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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
HDAC2 Inhibitor
HDAC2-IN-2 is a selective inhibitor of histone deacetylase 2 (HDAC2), exhibiting a Kd value ranging from 0.1 to 1 μM. This compound is instrumental in studying the role of HDAC2 in various biological processes, including gene expression regulation and cell differentiation. Its inhibitory action makes it a valuable tool for researchers investigating epigenetic modifications and potential therapeutic targets in cancer and neurodegenerative diseases. -
LSD1/HDAC6/MAO-A Inhibitor
LSD1/HDAC6-IN-2 is a potent inhibitor targeting LSD1, HDAC6, and MAO-A, with IC50 values of 5 nM, 11 nM, and 5 nM, respectively. It demonstrates significant inhibitory effects on the growth of multiple myeloma cell lines, including MM.1S, MM.1R, and RPMI-8226. This compound is suitable for research applications focused on acute myeloid leukemia and lymphoma, providing insights into potential therapeutic mechanisms. -
HDAC3 Inhibitor
PT3 is a selective inhibitor of histone deacetylase 3 (HDAC3), demonstrating an IC50 value of 0.25 μM. This compound shows promising brain penetration capabilities and bioavailability following oral administration. PT3 is valuable for investigating the role of HDAC3 in neurodegenerative disorders, particularly in the context of Alzheimer’s disease research. -
HDAC3 Inhibitor
(E,E)-RGFP966 is a selective inhibitor of Histone Deacetylase 3 (HDAC3) that is capable of penetrating the central nervous system. This compound is particularly relevant for the investigation of neurodegenerative disorders, including Huntington's disease. Its specificity for HDAC3 makes it a valuable tool in studying the epigenetic regulation of gene expression and the accompanying mechanistic pathways involved in this condition. -
DNMT And HDAC Aual Inhibitor
DNMT/HDAC-IN-1 is a dual inhibitor targeting DNA methyltransferases (DNMT) and histone deacetylases (HDACs), demonstrating IC50 values of 56.84 nM for HDAC1 and 17.39 nM for HDAC6. This compound induces apoptosis in tumor cells and is valuable for cancer research applications, providing insights into the mechanisms of epigenetic regulation in malignancies. Its role in modulating both DNMT and HDAC activities makes it a significant tool for investigating therapeutic strategies in oncology. -
HDAC1 Inhibitor
HDAC1-IN-7 is a potent inhibitor of histone deacetylase 1 (HDAC1), exhibiting an IC50 of 0.957 mM. This compound serves as a valuable tool for investigating the role of HDAC1 in various biological processes, including gene expression regulation and cellular differentiation. Its application is relevant in studies of cancer biology and neurodegenerative disorders, where modulation of HDAC1 activity may provide insights into therapeutic strategies. -
HDAC11 Inhibitor
HDAC11-IN-2 is a selective inhibitor of Histone Deacetylase 11 (HDAC11), exhibiting an IC50 of 51.1 µM for HDAC11 and 5 µM for HDAC8. This compound effectively inhibits de novo lipogenesis and promotes fatty acid oxidation, addressing hepatic lipid accumulation and its associated pathological features in MASLD mouse models. Additionally, HDAC11-IN-2 enhances the phosphorylation of AMPKα1 at Thr172, further regulating metabolic pathways involved in lipid metabolism within the liver. -
HDAC6 Inhibitor
Bavarostat is a potent inhibitor of histone deacetylase 6 (HDAC6) with an IC50 of 17 nM, capable of crossing the blood-brain barrier. As a PET radiotracer, it can be labeled with 18F for in vivo mapping of HDAC6 distribution and assessing target occupancy in non-human primate models. Bavarostat selectively enhances tubulin acetylation without affecting histone acetylation, making it a valuable tool for research into neurodegenerative diseases, such as Alzheimer’s, as well as various cancers. -
HDAC11 Inhibitor
TD034 is a selective, reversible, and noncovalent inhibitor of HDAC11, exhibiting an IC50 value of 5.1 nM and a Ki of 1.5 nM. This compound specifically targets HDAC11 without affecting other histone deacetylases or sirtuins, and it inhibits the defatty acylation of the substrate SHMT2. Additionally, TD034 reduces the levels of YAP1 through its action on HDAC11. This reagent is suitable for investigating the role of HDAC11 in lung cancer research. -
HDAC6/MAO-A/LSD1 Inhibitor
