Catalog No.
Product Name
Application
Product Information
Citations
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HDAC Inhibitor
AW01178 is a Class I histone deacetylase (HDAC) inhibitor that plays a critical role in regulating gene expression. This compound has been shown to induce the upregulation of E-cadherin at both the mRNA and protein levels, effectively inhibiting the epithelial-mesenchymal transition (EMT) in breast cancer cells. AW01178 is a valuable tool for researchers investigating the mechanisms of cancer progression and potential therapeutic strategies targeting HDAC activity. -
sEH/HDAC6 inhibitor
sEH/HDAC6-IN-1 is a selective, orally active dual inhibitor of soluble epoxide hydrolase (sEH) and histone deacetylase 6 (HDAC6), exhibiting IC50 values of 2 nM for human sEH, 0.72 nM for murine sEH, and 5 nM for HDAC6. This compound demonstrates notable analgesic and anti-inflammatory properties, making it a valuable tool for research into pain management and inflammatory disorders. The ability to simultaneously target these two enzymes provides insights into their roles in various biological processes. -
HDAC Inhibitor
HDAC6-IN-38 is a potent inhibitor of histone deacetylase 6 (HDAC6) with an IC50 of 3.25 nM. This compound has demonstrated the ability to inhibit the proliferation of MGC 803 cells, making it a valuable tool for studying the role of HDAC6 in cancer biology and potential therapeutic applications. Researchers can utilize HDAC6-IN-38 to explore epigenetic regulation and its implications in various diseases. -
HDAC11 Inhibitor
ZINC000028464438 is a selective inhibitor of histone deacetylase 11 (HDAC11), exhibiting an IC50 of 3.5 µM. This compound demonstrates minimal inhibition of other HDAC isoforms, ensuring specificity in experimental applications. ZINC000028464438 is suitable for research focused on the role of HDAC11 in cellular processes and potential therapeutic interventions in related diseases. -
HDAC/Top Inhibitor
HDAC/Top-IN-1 is a potent dual inhibitor targeting histone deacetylases (HDACs) and topoisomerases, with IC50 values of 0.036 μM, 0.14 μM, 0.059 μM, 0.089 μM, and 9.8 μM for HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, respectively. This compound effectively induces apoptosis and S phase cell-cycle arrest in HEL cells, demonstrating its antiproliferative properties. Additionally, HDAC/Top-IN-1 exhibits significant in vivo antitumor efficacy, making it a valuable tool for cancer research applications. -
HDAC6 Inhibitor
HDAC6-IN-51 is a selective inhibitor of Histone Deacetylase 6 (HDAC6) with an IC50 value of 42.9 nM, demonstrating potent inhibition. This compound has shown significant anti-lung fibrosis activity, making it a valuable tool for research related to fibrotic diseases and epigenetic regulation. Its specificity for HDAC6 positions it as a promising candidate for studying the role of deacetylation in cellular processes and therapeutic interventions. -
COX-2/HDAC Inhibitor
Andrographidine E is an inhibitor of cyclooxygenase-2 (COX-2) and histone deacetylases (HDAC), with an IC50 of 19 μM for COX-2 and a strong affinity for HDAC1 and HDAC3. This compound selectively binds to macrophages, suggesting its potential as an immunotargeting agent. Andrographidine E is valuable for research applications focused on inflammation and immune modulation. -
HDAC/Sirt2 Inhibitor
Mz325 is a dual inhibitor of histone deacetylases (HDAC) and Sirtuin 2 (Sirt2), with an IC50 of 9.7 μM for Sirt2. By modulating deacetylation processes, Mz325 exhibits bioactivity that can influence cellular pathways involved in cancer progression and neurodegenerative diseases. This compound is useful for research focused on the role of epigenetic regulation in these pathologies. -
HDAC2 Inhibitor
KTT-1 is a kinetically selective and orally bioavailable inhibitor of HDAC2, demonstrating significant selectivity over HDAC1. This compound effectively inhibits osteoclast differentiation by downregulating c-Fos expression. In preclinical models, KTT-1 has shown efficacy in suppressing symptoms of arthritis, particularly in the collagen-induced arthritis (CIA) mouse model. KTT-1 is suitable for research applications related to rheumatoid arthritis and neurodegenerative diseases. -
