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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
HDAC Inhibitor
HDAC-IN-32 is a selective histone deacetylase (HDAC) inhibitor, demonstrating IC50 values of 5.2 nM, 11 nM, and 28 nM for HDAC1, HDAC2, and HDAC6, respectively. This compound exhibits significant antiproliferative effects against various tumor cell lines and enhances antitumor immunity in vivo. HDAC-IN-32 is valuable for research applications aimed at understanding the role of HDACs in cancer biology and developing new therapeutic strategies. -
HDAC Inhibitor
HDAC-IN-52 is a pyridine-based inhibitor targeting histone deacetylases (HDACs) with IC50 values of 0.189 μM for HDAC1, 0.227 μM for HDAC2, 0.440 μM for HDAC3, and 0.446 μM for HDAC10. This compound exhibits potent HDAC inhibition, making it a valuable tool for investigating epigenetic regulation in cancer research. Its application extends to the study of cell differentiation, apoptosis, and potential therapeutic strategies in oncology. -
HDACs/CDKs Dual Inhibitor
CDK/HDAC-IN-3 is a dual inhibitor targeting histone deacetylases (HDACs) and cyclin-dependent kinases (CDKs). It exhibits potent and selective activity, with IC50 values of 98.32 nM, 98.85 nM, 100 nM, 62.12 nM, 93.28 nM, and 82.87 nM against CDK9, CDK12, CDK13, HDAC1, HDAC2, and HDAC3, respectively. This compound is particularly relevant for research in acute myeloid leukemia (AML), providing insights into therapeutic strategies for this disease. -
HDAC6 Inhibitor
HDAC6-IN-33 is a selective and irreversible inhibitor of histone deacetylase 6 (HDAC6), exhibiting an IC50 of 193 nM. This compound demonstrates a tight-binding affinity specifically for HDAC6, effectively inhibiting its activity through a two-step slow-binding mechanism. HDAC6-IN-33 is ideal for research applications aimed at studying the role of HDAC6 in various cellular processes and disease states, including neurodegeneration and cancer. -
HDAC6 Inhibitor
HDAC6-IN-46 is a selective inhibitor of histone deacetylase 6 (HDAC6), exhibiting an IC50 value of 6.2 nM. This compound has demonstrated potential for use in Alzheimer's disease research by modulating acetylation levels, which may influence neurodegenerative processes. Its specificity towards HDAC6 makes it a valuable tool for studying the therapeutic effects of HDAC inhibition in various neurological disorders. -
HDAC8 Inhibitor
HDAC8-IN-8 is a selective inhibitor of HDAC8, exhibiting IC50 values of 23.9 μM for human HDAC8 and 268.2 μM for snail HDAC8. Additionally, it demonstrates inhibitory effects on human HDAC1 and HDAC6, with IC50 values of 12.1 μM and 2.9 μM, respectively. This compound is particularly relevant for research on schistosomiasis and may be useful for studies focused on histone deacetylase modulation in various biological contexts. -
HDAC Inhibitor
Bocodepsin is a selective inhibitor of histone deacetylases (HDACs) that exhibits significant antitumor activity. This orally active compound is effective against both solid tumors and hematologic malignancies, making it a valuable tool in cancer research. Bocodepsin's mechanism of action involves the modulation of gene expression and apoptosis, contributing to its potential therapeutic applications in oncology. -
HDAC4/6 Inhibitor
HDAC-IN-87 is a nonselective inhibitor targeting HDAC4 and HDAC6, exhibiting pIC50 values of 6.9 and 5.8 respectively. This compound demonstrates fungicidal activity against the pathogens P. sorghi and P. pachyrhizi, making it a valuable tool for studies related to fungal infections. Additionally, an acute oral LD50 greater than 500 mg/kg has been observed in both male and female rats, indicating a favorable safety profile for in vivo applications. -
HDAC Inhibitor
HDAC1/2-IN-3 is a potent inhibitor of histone deacetylases 1 and 2 (HDAC1 and HDAC2), demonstrating IC50 values of 0-5 nM and 5-10 nM, respectively. This compound plays a significant role in modulating gene expression by disrupting histone deacetylation, making it useful in research applications related to cancer biology, neurodegenerative disorders, and epigenetic modifications. Its high selectivity and potency make it a valuable tool for investigating the mechanisms of HDAC-related pathways. -
HDAC Inhibitor
5-Phenylpentan-2-one is a potent inhibitor of histone deacetylases (HDACs), playing a critical role in the regulation of gene expression through histone acetylation. This compound exhibits significant biological activity in modulating cellular processes linked to epigenetic regulation and is particularly relevant for research in urea cycle disorders. Its HDAC inhibitory properties make it a valuable tool in studies focused on cancer, neurodegenerative diseases, and other conditions influenced by epigenetic changes. -