HDAC6-IN-3 is a potent inhibitor of histone deacetylase 6 (HDAC6), with an IC50 ranging from 0.02 to 1.54 μM for various HDAC isoforms, including HDAC1, HDAC2, HDAC3, and HDAC8. Additionally, it exhibits significant inhibitory activity against monoamine oxidase A (MAO-A) with an IC50 of 0.79 μM and lysine-specific demethylase 1 (LSD1). This compound serves as a valuable tool for research applications in cancer biology and epigenetics and is equipped with an alkyne functionality, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc). -
HDAC6 Inhibitor
HDAC6-IN-23 is a potent inhibitor of the histone deacetylase HDAC6, exhibiting oral bioavailability. This compound demonstrates significant biological activity by modulating histone acetylation, which plays a crucial role in gene regulation and cellular processes. It is primarily utilized in research focused on neurodegenerative disorders, cancer therapy, and the study of protein homeostasis. -
HDAC6/10 Inhibitor
HDAC-IN-4 is a selective inhibitor of HDAC6 and HDAC10, demonstrating pIC50 values of 7.2 and 6.8 in BRET assays, respectively. This compound exhibits antitumoral activity, making it a significant tool for the investigation of cancer biology and the modulation of gene expression. Its selective inhibition of these histone deacetylases positions HDAC-IN-4 as a valuable reagent for research focusing on epigenetic regulation and potential therapeutic applications in cancer treatment. -
HDAC Inhibitor
BG48 is a potent histone deacetylase (HDAC) inhibitor that selectively targets HDAC1 and HDAC2. By inhibiting the enzymatic activity of these enzymes, BG48 modulates gene expression and can influence cellular processes such as differentiation, proliferation, and apoptosis. This compound is valuable for research applications in cancer biology, neurodegenerative diseases, and epigenetic studies. -
HDAC I/IIb Inhibitor
Purinostat is a selective inhibitor of histone deacetylases (HDAC) I and IIb, exhibiting potent anti-leukemic activity. It effectively reduces the survival of Philadelphia chromosome-positive leukemic cells and CD34+ leukemic progenitors from chronic myeloid leukemia patients. By targeting HDAC I/IIb, Purinostat disrupts critical pathways for leukemic stem cell survival, influencing factors such as c-Myc, β-Catenin, E2F, Ezh2, Alox5, and mTOR. Additionally, Purinostat enhances glutamate metabolism in leukemic stem cells by upregulating GLS1. -
HDAC Inhibitor
HNHA is a potent histone deacetylase (HDAC) inhibitor with an IC50 of 100 nM. The compound effectively induces cell cycle arrest at the G1/S phase through the upregulation of p21. HNHA has demonstrated the ability to inhibit tumor growth and neovascularization, suggesting potential applications in cancer research, particularly in the context of breast cancer therapeutics. -
HDAC Inhibitor
HDAC-IN-40 is a potent alkoxyamide-based inhibitor of histone deacetylases (HDACs), specifically targeting HDAC2 and HDAC6 with Ki values of 60 nM and 30 nM, respectively. This compound exhibits significant antitumor activity, making it a valuable tool for cancer research. HDAC-IN-40 can be utilized to explore the role of histone deacetylation in tumor development and progression, as well as to investigate potential therapeutic interventions in various cancers. -
HDAC1/2 Inhibitor
BG47 is a selective inhibitor of histone deacetylases HDAC1 and HDAC2, functioning as an optoepigenetic probe. Upon light-induced trans-to-cis isomerization, BG47 competitively inhibits the deacetylase activity of its targets, resulting in increased acetylation of Histone H3K9. This compound is relevant for research applications in neurological diseases, providing insights into epigenetic regulation and its implications in various disorders. -
PARP Inhibitor
PARP/EZH2-IN-1 is a potent dual inhibitor targeting PARP and EZH2, with respective IC50 values of 6.87 nM and 36.51 nM. This reagent demonstrates significant biological activity in the treatment of triple-negative breast cancer, particularly in cells with wild-type BRCA. Its unique mechanism of action makes it a valuable tool for research into cancer biology and therapeutic development. -
HDAC Inhibitor
HDAC-IN-48 is a potent inhibitor of histone deacetylases (HDACs) that exhibits significant cytotoxicity, with a GI50 of approximately 20 nM. This hybrid molecule incorporates pharmacophores from SAHA and CETZOLE, effectively inducing ferroptosis while inhibiting HDAC activity. Additionally, HDAC-IN-48 features an alkyne group, allowing it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions, making it a valuable tool for click chemistry applications in chemical biology and therapeutic research. -