sEH/HDAC6 Inhibitor
sEH/HDAC6-IN-2 is a potent dual inhibitor targeting soluble epoxide hydrolase (sEH) and histone deacetylase 6 (HDAC6), demonstrating IC50 values of 0.9 nM for human sEH, 46.8 nM for mouse sEH, and 8 nM for HDAC6. This compound is significant for investigating inflammatory pain mechanisms and related biological pathways, potentially aiding in the development of novel analgesics. Its dual activity positions it as a valuable tool in research focused on neuroinflammation and pain management. -
PROTAC HDAC4 Degrader
PROTAC HDAC4 Degrader-1 is a selective PROTAC that targets and promotes the degradation of HDAC4, a histone deacetylase involved in regulating gene expression. This compound effectively decreases HDAC4 protein levels, leading to S phase cell cycle arrest and reduced tumor cell proliferation, as evidenced by its impact on colony formation. Additionally, PROTAC HDAC4 Degrader-1 demonstrates efficacy in vivo in H460 mouse models, making it a valuable tool for cancer research, particularly in studies related to lung cancer. -
HDAC6/Proteasome Inhibitor
AMC-3-030 is a selective inhibitor targeting histone deacetylase 6 (HDAC6) and the chymotrypsin-like activity of the proteasome, demonstrating IC50 values of 884 nM and 4.17 nM, respectively. This compound exhibits a proliferative inhibitory effect and has been shown to reduce levels of α-tubulin and β-actin. AMC-3-030 serves as a valuable tool for investigating mechanisms related to multiple myeloma and other related research applications. -
HDAC/PDE5 Inhibitor
CM-414 is a potent dual inhibitor of phosphodiesterase 5 (PDE5) and histone deacetylases (HDACs), exhibiting IC50 values of 60 nM for PDE5 and ranging from 91 nM to 490 nM for various HDAC isoforms, including HDAC6 and HDAC1. This compound effectively reduces levels of amyloid-beta (Aβ) and phosphorylated tau (pTau) in Tg2576 mouse models, making it a valuable tool for Alzheimer's disease research. Its ability to penetrate the blood-brain barrier enhances its potential for studying neurodegenerative disorders and therapeutic interventions. -
HDAC Inhibitor
H8-A5 is a specific inhibitor of human histone deacetylase 8 (HDAC8) that employs a zinc-binding group (ZBG) within its pharmacophore design to enhance its selectivity. With IC50 values ranging from 1.8 to 1.9 μM, H8-A5 demonstrates potent antiproliferative activity in MDA-MB-231 breast cancer cells, making it a valuable tool for cancer research. Molecular docking and dynamics studies indicate strong binding affinity to HDAC8, suggesting its potential for therapeutic development in targeting HDAC-mediated pathways in oncology. -
HDAC6 Inhibitor
HDAC6-IN-37 is an inhibitor of histone deacetylase 6 (HDAC6) with demonstrated neuroprotective effects. This compound has been shown to restore the morphology of hippocampal neurons and reduce the expression of amyloid-beta (Aβ), Tau, and phosphorylated Tau (p-Tau) proteins in the hippocampus of Alzheimer's disease (AD) model rats. Additionally, HDAC6-IN-37 inhibits the formation of senile plaques and neurofibrillary tangles while regulating oxidative stress and restoring neurotransmitter balance in brain tissue, making it a valuable tool for Alzheimer's disease research and therapeutic exploration. -
CK2/HDAC Inhibitor
IOR-160 is a dual inhibitor targeting casein kinase 2 (CK2) and histone deacetylases (HDACs). It showcases high selectivity for CK2, with an IC50 of 1.7 nM, and demonstrates broad inhibitory effects on HDACs 1, 2, 3, and 6, with IC50 values of 3.3 nM, 24.0 nM, 3.9 nM, and 13.0 nM, respectively. Through the inhibition of AKT phosphorylation and the enhancement of acetylated α-tubulin levels, IOR-160 effectively modulates critical cellular signaling pathways. This compound is particularly relevant in research focused on triple-negative breast cancer, where it has been shown to inhibit tumor growth and reduce tumor burden. -