HDAC Inhibitor
HFY-4A is a potent histone deacetylase (HDAC) inhibitor. It demonstrates significant activity against breast cancer by inhibiting cell proliferation, migration, and invasion, as well as inducing apoptosis. Additionally, HFY-4A promotes immunogenic cell death (ICD) and has been shown to inhibit tumor growth in breast cancer xenograft mouse models, making it a valuable tool for cancer research applications. -
HDAC6 Inhibitor
HDAC6-IN-26 is a potent inhibitor of histone deacetylase 6 (HDAC6), a key enzyme involved in the regulation of cellular acetylation. By inhibiting HDAC6, this compound can modulate cellular processes such as protein degradation, inflammation, and stress responses. HDAC6-IN-26 is valuable for research applications targeting neurodegenerative diseases, cancer, and other disorders associated with altered acetylation states. -
HDAC6 Inhibitor
HDAC6-IN-21 is a reversible inhibitor of histone deacetylase 6 (HDAC6), a key enzyme involved in the regulation of cellular acetylation processes. This compound demonstrates significant biological activity in modulating HDAC6-mediated pathways, making it valuable for research applications in neurodegenerative diseases and cancer biology. By inhibiting HDAC6, HDAC6-IN-21 can aid in the investigation of protein aggregation and cellular stress responses, providing insights into therapeutic potential. -
HDAC6 Inhibitor
HDAC6-IN-13 is a potent and highly selective inhibitor of HDAC6, exhibiting an IC50 of 0.019 μM. While selectively targeting HDAC6, this compound also affects HDAC1, HDAC2, and HDAC3, with IC50 values of 1.53, 2.06, and 1.03 μM, respectively. Notably, HDAC6-IN-13 demonstrates significant blood-brain barrier permeability and possesses anti-inflammatory properties, making it a valuable tool for research in neuroinflammation and associated neurological disorders. -
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. -
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. -
Telomerase Inhibitor
Braco-19 is a potent telomerase inhibitor that disrupts the capping and catalytic function of telomerase, leading to accelerated cellular senescence or selective cell death. As a G-quadruplex (GQ) binding ligand, Braco-19 effectively stabilizes G-quadruplex formation at the 3' telomeric DNA overhang, enhancing its biological activity. Additionally, Braco-19 demonstrates efficacy as an inhibitor of HAdV virus replication, making it a valuable tool for research in aging, cancer therapeutics, and virology studies. -
Viral DNA Polymerase Inhibitor
Foscarnet sodium, a viral DNA polymerase inhibitor, effectively suppresses viral replication through the reversible inhibition of polymerase activity. This compound is primarily utilized as an antiviral agent against herpesviruses, particularly in the treatment of cytomegalovirus retinitis. Its mechanism of action makes it a valuable tool for studying viral replication and evaluating therapeutic strategies against herpesvirus infections. -
Topoisomerase Inhibitor
Aclacinomycin A hydrochloride is a potent anthracycline antitumor antibiotic that primarily targets topoisomerase I and II. This compound inhibits nucleic acid synthesis, particularly RNA, and may also affect the 26S protease complex along with ubiquitin-ATP-dependent proteolysis. Due to its mechanisms of action, Aclacinomycin A hydrochloride serves valuable applications in cancer research and the study of cellular processes involving nucleic acids and proteolytic pathways. -
PARP10/PARP15 Inhibitor
PARP10/15-IN-3 is a dual inhibitor targeting PARP10 and PARP15, exhibiting IC50 values of 0.14 µM and 0.40 µM, respectively. This compound effectively penetrates cellular membranes and has demonstrated the ability to rescue cells from apoptosis. PARP10/15-IN-3 serves as a valuable tool for investigating the roles of PARP10 and PARP15 in cellular processes and offers potential applications in studies related to cancer therapy and cell survival mechanisms. -
eIF4A Inhibitor
rel-Zotatifin is a racemic isomer of Zotatifin, functioning as an inhibitor of the eukaryotic translation initiation factor 4A (eIF4A). This compound exhibits biological activity by promoting eIF4A binding to specific mRNA sequences in the 5’-UTRs, thereby disrupting the assembly of the eIF4F initiation complex. Its key research applications include the study of translation regulation and potential therapeutic interventions in conditions driven by aberrant protein synthesis. -
HDAC Class I Inhibitor
