of histone deacetylase 1 (HDAC1), demonstrating oral bioavailability and minimal cross-reactivity with other HDAC family members. This compound exhibits neuroprotective properties, enhancing cognitive and motor functions by mitigating neuronal loss and gliosis. HDAC1 activator-1 effectively activates HDAC1 in SH-SY5Y neuroblastoma cells, influencing cell cycle regulation and DNA damage responses. It is applicable in research investigating TDP-43 proteinopathy-related neurodegenerative disorders, including Amyotrophic Lateral Sclerosis (ALS) and cerebral ischemia-associated neurological injuries. -
HDAC3 Inhibitor
HDAC3-IN-1 is a potent and selective inhibitor of histone deacetylase 3 (HDAC3), exhibiting an IC50 value of 5.96 nM. This compound effectively modulates gene expression through the inhibition of histone deacetylation, making it a valuable tool for studying epigenetic regulation and cellular signaling pathways. HDAC3-IN-1 is applicable in research areas such as cancer biology, neurodegenerative disorders, and potential therapeutic development for various diseases involving epigenetic dysregulation. -
HDAC Inhibitor
NT376 is a potent and selective inhibitor of class-IIa Histone deacetylases (HDAC), demonstrating an IC50 value of 32 nM in HT-29 cells. It exhibits significant biological activity that supports its role in cancer research and the investigation of central nervous system disorders, including Alzheimer's and Huntington's diseases. NT376 serves as a valuable tool for studying the epigenetic regulation of gene expression and potential therapeutic pathways in these conditions. -
HDAC6 Inhibitor
HDAC6-IN-66 is a potent and selective inhibitor of histone deacetylase 6 (HDAC6), exhibiting an IC50 of 1.8 nM. This compound effectively induces acetylation of α-tubulin while preferentially impacting histone H3. HDAC6-IN-66 serves as a valuable tool for cancer research, facilitating studies on the role of HDAC6 in oncogenic processes and potential therapeutic interventions. -
HDAC6 Inhibitor
HDAC6-IN-9 is a potent and selective inhibitor of HDAC6, demonstrating IC50 values of 4.2 nM for HDAC6 and significantly lower values for HDAC1, HDAC3, HDAC8, and HDAC10. This compound exhibits notable anti-proliferative activity, making it a valuable tool for research in cancer biology and therapeutic development. Its selectivity enables investigations into the specific roles of HDAC6 in cellular processes and disease states. -
HDAC Inhibitor
HDAC-IN-45 is a small molecule inhibitor targeting histone deacetylases (HDACs), specifically demonstrating significant inhibition of HDAC1, HDAC2, and HDAC3 with IC50 values of 0.108 µM, 0.585 µM, and 0.563 µM, respectively. This compound exhibits pronounced anticancer activity and forms a hydrogen bond with the Y303 residue, which may contribute to its mechanism of action. HDAC-IN-45 is valuable for cancer research, particularly in studies focused on epigenetic regulation and therapeutic interventions in tumorigenesis. -
HDAC Inhibitor
4-Iodo-SAHA is an orally active inhibitor of class I and class II histone deacetylases (HDACs), demonstrating EC50 values of 1.1, 0.95, 0.12, 0.24, 0.85, and 1.3 μM across the Skbr3, HT29, U937, JA16, and HL60 cell lines, respectively. This compound exhibits significant potential for tumor growth inhibition and is valuable for cancer research applications, including the investigation of epigenetic regulation and therapeutic interventions in HDAC-related malignancies. -
HDAC Inhibitor
HDAC-IN-26 is a highly selective inhibitor of class I histone deacetylases (HDACs), exhibiting an EC50 value of 4.7 nM. This compound plays a crucial role in modulating gene expression by preventing the deacetylation of histones, thereby facilitating an open chromatin state. HDAC-IN-26 is valuable for research applications involving cancer biology, neurodegenerative diseases, and epigenetic regulation. -
BChE/HDAC6 Inhibitor