HDAC5 Activator
G194-0712 is a selective activator of histone deacetylase 5 (HDAC5), exhibiting an EC50 of 7.96 μM and a Kd of 2.53 μM. This compound promotes ACTN4-K417 deacetylation and enhances nuclear import while upregulating CSTA expression. G194-0712 has demonstrated efficacy in accelerating wound closure in chronic wound models, particularly in reducing wound area and epithelial gaps. Its applications extend to the study of chronic skin wounds, including diabetic, ischemic, and radiation injury-related wounds. -
HDACs Inhibitor
NL-103 is a potent histone deacetylase (HDAC) inhibitor, exhibiting IC50 values of 21.3 nM, 57 nM, 74 nM, and 680 nM for HDAC1, HDAC2, HDAC3, and HDAC6, respectively. This compound also targets the Hedgehog signaling pathway, leading to the downregulation of Gli2 expression. NL-103 is primarily utilized in cancer research, providing valuable insights into HDAC regulation and its role in tumor biology. -
Ligand For HDAC6/10
HDAC-IN-90 is a potent ligand for histone deacetylases HDAC6 and HDAC10. This compound exhibits selective inhibition, making it a valuable tool in the study of epigenetic regulation and cellular signaling pathways. It is particularly useful for the synthesis of PROTAC HDAC degrader-2, facilitating targeted degradation of HDAC proteins for research applications related to cancer and neurodegenerative diseases. -
HDAC Inhibitor
HDAC-IN-29 is a potent pan-histone deacetylase (HDAC) inhibitor that targets a broad range of HDAC isoforms. This compound demonstrates significant antitumor activity, making it a valuable tool in cancer research. Its ability to modulate histone acetylation provides insights into epigenetic regulation and potential therapeutic applications in oncology. -
Dual HDAC/HSP90 Inhibitor
HDAC/HSP90-IN-2 is a dual inhibitor of histone deacetylases (HDAC) and heat shock protein 90 (HSP90), exhibiting an IC50 of 360 nM for HDAC and 77 nM for HSP90α. This compound effectively induces HSP70 expression, downregulates client proteins associated with HSP90, and enhances the acetylation of α-tubulin and histone H3 in cancer cells. Additionally, HDAC/HSP90-IN-2 reduces PD-L1 expression in H1975 cells treated with IFN-γ. Its applications are particularly relevant in cancer research, including studies focused on lung and colon cancer. -
A2AAR/HDAC Inhibitor
A2AAR/HDAC-IN-1 is a potent dual inhibitor targeting the A2A adenosine receptor (A2AAR) and histone deacetylase 1 (HDAC1), with a Ki of 163.5 nM for A2AAR and an IC50 of 145.3 nM for HDAC1. This compound demonstrates significant anticancer activity, making it a valuable reagent for research in cancer therapeutics and epigenetic modulation. Its oral bioavailability enhances its utility in in vivo studies, facilitating investigations into the mechanisms underlying tumor growth and proliferation. -
HDAC6 Inhibitor
HDAC6-IN-62 is a potent and selective inhibitor of histone deacetylase 6 (HDAC6), exhibiting an IC50 value of 0.25 nM. This compound plays a significant role in modulating acetylation processes and has potential applications in the research of Charcot-Marie-Tooth disease and other neurodegenerative disorders. Its specificity for HDAC6 allows for targeted investigations into the pathways influenced by this enzyme. -
HDAC Inhibitor
Rodin-C is a selective HDAC inhibitor that demonstrates IC50 values of 0.059, 0.18, and 5.39 μM for HDAC1, HDAC2, and HDAC11, respectively, showcasing its specificity over HDAC3-10. It effectively inhibits the HDAC-CoREST complex while exhibiting low hematological toxicity. Rodin-C is suitable for research applications in neurologic disorders, including studies focused on Alzheimer’s disease. -
HDAC Inhibitor