HDAC11 Inhibitor
HDAC11-IN-3 is a selective inhibitor of HDAC11, exhibiting an IC50 of 4.1 nM. This compound demonstrates potent anti-acute myeloid leukemia (AML) activity against U937 and OCI-AML2 cell lines with an IC50 of 10 μM. It effectively induces apoptosis, cell cycle arrest, and differentiation while upregulating iron transporters transferrin (TF) and transferrin receptor (TFRC). Additionally, HDAC11-IN-3 activates the p62-Keap1-Nrf2-HMOX1 pathway, resulting in elevated intracellular iron levels and subsequent ferroptosis in AML cells. This reagent is suited for studies investigating the molecular mechanisms of AML and can be utilized alone or in combination with other therapeutic agents like Cytarabine. -
DNA Topoisomerase II/Topoisomerase I Inhibitor
Eupolauridine is a selective inhibitor of DNA topoisomerase II, showing inhibitory concentrations (IC50) of 20 μM for fungal topoisomerase I and 33 μM for human topoisomerase I. This compound exerts antifungal activity by impairing the catalytic function of topoisomerase II and stabilizing its cleavage complex with DNA, resulting in DNA damage. Eupolauridine holds potential for research applications in the study of fungal infectious diseases. -
Topoisomerase I/II Inhibitor
Luotonin A is a potent inhibitor of topoisomerase I and II. It exhibits significant antiviral activity against tobacco mosaic virus (TMV) and demonstrates antitumor properties. This compound is valuable for research applications in virology and oncology, providing insights into enzyme inhibition and potential therapeutic strategies against viral infections and cancer. -
Topoisomerase II Inhibitor
Amrubicin hydrochloride is a potent inhibitor of DNA topoisomerase II, a key enzyme involved in DNA replication and repair. This compound exhibits significant antitumor activity and has been studied for its efficacy in various cancer models. It is utilized in research to explore mechanisms of action in chemotherapy and to evaluate potential therapeutic strategies against tumors. -
Type IIA Topoisomerases Inhibitor
GSK945237 is a potent inhibitor of bacterial type IIA topoisomerases, exhibiting strong bactericidal activity. It demonstrates broad-spectrum efficacy against both Gram-positive and Gram-negative bacteria, with an IC50 of 0.034 μg/mL against Helicobacter influenzae DNA gyrase. In vivo studies indicate significant effectiveness in a rat model of respiratory tract infection, highlighting its potential applications in anti-infection research. -
Topoisomerase II Inhibitor
CP-67015 is a potent topoisomerase II inhibitor that exhibits direct mutagenic effects in mammalian cells, impacting both gene and chromosomal levels. As a quinolone antibiotic, it demonstrates significant biological activity, making it a valuable tool for researchers investigating DNA manipulation and repair mechanisms. CP-67015 is suitable for studies focused on the role of topoisomerase II in cellular processes and the effects of targeted DNA damage. -
Topoisomerase Inhibitor
(1R,2S,7R)-Sitafloxacin is a potent inhibitor of topoisomerases, specifically targeting DNA gyrase with an IC50 of 0.18 μg/mL. This stereoisomer's activity highlights its potential in elucidating the role of topoisomerase-mediated DNA manipulation in various biological processes. It serves as a valuable tool in molecular and cellular research applications focusing on DNA replication and repair mechanisms. -
DNA Topoisomerase Inhibitor
(5-Cl)-Exatecan is a potent inhibitor of DNA topoisomerase, primarily utilized in cancer research settings. This compound functions as an antibody-drug conjugate (ADC) cytotoxin, targeting and disrupting the DNA replication process in cancer cells. Its efficacy in selectively inducing cytotoxicity makes it a valuable tool for studying cancer therapeutics and exploring the mechanisms of drug resistance. -
Telomerase Inhibitor
L2H2-6OTD is a potent telomerase inhibitor that functions through G-quadruplex stabilization. This compound demonstrates significant telomerase inhibitory activity with an IC50 value of 15 nM, making it a valuable tool in cancer research. It can be utilized to investigate telomere biology, the mechanisms underlying cellular aging, and potential therapeutic strategies targeting telomerase in cancer cells. -
Topoisomerase Inhibitor
