Catalog No.
Product Name
Application
Product Information
Citations
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POLA1/HDAC 11 Inhibitor
MIR002 is a potent, orally bioavailable dual inhibitor targeting DNA polymerase α (POLA1) and histone deacetylase 11 (HDAC11). It induces p53 acetylation, upregulates p21 expression, and triggers G1/S cell cycle arrest followed by apoptosis. MIR002 demonstrates significant antitumor efficacy in vivo, highlighting its potential as a therapeutic agent for cancers driven by POLA1 and HDAC11 dysregulation. -
HDAC1 and HDAC2 inhibitor
KPZ560 is a potent inhibitor of histone deacetylases HDAC1 and HDAC2, with IC₅₀ values of 12 nM and 68 nM, respectively. It has been shown to enhance dendritic spine density in granule neurons of mice, indicating potential neurotrophic effects. Additionally, KPZ560 inhibits the proliferation of MCF breast cancer cells, supporting its potential application in both neurobiological and oncological research. -
HDAC6 inhibitor
MPI_5a is a potent and selective inhibitor of histone deacetylase 6 (HDAC6), with an IC₅₀ of 36 nM. It exhibits minimal activity against other HDAC isoforms, demonstrating high isoform selectivity. In cellular assays, MPI_5a effectively inhibits acylated tubulin accumulation with an IC₅₀ of 210 nM, highlighting its utility in modulating HDAC6-dependent processes for potential therapeutic applications. -
HDAC6 inhibitor
QTX125 is a potent and highly selective inhibitor of histone deacetylase 6 (HDAC6), demonstrating excellent specificity over other HDAC isoforms. It exhibits significant antitumor activity through selective inhibition of HDAC6-mediated pathways. Both the salt and free base forms of QTX125 display comparable biological activity at equivalent molar concentrations, ensuring consistent pharmacological effects across different formulations. -
VDR agonist
Triciferol is a multifunctional small molecule that acts as both a vitamin D receptor (VDR) agonist and a histone deacetylase (HDAC) antagonist. It binds directly to VDR with an IC₅₀ of 87 nM and exhibits 1,25-dihydroxyvitamin D₃ (1,25D)-like potency in activating multiple VDR target genes. In addition to its transcriptional effects, Triciferol induces significant tubulin hyperacetylation and enhances histone acetylation, contributing to its antiproliferative and cytotoxic activities. This dual mechanism highlights its potential as a therapeutic agent in cancer and epigenetic modulation. -
HDAC3/8 PROTAC degrader
YX968 is a potent and selective PROTAC degrader targeting histone deacetylases HDAC3 and HDAC8, with DC₅₀ values of 1.7 nM and 6.8 nM, respectively. By inducing degradation of these epigenetic regulators, YX968 promotes apoptosis and exhibits significant antitumor activity, representing a promising therapeutic strategy for cancers driven by aberrant HDAC3/8 activity. -
FFAR3 agonist
AR420626 is a selective agonist of free fatty acid receptor 3 (FFAR3, also known as GPR41), with an IC₅₀ of 117 nM. It demonstrates anti-inflammatory, antitumor, and antidiabetic activities. AR420626 improves neurogenic diarrhea by modulating neural pathways mediated by nicotinic acetylcholine receptors (nAChRs). In cancer models, it suppresses the growth of HepG2 xenografts and inhibits hepatoma cell proliferation through apoptosis induction. Additionally, AR420626 mitigates allergic asthma and eczema and enhances glucose uptake by activating FFAR3-mediated Ca²⁺ signaling, offering potential therapeutic benefits in metabolic disorders such as diabetes. -
HDAC Degrader
JPS016 is a benzamide-based PROTAC that recruits the Von Hippel-Lindau (VHL) E3 ligase to selectively degrade class I histone deacetylases (HDACs). It is a potent degrader of HDAC1/2, leading to broad transcriptional changes and enhanced apoptosis in HCT116 cells, supporting its application in epigenetic and cancer research. -
HDAC4 Inhibitor
HDAC-IN-2 is a selective inhibitor of histone deacetylase 4 (HDAC4) with a notable affinity for Class IIa enzymes. This compound is a valuable research tool for the investigation of epigenetic regulation and the modulation of gene expression. It is particularly suitable for high-throughput screening applications and can aid in the development of novel therapeutic strategies targeting HDAC-mediated pathways. -
HDAC6 Inhibitor
HDAC6-IN-39 is a potent inhibitor of histone deacetylase 6 (HDAC6) with an IC50 of 0.0096 μM. By selectively targeting HDAC6, this compound modulates protein acetylation levels, influencing various cellular processes including protein aggregation and autophagy. HDAC6-IN-39 is useful in research focused on neurodegenerative diseases, cancer therapy, and the regulation of immune responses. -
HDAC Inhibitor
Martinostat is a hydroxylated dialkylcarbamate compound that functions as a histone deacetylase (HDAC) inhibitor. It exhibits significant biological activity by altering acetylation levels, which can influence gene expression and cellular responses. This reagent has applications in the study of neurological disorders and cancer, as well as potential use in quantitative imaging of HDAC activity in vivo across various tissues, including the central nervous system and major peripheral organs. -
HDAC Inhibitor
YF438 is a potent histone deacetylase (HDAC) inhibitor that exhibits significant anti-cancer activity both in vitro and in vivo. It effectively impedes the growth and metastasis of triple-negative breast cancer (TNBC) cells by disrupting the interaction between HDAC and MDM2, leading to the dissociation of MDM2-MDMX complexes and promoting MDM2 degradation. This compound is valuable for research focused on cancer biology and the development of targeted therapies for aggressive tumor types. -
HDAC inhibitor
KBH-A42 is a potent histone deacetylase (HDAC) inhibitor that exhibits notable anti-inflammatory activity. It effectively reduces TNF-α and nitric oxide (NO) production in LPS-induced murine macrophage RAW 264.7 cells, demonstrating IC50 values of 1.10 µM and 2.71 µM, respectively. This compound is valuable for research applications focused on inflammation and related signaling pathways. -
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. -
HDACi
ZYJ-25e is a potent histone deacetylase inhibitor (HDACi) that selectively targets HDAC6 and HDAC8, exhibiting IC50 values of 0.047 μM and 0.139 μM, respectively. As a tetrahydroisoquinoline-bearing hydroxamic acid analogue, ZYJ-25e demonstrates significant antitumor efficacy in the MDA-MB231 xenograft model. This compound is valuable for research applications exploring the role of HDAC inhibition in cancer therapeutics. -
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. -
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.