HDAC-IN-74 is a dual inhibitor targeting histone deacetylases (HDAC) and ribonucleotide reductase (RR), exhibiting IC50 values of 10.80 μM for HDAC and 9.34 μM for RR. This compound demonstrates significant biological activity by modulating histone acetylation and affecting nucleotide synthesis. Its applications in anticancer research include investigating mechanisms of cell proliferation and apoptosis. -
HDAC Inhibitor
LW479 is a novel histone deacetylase (HDAC) inhibitor that exhibits significant potential in cancer research, particularly for breast cancer prevention. By modulating histone acetylation, LW479 can influence gene expression and promote apoptotic pathways. This compound serves as a valuable tool for investigating the role of HDACs in cancer biology and may provide insights into therapeutic strategies for breast cancer. -
HDAC6 Inhibitor
HDAC6-IN-75 is a potent inhibitor of histone deacetylase 6 (HDAC6) with an IC50 value of 0.17 nM. This compound is capable of inducing the accumulation of acetylated α-tubulin in glioma cells, leading to significant alterations in cell cycle dynamics, an increase in SubG1 cell populations, and the promotion of apoptosis in both glioma cells and glioblastoma stem cells. HDAC6-IN-75 is particularly useful for research applications focused on glioma. -
BChE/HDAC6 Inhibitor
BChE/HDAC6-IN-2 is a potent dual inhibitor targeting both butyrylcholinesterase (BChE) and histone deacetylase 6 (HDAC6), demonstrating IC50 values of 1.8 nM and 71.0 nM, respectively. This compound exhibits significant neuroprotective properties and scavenges reactive oxygen species (ROS), alongside effectively chelating metal ions such as Fe2+ and Cu2+. Furthermore, BChE/HDAC6-IN-2 inhibits tau phosphorylation and presents moderate immunomodulatory effects, making it a valuable reagent for research into neurodegenerative diseases and related pathways. -
PROTAC HDAC8 Degrader
YX862 is a selective PROTAC degrader targeting HDAC8, designed to induce robust degradation of this histone deacetylase. It achieves over 95% degradation of HDAC8 at a concentration of 250 nM in MDA-MB-231 cells. This compound serves as a valuable tool for investigating the role of HDAC8 in various biological processes and provides insights into potential therapeutic strategies for HDAC8-related diseases. -
HDAC6 Inhibitor
HDAC6-IN-12 is a potent inhibitor of histone deacetylase 6 (HDAC6), exhibiting significant anticancer activity. It functions by integrating into DNA strands, leading to DNA damage and ultimately promoting apoptosis in cancer cells. This compound is valuable for investigating the role of HDAC6 in cancer biology and therapeutic strategies targeting this pathway. -
HDAC/Hsp90 Inhibitor
HDAC/HSP90-IN-3 is a potent dual inhibitor targeting fungal Hsp90 and histone deacetylases (HDAC) with IC50 values of 0.83 μM and 0.91 μM, respectively. This compound demonstrates significant antifungal activity against azole-resistant Candida albicans. Additionally, HDAC/HSP90-IN-3 effectively suppresses key virulence factors and down-regulates drug-resistant genes such as ERG11 and CDR1, making it valuable for research in antifungal resistance and pathogenicity. -
HDAC6 Inhibitor
KH-259 is a selective inhibitor of histone deacetylase 6 (HDAC6), exhibiting an IC50 of 0.26 μM. This compound demonstrates noteworthy antidepressant effects in murine models by targeting HDAC6 within the central nervous system. KH-259 is valuable for research related to neurodegenerative diseases and the development of therapeutic strategies targeting epigenetic regulation. -
HDAC Inhibitor
Tinostamustine hydrochloride is an HDAC inhibitor that exhibits potent anti-multiple myeloma activity. This compound promotes CD38 expression and enhances the acetylation of histone H3, which increases the sensitivity of tumor cells to the anti-CD38 monoclonal antibody daratumumab. Additionally, Tinostamustine hydrochloride elevates the expression of MICA and MICB, thereby activating natural killer (NK) cells. Research indicates that this compound can significantly delay tumor growth and improve survival rates in murine models. -
HDAC Inhibitor