MC-DOXHZN (hydrochloride) is a topoisomerase II inhibitor that serves as an albumin-binding proagent of Doxorubicin. This compound features acid-sensitive properties, enabling it to selectively release Doxorubicin in tumor microenvironments. MC-DOXHZN is particularly valuable for antibody-drug conjugate (ADC) synthesis, facilitating targeted cancer therapies. Its unique mechanism enhances the potential for effective treatment strategies in oncology research. -
TROP2 Directed Agent, Topoisomerase I Inhibitor
Sacituzumab tirumotecan is an antibody-drug conjugate that functions as a TROP2-directed agent and a topoisomerase I inhibitor. With a TROP2 EC50 of 2.787 ng/ml and a topoisomerase I IC50 of 0.7 μmol/L, it effectively delivers its cytotoxic payload to target cells. This compound is utilized in research focusing on metastatic triple-negative breast cancer and metastatic non-small cell lung cancer, making it crucial for studies aimed at understanding treatment mechanisms and therapeutic efficacy in these challenging malignancies. -
Topoisomerase Inhibitor
(4-NH2)-Exatecan is a topoisomerase inhibitor and a derivative of Exatecan. It exhibits significant biological activity by disrupting the DNA replication process, making it a valuable tool in cancer research. Additionally, (4-NH2)-Exatecan is suitable for the synthesis of antibody-drug conjugates (ADCs), facilitating targeted therapeutic applications in oncology. -
Topoisomerase I Inhibitor
NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT is a topoisomerase I inhibitor that effectively interferes with DNA replication and transcription by stabilizing the DNA-enzyme complex. This compound demonstrates significant potential in antibody-drug conjugate (ADC) applications, showing efficient delivery to cells for targeted therapy. Its efficacy has been validated in both in vivo and in vitro models, making it a valuable tool for cancer research and therapeutic development. -
DNA Topoisomerase I Inhibitor
Ac-Exatecan is an acetylation-modified derivative of Exatecan, primarily functioning as an inhibitor of DNA Topoisomerase I, with an IC50 of 2.2 μM. This compound exhibits significant antitumor activity, making it a valuable payload for antibody-drug conjugate (ADC) applications. Ac-Exatecan is particularly effective against cells with P-glycoprotein-mediated multidrug resistance, offering potential in overcoming therapeutic challenges associated with resistant tumor types. -
DNA topoisomerase I Inhibitor
(αR)-Cyclopropaneacetamide-Exatecan is a potent inhibitor of DNA topoisomerase I, exhibiting enhanced membrane permeability with an IC50 value of 1.34 μM against the human enzyme. This compound induces cytotoxicity through the suppression of topoisomerase I activity, displaying anticancer effects that are independent of HER2 expression levels. Derived from Exatecan, (αR)-Cyclopropaneacetamide-Exatecan serves as an antibody-drug conjugate cytotoxin and is applicable in research on various advanced cancers, including breast, gastric, colorectal, and non-small cell lung cancers. -
Topoisomerase Inhibitor
Mal-Exatecan is a maleimide-modified derivative of Exatecan, acting primarily as a DNA topoisomerase I inhibitor. This compound demonstrates potent antitumor activity by stabilizing the topoisomerase-DNA complex, leading to DNA strand breaks and subsequent cell death in rapidly dividing cancer cells. Mal-Exatecan is primarily utilized in cancer research to explore therapeutic strategies targeting topoisomerase I. -
DNA topoisomerase I Inhibitor
DRF-1042 is a potent inhibitor of DNA topoisomerase I, derived from Camptothecin. It demonstrates significant anticancer activity against a diverse range of human cancer cell lines, including those exhibiting multi-drug resistance (MDR). This compound is valuable for research applications focused on cancer therapeutics and the mechanisms of resistance in tumor cells. -
Topoisomerase I Inhibitor
Exatecan mesylate dihydrate is a potent inhibitor of DNA topoisomerase I, exhibiting an IC50 of 2.2 μM (0.975 μg/mL). This compound is particularly relevant in cancer research, as it interferes with DNA relaxation during replication, subsequently leading to apoptosis in rapidly dividing cells. Its application extends to various studies focused on chemotherapeutic mechanisms and the development of novel anti-cancer therapies. -
DNA topoisomerase I Inhibitor
