Catalog No.
Product Name
Application
Product Information
Citations
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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. -
PROTAC HDAC Degrader
JPS036 is a benzamide-based HDAC degrader that operates through the Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimera (PROTAC) mechanism. This compound selectively degrades class I histone deacetylases (HDAC1 and HDAC2), demonstrating significant biological activity by promoting the expression of differentially expressed genes and enhancing apoptosis in HCT116 cells. JPS036 serves as a valuable research tool for studying the roles of HDACs in cellular processes and disease models. -
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. -
HDAC6 Inhibirotr
HDAC6-IN-65 is a selective inhibitor of histone deacetylase 6 (HDAC6) with an IC50 of 0.9 nM, demonstrating additional inhibitory effects on HDAC3 with an IC50 of 39.4 nM. This compound induces the accumulation of acetylated α-tubulin and acetylated histone H3 in Neuro-2a cells, serving as a marker for class I HDAC inhibition. HDAC6-IN-65 provides valuable insights in the study of melanoma and related cancer research applications. -
SIRT1 Activator
BML-278 is a potent SIRT1 activator with an effective concentration (EC150) of 1 μM. It enhances histone modifications by increasing H3K9 methylation and inhibiting H3K9 acetylation, which contributes to improved early embryonic development. Additionally, BML-278 induces G1/S phase cell cycle arrest and reduces senescence in primary human mesenchymal cells. In U937 cells, this compound reduces tubulin acetylation while promoting increased mitochondrial density in murine C2C12 myoblasts, highlighting its versatility in cellular and developmental research applications. -
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. -
Nucleoside Analog
Galocitabine is a nucleoside analog that functions primarily by inhibiting nucleic acid synthesis, leading to the suppression of cancer cell proliferation and antiviral activity. This compound exhibits notable efficacy against various cancer types and can be utilized in research focused on exploring therapeutic strategies for oncological and viral diseases. Its mechanism makes it a valuable tool in studying cellular responses and treatment pathways in cancer biology and virology. -
Fluorescence Dye
Cy5 maleimide is a cyanine-based fluorescent dye that covalently binds to thiol groups in proteins and other biomolecules. Characterized by its long wavelength emission, high extinction coefficient, and excellent water solubility, Cy5 maleimide is ideal for applications in fluorescence microscopy, flow cytometry, and other labeling techniques. The straightforward mixing reaction facilitates efficient labeling of proteins and antibodies, making it a valuable tool for various biological research applications, including immunoassays and in vivo imaging studies. -
Fluorescent Dye
CY5-N3 (Sulfo-Cyanine5-azide) is a cell-permeable fluorescent dye, with excitation and emission wavelengths of 646 nm and 662 nm, respectively. This compound is designed for use in live cell imaging applications, enabling visualization of cellular processes in real time. CY5-N3 can be utilized effectively in Click chemistry reactions for conjugating with various biomolecules, facilitating enhanced imaging strategies in biological research. -
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. -
EIF2α Activator
HR-19011 is an eIF2α phosphorylation activator that specifically targets the heme-regulated inhibitor HRI (EIF2AK1). It demonstrates significant growth inhibitory activity against K562 leukemia cells, with an IC50 value of 3.91 µM. By activating the integrated stress response through the HRI-eIF2α-ATF4 axis, HR-19011 effectively contributes to the suppression of hematologic malignancies. Its favorable safety profile in vivo further supports its use in research focused on leukemia and other blood-related cancers. -
DNA Alkylator
DGN549-L is a DNA alkylator that facilitates the alkylation of DNA, allowing for efficient conjugation to antibodies at lysine residues. This compound is particularly useful in the synthesis of antibody-drug conjugates (ADCs), enabling targeted delivery of therapeutic agents. Its application in bioconjugation research supports advancements in precision medicine and therapeutic development. -
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 Substrate
ATR kinase substrate peptide (ASELPASQPQPFSAKKK) functions as a specific substrate for ATR protein kinase, facilitating the detection of ATR kinase activity in biological research. This peptide is instrumental in studying cellular responses to DNA damage and the associated signaling pathways. It plays a critical role in validating ATR kinase activity and exploring its implications in cancer biology and therapeutic development. -
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. -
PROTAC ATR Degrader
PROTAC ATR degrader-1 (compound ZS-7) is a potent degrader targeting ataxia telangiectasia and Rad3-related (ATR) proteins, demonstrated by a DC50 of 0.53 μM. This compound facilitates selective degradation of ATR, making it a valuable tool for cancer research and the study of DNA damage response pathways. Its application in cellular models aids in understanding the therapeutic potential of ATR inhibition in various malignancies. -
ATM Inhibitor
M3541 is a potent, ATP-competitive inhibitor of Ataxia Telangiectasia Mutated (ATM) kinase, exhibiting an IC50 of 0.25 nM. This compound demonstrates significant selectivity against other protein kinases. M3541 effectively hinders the repair of double-strand breaks (DSB) and displays notable antitumor activity, making it a valuable tool for cancer research and therapeutic studies targeting DNA damage response pathways. -
ATM/ATR
SKLB-197 is a selective inhibitor of ATR (ATM and Rad3-related protein) with an IC50 value of 0.013 μM, demonstrating minimal activity against a panel of 402 other protein kinases. This compound exhibits significant antitumor efficacy specifically in ATM-deficient tumors, showing potent activity in both in vitro and in vivo models. SKLB-197 serves as a valuable tool for investigating the roles of ATM and ATR in cancer biology and for the development of targeted therapies. -
ATR Inhibitor
ATR-IN-4 is a selective inhibitor of the ATR (Ataxia Telangiectasia Mutated and Rad3-related) kinase. This compound exhibits significant antiproliferative activity against human prostate cancer cells (DU145) and human lung cancer cells (NCI-H460), yielding IC50 values of 130.9 nM and 41.33 nM, respectively. ATR-IN-4 is valuable for research investigating DNA damage response pathways and potential therapeutic strategies in cancer treatment. -
Atm Inhibitor
ATM Inhibitor-10 is a selective ATM inhibitor characterized as a 3-quinoline carboxamide with an IC50 of 0.6 nM. This compound demonstrates significant anti-tumor activity in SW620 xenograft models and shows synergistic effects when combined with Top I inhibitors. It serves as a valuable tool for studies involving DNA damage response and cancer therapeutics. -
PROTAC ATR Degrader
Abd110 is a Lenalidomide-based PROTAC that targets and degrades ATR kinase. It selectively reduces levels of ATR and phospho-ATR while sparing related kinases such as ATM and DNA-PKcs. This compound is valuable for research applications focused on ATR-mediated pathways and innate cellular responses to DNA damage. -
ATM Kinase Activity Inducer
GJ071 oxalate is an ATM kinase activity inducer that targets ataxia telangiectasia mutated (ATM) kinase. It is specifically designed for use in A-T cells harboring homozygous TGA or TAG stop codons. This compound enhances ATM kinase activity, facilitating studies on DNA damage response mechanisms and therapeutic strategies for ataxia telangiectasia and related disorders. -
ATM Inhibitor
(S)-WSD0628 is a selective ATM inhibitor that effectively inhibits the phosphorylation of ATM in MCF-7 cells, with an IC50 of less than 100 nM. This compound demonstrates radiosensitizing properties, enhancing the efficacy of radiotherapy in cancer treatments. Additionally, (S)-WSD0628 is capable of crossing the blood-brain barrier, making it a valuable tool for research applications in neuro-oncology and other fields where central nervous system exposure is essential.