BChE/HDAC6-IN-1 is a selective dual inhibitor targeting both butyrylcholinesterase (BChE) and histone deacetylase 6 (HDAC6), with IC50 values of 4 nM and 8.9 nM, respectively. This compound demonstrates significant potential in ameliorating cognitive impairment in an Aβ1–42-induced mouse model, making it a valuable tool in Alzheimer's disease research. Its ability to modulate both cholinergic and epigenetic pathways positions BChE/HDAC6-IN-1 as a promising candidate for studies focused on neurodegenerative disorders. -
HDAC2 Inhibitor
HDAC2-IN-1 is a competitive inhibitor of histone deacetylase 2 (HDAC2), demonstrating an IC50 of 0.5 μM. This orally active compound exhibits additional inhibitory effects on HDAC1 and HDAC8, with IC50 values of 1.61 μM and 0.98 μM, respectively. Its ability to penetrate the blood-brain barrier positions HDAC2-IN-1 as a valuable tool for investigating the role of HDACs in neurodegenerative diseases and other neurological disorders. -
HDAC6 Inhibitor
HDAC6-IN-52 is a potent inhibitor of histone deacetylase 6 (HDAC6), demonstrating a complete inhibition at 10 μM. This compound is significant in the context of central nervous system diseases, particularly neurodegenerative disorders such as Alzheimer’s disease and progressive supranuclear palsy. HDAC6-IN-52 is valuable for research investigating the therapeutic potential of HDAC6 modulation in neurological conditions. -
HDAC Inhibitor
HDAC-IN-20 is a potent inhibitor of histone deacetylases (HDACs), offering oral bioavailability. It exhibits significant anti-cancer activity, making it a valuable tool for investigating tumor biology and exploring epigenetic regulation in cancer research. This compound facilitates the study of HDAC's role in oncogenesis and therapeutic responses, thereby contributing to the understanding of cancer treatment strategies. -
HDAC6 Inhibitor
MPT0G413 is a selective HDAC6 inhibitor with an IC50 of 3.92 nM, demonstrating potent oral bioavailability and the ability to penetrate the blood-brain barrier. This compound effectively reduces tau protein phosphorylation and aggregation, thereby addressing cognitive deficits related to memory and learning. MPT0G413 is suitable for research applications in neurological disorders, including Alzheimer's disease. -
HDAC6 Inhibitor
NR160 is a selective inhibitor of histone deacetylase 6 (HDAC6), exhibiting an IC50 value of 30 nM. This compound demonstrates low cytotoxicity in leukemia cell lines and enhances the induction of apoptosis when used in conjunction with proteasome inhibitor Bortezomib, as well as chemotherapeutic agents Epirubicin and Daunorubicin. NR160 serves as a valuable tool for researchers investigating the therapeutic potential of HDAC6 inhibition in cancer treatment. -
PHD2/HDACs Inhibitor
PHD2/HDACs-IN-1 is a dual inhibitor targeting both PHD2 and various HDACs, demonstrating potent inhibitory activity with IC50 values of 1.15 μM for PHD2, 19.75 μM for HDAC1, 26.60 μM for HDAC2, and 15.98 μM for HDAC6. This compound showcases low toxicity and exhibits renoprotective effects, making it suitable for research related to cisplatin-induced acute kidney injury (AKI). Its ability to modulate epigenetic regulation and hypoxic signaling pathways positions it as a valuable tool in exploring the underlying mechanisms of renal stress responses. -
HDAC Inhibitor
YF479 is a potent inhibitor of histone deacetylases (HDACs), demonstrating significant biological activity in the modulation of gene expression. This compound impairs cell viability and suppresses both colony formation and tumor cell motility. Additionally, YF479 effectively inhibits breast tumor growth and metastasis, making it a valuable tool for research in breast cancer clinical trials. -
CYP17A1/HDAC6 Inhibitor
CYP17A1/HDAC6-IN-1 is a dual inhibitor targeting both CYP17A1 and HDAC6, exhibiting IC50 values of 0.284 μM and 0.6015 μM, respectively. This compound demonstrates significant anti-tumor activity, making it a valuable tool for research in cancer biology. Its ability to simultaneously inhibit these targets suggests potential applications in therapeutic strategies against malignancies driven by steroidogenesis and histone deacetylation. -