HDAC6-IN-8 is a potent inhibitor of histone deacetylase 6 (HDAC6), targeting the enzyme to modulate acetylation levels within cells. This compound exhibits selective inhibitory activity against HDAC6, making it valuable for studies focused on the role of HDAC6 in various cellular processes, including neuroprotection and cancer progression. Its application in epigenetic research and therapeutic development positions HDAC6-IN-8 as a critical tool in the exploration of HDAC6-related pathways. -
HDAC6 Inhibitor
NN-390 is a potent and selective inhibitor of histone deacetylase 6 (HDAC6), exhibiting an IC50 value of 9.8 nM. This compound effectively penetrates the blood-brain barrier, making it a valuable tool for neurological studies. NN-390 demonstrates potential applications in the research of metastatic Group 3 medulloblastoma (MB), offering insights into therapeutic strategies for this aggressive pediatric brain tumor. -
HDAC Activator
Curcuphenol is a histone deacetylase (HDAC) activator known for its ability to reverse immune escape mechanisms in tumor cells. By restoring the expression of antigen presentation machinery, Curcuphenol enhances immune recognition of metastatic tumors. Its synthetic analogs also exhibit similar HDAC-enhancing activity, making them valuable tools for research focused on tumor immunology and potential therapeutic strategies in cancer. -
G4/HDAC Target Agent
G4/HDAC-IN-1 is a dual-targeting compound that inhibits histone deacetylase (HDAC) activity and promotes the formation of G-quadruplex (G4) structures. With an IC50 value of 1.1 μM, this reagent effectively impedes the proliferation of triple-negative breast cancer (TNBC) cells and suppresses tumor growth in TNBC xenograft models. G4/HDAC-IN-1 is highly relevant for research into cancer biology and potential therapeutic strategies. -
HDAC6/HSP90 Inhibitor
HDAC6/HSP90-IN-1 is a potent dual inhibitor targeting both HDAC6 and HSP90, demonstrating IC50 values of 4.3 nM and 46.8 nM, respectively. This compound effectively down-regulates PD-L1 expression in INF-γ treated H1975 lung cancer cells, contributing to its potential in cancer therapy. Additionally, HDAC6/HSP90-IN-1 has shown promising efficacy in inhibiting tumor growth in human H1975 xenograft mice models, making it a valuable tool for cancer research. -
Class I HDAC Inhibitor
Largazole thiol is a potent and selective class I histone deacetylase (HDAC) inhibitor that effectively penetrates the blood-brain barrier. This compound exhibits significant antitumor and neuroprotective activities, making it a valuable tool for studying various cancer models, specifically glioblastoma. Its inhibition of HDAC activity may provide insights into therapeutic strategies for neurodegenerative diseases and cancer treatment. -
HDAC6 Inhibitor
XP5 is a potent, orally active inhibitor of HDAC6, exhibiting an IC50 of 31 nM. This compound demonstrates significant antiproliferative activity across various cancer cell lines, including those exhibiting resistance to HDAC inhibitors such as YCC3/7 gastric cancer cells (IC50 = 0.16-2.31 μM). Furthermore, XP5 has been shown to enhance antitumor immunity when used in conjunction with a PD-L1 inhibitor in melanoma research applications. -
PARP-1/HDAC Inhibitor
PARP-1/HDAC-IN-1 is a dual inhibitor targeting PARP-1 and HDAC6, exhibiting IC50 values of 68.90 nM and 510 nM, respectively. This compound demonstrates significant anticancer properties, as well as anti-migration and anti-angiogenesis activities. Its applications are relevant in cancer research, particularly in studies exploring the modulation of DNA repair mechanisms and cellular signaling pathways. -
HDAC8 Inhibitor
HDAC8-IN-12 is a selective inhibitor of histone deacetylase 8 (HDAC8) with an IC50 of 0.12 nM. This non-hydroxamic acid compound demonstrates significant anti-tumor activity, particularly in breast cancer models, by activating T cells and skewing the macrophage population towards M1 while reducing M2 macrophages. In an orthotopic mouse model of breast cancer, HDAC8-IN-12 at a dose of 50 mg/kg exhibits notable tumor suppressive effects, making it a valuable tool for research in cancer immunotherapy and epigenetic regulation. -