Rebeccamycin is a potent inhibitor of DNA topoisomerase I, a key enzyme involved in DNA replication and transcription. This antitumor antibiotic primarily exerts its cytotoxic effects by stabilizing the topoisomerase I-DNA cleavage complex, leading to DNA damage and apoptosis in cancer cells. Rebeccamycin shows minimal activity against protein kinase C and topoisomerase II, making it a selective agent for research in cancer biology and therapeutic development. -
Topoisomerase I Inhibitor
Exatecan hydrochloride is a potent inhibitor of DNA topoisomerase I, exhibiting an IC50 value of 2.2 μM (0.975 μg/mL). This compound is primarily utilized in cancer research, facilitating investigations into the mechanisms of tumor cell proliferation and survival by disrupting the topological state of DNA during replication. Its activity makes it a valuable tool for exploring therapeutic options and treatment strategies in oncology. -
Topoisomerase I Inhibitor
Exatecan analog 38 is a potent topoisomerase I inhibitor derived from camptothecin. This compound exhibits significant cytotoxicity against various cancer cell lines, making it a valuable tool for oncology research. Exatecan analog 38 can be utilized in the development of antibody-drug conjugates (ADCs) by conjugating it to monoclonal antibodies through linkers, enhancing targeted therapeutic applications. -
Topoisomerase I Inhibitor
LD2-3 is a potent inhibitor of topoisomerase I, an enzyme crucial for DNA replication and transcription. This compound can be conjugated to monoclonal antibodies via linkers to create antibody-drug conjugates (ADCs), facilitating targeted therapy applications. LD2-3 is particularly suited for use in studies involving carcinoembryonic antigen (CEA) overexpressing tumors, enabling researchers to explore its efficacy in a precision oncology context. -
eIF4A Inhibitor
eIF4A-IN-2 is a potent inhibitor of the eukaryotic translation initiation factor 4A (eIF4A). This compound demonstrates significant cytotoxic activity and can be utilized as a valuable payload in the synthesis of antibody-drug conjugates (ADCs). Researchers investigating translation regulation and therapeutic strategies in cancer may find eIF4A-IN-2 particularly useful for advancing their studies. -
HDAC1 Inhibitor, NTR/pH Fluorescence Inducer
HDAC-IN-101 is a selective inhibitor of HDAC1, exhibiting an IC50 of 65 nM against human HDAC1. This compound effectively inhibits cancer cell proliferation by targeting HDAC1 activity. In addition, HDAC-IN-101 is metabolically activated by overexpressed nitroreductase to produce H6AQ, which displays fluorescence under low pH conditions. Its unique properties make it valuable for applications in cancer research and cellular imaging studies. -
ATR Inhibitor
ATR-IN-31 is a selective ATR kinase inhibitor that exhibits an IC50 of 7 nM, demonstrating its potent activity. This compound functions by specifically inhibiting ATR kinase activity without significantly affecting ATM kinase. ATR-IN-31 has shown efficacy in reducing the viability of prostate cancer cells, making it a valuable tool for research focused on prostate cancer. -
ATM/ DNA-PKcs Inhibitor
XRD-0394 is a highly potent and orally active inhibitor of ATM and DNA-PKcs, exhibiting IC50 values of 0.39 nM and 0.89 nM, respectively. This compound demonstrates selectivity for its target enzymes over other members of the PIKK and PI3K families. In preclinical studies, XRD-0394 has been shown to significantly enhance the cytotoxic effects of ionizing radiation on tumor cells both in vitro and in vivo. Additionally, it can synergize with PARP and topoisomerase I inhibitors, making it a valuable tool for research in cancer treatment and DNA repair mechanisms. -
ATR Inhibitor
(S)-Ceralasertib is an ATR inhibitor, specifically targeting ataxia telangiectasia mutated and rad3 related (ATR) signaling pathways. This compound exhibits significant potential in cancer research by enhancing the sensitivity of tumor cells to DNA-damaging agents through inhibition of the ATR pathway. (S)-Ceralasertib is utilized in studies aimed at understanding the roles of DNA repair mechanisms and evaluating combination therapies for various cancers. -
ATM Inhibitor
WSD0628 is a potent ATM inhibitor known for its ability to cross the blood-brain barrier. It exhibits significant radiosensitizing effects, making it a valuable tool for research in cancer therapy and radiobiology. Its inhibition of the ATM pathway has implications for enhancing the efficacy of radiotherapy in various malignancies.