HDAC-IN-27 dihydrochloride is a potent inhibitor of class I histone deacetylases (HDAC1-3) with IC50 values ranging from 0.43 to 3.01 nM. This compound displays significant antitumor activity both in vitro and in vivo, particularly against acute myeloid leukemia (AML) cell lines, through mechanisms that include apoptosis induction and increased histone acetylation (AcHH3 and AcHH4). HDAC-IN-27 dihydrochloride is an important tool for investigating the roles of HDACs in cancer biology, specifically within the context of AML research. -
SIRT1 Inhibitor
JGB1741 is a potent and selective inhibitor of SIRT1, exhibiting an IC50 of approximately 15 μM. It displays weak inhibitory effects on SIRT2 and SIRT3, with IC50 values greater than 100 μM. JGB1741 enhances the levels of acetylated p53, promoting p53-mediated apoptosis through modulation of the Bax/Bcl2 ratio, cytochrome c release, and PARP cleavage. This compound is valuable for research applications focusing on breast cancer. -
DNA Topoisomerase I Inhibitor
Isodiospyrin is a natural dimeric naphthoquinone that functions as an inhibitor of human DNA topoisomerase I. By blocking DNA relaxation and the kinase activities of this enzyme, Isodiospyrin exhibits significant anticancer, antibacterial, and antifungal properties. This compound is valuable for research applications focused on cancer therapy and microbial resistance. -
PARP-1 Inhibitor
CEP-6800 is a potent inhibitor of PARP-1, known for its ability to enhance the efficacy of chemotherapeutic agents. It effectively reduces poly(ADP-ribose) accumulation induced by irinotecan and temozolomide in LoVo and HT29 xenograft models. Additionally, CEP-6800 demonstrates potential in suppressing tumor growth in Calu-6. This compound is valuable for research in cancer biology and therapy development. -
PARP-1/-2 inhibitor
CEP-9722 is a selective, orally active inhibitor of PARP-1 and PARP-2, exhibiting IC50 values of 20 nM and 6 nM, respectively. This compound demonstrates significant anticancer activity, making it a valuable tool for research in cancer therapy and DNA repair mechanisms. Its ability to inhibit these critical enzymes positions CEP-9722 as an important reagent for studying cellular responses to DNA damage and tumor susceptibility to therapeutic agents. -
PARP7 Inhibitor
PARP7-IN-21 is a potent inhibitor of PARP7, demonstrating an IC50 of less than 10 nM. This compound effectively interferes with the activity of PARP7, which is involved in the regulation of cellular processes such as DNA repair and signaling pathways related to stress response. PARP7-IN-21 is valuable for research applications focused on cancer biology, neurodegenerative diseases, and other conditions associated with PARP7 dysregulation. -
CDK9/PARP Inhibitor
CDK9/PARP-IN-1 is a potent inhibitor of CDK9 and PARP1, demonstrating IC50 values of 118 nM and 107 nM, respectively. This dual inhibition results in significant antiproliferative effects across various cancer cell lines, making it a valuable tool for cancer research. CDK9/PARP-IN-1 is particularly relevant for studies investigating the therapeutic potential of targeting these pathways in oncology. -
PARP1/CDK12 Inhibitor
Antitumor agent-104 is a potent inhibitor of PARP1 and CDK12, targeting critical pathways in DNA damage repair in tumors. By inhibiting PARP1 enzymatic activity, it effectively reduces PAR protein levels, thus impairing the cellular mechanisms that protect tumor cells. This compound serves as a valuable tool in cancer research, especially in studies focused on understanding tumor biology and exploring novel therapeutic strategies. -
PARP1 Inhibitor
PARP1-IN-53 is a potent PARP1 inhibitor with an IC50 of 0.1 nM, demonstrating high selectivity over PARP2, which has an IC50 of 23 nM. This quinazolinone derivative effectively interferes with the poly(ADP-ribose) polymerase 1 enzyme, making it a valuable compound for cancer research. Its specific action on PARP1 enables detailed studies into the mechanisms of DNA repair and cell survival in oncology. -
PARP Inhibitor
INO-1001 mesylate is a selective inhibitor of poly (ADP-ribose) polymerase (PARP), a critical enzyme involved in DNA repair processes. It enhances the sensitivity of cancer cells to radiation therapy by disrupting DNA repair mechanisms, leading to increased necrotic cell death. This compound is of interest in cancer research, particularly in studies aimed at overcoming resistance to radiation and improving therapeutic outcomes in tumorigenesis. -
PARP-1/2 Inhibitor
CEP-8983 is a potent inhibitor of PARP-1 and PARP-2, with IC50 values of 20 nM and 6 nM, respectively. This compound effectively enhances the sensitivity of chemotherapy-resistant cell lines and subcutaneous xenograft models to the anticancer agents Temozolomide and Camptothecin. Its ability to disrupt DNA repair mechanisms makes CEP-8983 a valuable tool for cancer research, particularly in studies focusing on therapeutic resistance and combination therapies.