HDAC Inhibitor
Dihydrochlamydocin is a potent inhibitor of histone deacetylases (HDAC). This compound exhibits notable cytostatic activity against mastocytoma cells, making it valuable for studies in cancer biology and epigenetic regulation. Its ability to modulate histone acetylation provides insights into therapeutic strategies for various malignancies. -
HDAC3 Inhibitor
T326 is a selective inhibitor of histone deacetylase 3 (HDAC3) with an IC50 of 0.26 μM. This compound demonstrates significant potential in cancer research and studies related to HIV infection. T326's ability to modulate acetylation states positions it as a valuable tool for investigating therapeutic strategies targeting HDAC3. -
Class I HDAC Inhibitor
Largazole is a potent and selective Class I HDAC inhibitor, primarily targeting HDAC2 with an IC50 of 0.07 nM. Isolated from marine cyanobacteria, Largazole demonstrates significant antitumor activity against glioblastoma cell lines, including SF-268, SF-295, and SH-SY5Y, with IC50 values ranging from 62 to 102 nM. In addition to its antitumor properties, Largazole enhances the expression of key neuroprotective factors such as brain-derived neurotrophic factor (BDNF) and the transcription factor Pax6, making it a valuable reagent for research in glioblastoma and Alzheimer's disease. -
HDAC6 Inhibitor
HDAC6-IN-34 is a selective inhibitor of histone deacetylase 6 (HDAC6) with an IC50 of 18 nM, exhibiting oral bioactivity. This compound significantly increases the acetylation of tubulin while leaving histone acetylation unaffected in cutaneous T-cell lymphoma cells. In addition, HDAC6-IN-34 effectively inhibits TNF-α secretion in lipopolysaccharide-stimulated macrophages. Notably, it demonstrates potent anti-arthritic efficacy in rat models, making it a valuable tool for researching inflammatory diseases and cancer therapies. -
AChE/HDAC Inhibitor
AChE/HDAC-IN-1 is a potent dual inhibitor of acetylcholinesterase (AChE) and histone deacetylases (HDAC) with IC50 values of 0.12 nM and 0.23 nM, respectively. This compound also demonstrates antioxidant activity and metal chelating properties, making it a valuable tool in understanding neurodegenerative processes. AChE/HDAC-IN-1 is suitable for research applications related to Alzheimer's disease and other conditions associated with cholinergic dysfunction and epigenetic modifications. -
HDAC1 Inhibitor
HDAC1-IN-3 is a selective inhibitor of Histone Deacetylase 1 (HDAC1), demonstrating significant antimalarial activity against both wild-type and multidrug-resistant strains of parasites. This compound effectively exhibits a robust in vivo efficacy, resulting in notable parasiticidal effects across all developmental stages of malaria parasites. Its mechanism of action supports further exploration in antimalarial research and potential therapeutic development. -
HDAC/PDE5 Inhibitor
CM-545 is a dual inhibitor targeting both histone deacetylases (HDACs) and phosphodiesterase 5 (PDE5). With pIC50 values of 7.47 for PDE5, 6.65 for HDAC1, 6.14 for HDAC2, 6.55 for HDAC3, and 6.84 for HDAC6, CM-545 demonstrates potent inhibitory activity. This compound has applications in cancer research and therapeutic interventions related to neurodegenerative diseases and cardiovascular conditions, owing to its modulation of histone acetylation and cyclic nucleotide signaling pathways. -
HDAC1/2 Inhibitor
HDAC1-IN-10 is a selective inhibitor targeting HDAC1 and HDAC2, exhibiting potent activity with IC50 values of 6 nM and 190 nM, respectively, while showing minimal activity against HDAC3-8 (IC50 > 50 μM). This compound demonstrates efficacy in inhibiting tumor growth in HCT-116 colon cancer xenograft models, making it a valuable tool for studying the role of histone deacetylases in colon cancer research. It serves as a potential lead for therapeutic strategies aimed at HDAC-related malignancies.