HDAC8 Inhibitor
HDAC8-IN-2 is a potent inhibitor of histone deacetylase 8 (HDAC8) with IC50 values of 0.27 μM for Schistosoma mansoni HDAC8 and 0.32 μM for human HDAC8. This compound demonstrates significant efficacy in killing schistosome larvae and markedly reduces the egg-laying capacity of adult worm pairs. These properties make HDAC8-IN-2 a valuable tool for research focused on schistosomiasis and histone deacetylation processes. -
HDAC3 Inhibitor
HDAC3-IN-4 is a selective inhibitor of histone deacetylase 3 (HDAC3) with an IC50 of 89 nM, demonstrating effective targeting of this enzyme. It promotes the degradation of PD-L1 through the modulation of cathepsin B (CTSB) activity in lysosomes, exhibiting a DC50 of 5.7 μM. HDAC3-IN-4 shows high selectivity for HDAC3 compared to other HDAC isoforms, including HDAC1, HDAC6, HDAC7, and HDAC8, making it a valuable tool for studying epigenetic regulation and potential immunotherapeutic approaches. -
HDAC Inhibitor
FITC-SAHA is a fluorescein-conjugated derivative of SAHA, serving as a potent inhibitor of histone deacetylases (HDACs). This compound effectively modulates histone acetylation, influencing gene expression and cellular processes. FITC-SAHA is primarily utilized in cancer research and studies related to Alzheimer's disease, facilitating the investigation of HDAC's role in these conditions. Its fluorescent labeling aids in the visualization and analysis of cellular and molecular interactions. -
PfHDAC1 Inhibitor
HDAC1-IN-4 is a potent inhibitor of Plasmodium falciparum histone deacetylase 1 (PfHDAC1), demonstrating significant antimalarial activity with an IC50 of less than 5 nM. This compound exhibits a favorable safety profile with reduced cytotoxicity. HDAC1-IN-4 serves as a valuable tool for investigating the role of histone deacetylases in malaria research and may provide insights for novel therapeutic strategies against Plasmodium falciparum infections. -
PI3K/HDAC Inhibitor
PI3K/HDAC-IN-2 is a potent dual inhibitor of phosphoinositide 3-kinase (PI3K) and histone deacetylase (HDAC), demonstrating IC50 values of 226 nM for PI3Kα, 279 nM for PI3Kβ, 467 nM for PI3Kγ, and 29 nM for PI3Kδ. It also exhibits selective inhibition with IC50 values of 1.3 nM for HDAC1, 3.4 nM for HDAC2, 972 nM for HDAC4, 17 nM for HDAC6, and 12 nM for HDAC8. Due to its significant anticancer properties, PI3K/HDAC-IN-2 is valuable for research applications in cancer biology and therapeutic development. -
HDAC
Estrogen Receptor β/HDAC Probe 1 is a near-infrared fluorescent probe designed to simultaneously target the estrogen receptor β and histone deacetylase (HDAC). This probe enables the study of dynamic interactions between these two critical proteins, facilitating the investigation of their roles in cellular signaling and gene regulation. It is particularly useful in cancer research and other studies involving estrogen signaling pathways and epigenetic modifications. -
mTOR/HDAC Inhibitor
mTOR/HDAC-IN-1 is a dual inhibitor targeting mTOR and HDAC, exhibiting IC50 values of 0.49 nM and 0.91 nM for mTOR and HDAC1, respectively. This compound demonstrates significant anti-cancer activity, making it a valuable tool for research in cancer therapeutics and signaling pathways. Its selective inhibition profile offers potential for elucidating the roles of mTOR and HDAC in tumorigenesis and for developing novel cancer treatment strategies. -
HDAC3 Inhibitor
HDAC3-IN-T247 is a potent and selective inhibitor of HDAC3 (histone deacetylase 3), demonstrating an IC50 of 0.24 µM. This compound selectively enhances the acetylation of NF-κB in HCT116 cells, making it valuable for studies in cancer and viral pathogenesis. HDAC3-IN-T247 exhibits significant anticancer properties by inhibiting the proliferation of cancer cells and can also activate HIV gene expression in latently infected cells, thus serving as a useful tool for investigations in oncology and HIV research.
