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Catalog No.
Product Name
Application
Product Information
Citations
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PARP7 Inhibitor
PARP7-IN-15 is a selective inhibitor of PARP7, exhibiting an IC50 of 0.56 nM. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. Its potency in inhibiting PARP7 can facilitate studies focused on DNA repair mechanisms and cancer cell proliferation. -
PARP Inhibitor
Nesuparib is a potent inhibitor of PARP 1 and 2, as well as Tankyrase 1 and 2, with IC50 values of 5 nM, 1 nM, and 2 nM, respectively. This orally bioavailable compound demonstrates significant antitumor activity, making it a valuable tool for researching advanced solid tumors. Its selective inhibition of critical DNA repair pathways highlights its potential in cancer therapy and provides important insights into targeted treatment strategies. -
PARP1/2/6 Inhibitor
AZ9482 is a potent inhibitor of PARP1, PARP2, and PARP6, exhibiting IC50 values of 1 nM for both PARP1 and PARP2, and 640 nM for PARP6. This compound effectively disrupts the DNA repair pathway in cancer cells, making it a valuable tool for studying cellular response to DNA damage. AZ9482 is appropriate for applications in cancer research, particularly in the context of synthetic lethality and therapeutic resistance. -
PARP-1/2/7 Inhibitor
PARP7-IN-16 is a selective and orally bioavailable inhibitor of PARP-1, PARP-2, and PARP-7, exhibiting IC50 values of 0.94 nM, 0.87 nM, and 0.21 nM, respectively. This compound serves as a valuable research tool for investigating the roles of PARP enzymes in cellular processes and their implications in oncogenesis. It is particularly relevant for studies focusing on breast cancer and prostate cancer, providing insights into therapeutic strategies that target DNA repair mechanisms. -
PARP Inhibitor
K-756 is a selective tankyrase (TNKS) inhibitor that effectively inhibits the ADP-ribosylation activity of TNKS1 and TNKS2, exhibiting IC50 values of 31 nM and 36 nM, respectively. This compound plays a significant role in the study of various cancer-related pathways and cellular processes influenced by tankyrase activity. K-756 is applicable in research focused on DNA repair mechanisms, cellular signaling, and the modulation of Wnt signaling pathways. -
PARP10/15 Inhibitor
PARP10/15-IN-1 is a selective inhibitor targeting both PARP10 and PARP15, exhibiting IC50 values of 160 nM and 370 nM, respectively. This compound serves as a valuable tool for cancer research, enabling the investigation of PARP10 and PARP15's roles in tumorigenesis and therapeutic resistance. Its dual inhibitory properties facilitate studies aimed at understanding the molecular mechanisms of cancer progression and the potential for targeted therapies. -
PARP10 Inhibitor
PARP10-IN-3 is a selective inhibitor of the mono-ADP-ribosyltransferase PARP10, exhibiting an IC50 of 480 nM against human PARP10. Additionally, it demonstrates significant inhibitory activity towards PARP2 and PARP15 with IC50 values of 1.7 μM. This compound serves as a valuable tool in research applications targeting the role of PARP enzymes in cellular processes and their implications in various diseases, including cancer. -
PARP1/2 Inhibitor
Simmiparib is a potent and orally active inhibitor of PARP1 and PARP2, demonstrating IC50 values of 1.75 nM and 0.22 nM, respectively. This compound effectively induces the accumulation of DNA double-strand breaks and triggers G2/M phase arrest in homologous recombination repair-deficient cells, leading to apoptosis. Simmiparib exhibits significant antitumor activity in various cancer models, including xenografts in nude mice, making it a valuable tool for cancer research and therapeutic development. -
PARP-1 Inhibitor
PARP1-IN-5 dihydrochloride is a potent and selective inhibitor of PARP-1, with an IC50 of 14.7 nM. This compound exhibits low toxicity and is suitable for oral administration. PARP1-IN-5 dihydrochloride is primarily utilized in cancer research to investigate the role of PARP-1 in tumorigenesis and therapy resistance. -
PARP7 Inhibitor
PARP7-IN-17 is a potent PARP7 inhibitor with an IC50 of 4.5 nM, demonstrating effective oral bioavailability. This compound exhibits significant antitumor activity, making it a valuable tool for research into cancer therapeutics and the biological role of PARP7 in tumorigenesis. Its selective inhibition of PARP7 may aid in the development of targeted cancer treatments. -
PARP7 Inhibitor
PARP7-IN-22 is a potent PARP7 inhibitor with an IC50 of 0.6 nM. This compound is orally active and enhances type I interferon signaling in vitro, facilitating T cell infiltration into tumor tissues and significantly inhibiting tumor growth. PARP7-IN-22 is of particular interest for research in cancer immunotherapy, providing valuable insights into therapeutic strategies that target immune responses in oncology. -
PARP Inhibitor
PARP7-IN-16 free base is a selective, orally active inhibitor of PARP-1, PARP-2, and PARP-7, exhibiting IC50 values of 0.94 nM, 0.87 nM, and 0.21 nM, respectively. This compound is valuable for investigating the role of PARP enzymes in DNA repair mechanisms and is particularly relevant in studies focused on breast and prostate cancer. Researchers can utilize PARP7-IN-16 free base to explore therapeutic strategies targeting these types of malignancies. -
PARP1 Inhibitor
PARP1-IN-11 is a selective inhibitor of the poly(ADP-ribose) polymerase 1 (PARP1) enzyme, demonstrating a potent inhibitory activity with an IC50 value of 0.082 µM. This compound exhibits complete inhibition of PARP2 and significantly inhibits the activity of PARP3, as well as tankyrases TNKS1 and TNKS2. PARP1-IN-11 is valuable for research applications focused on DNA repair mechanisms, cancer therapeutics, and the study of cellular responses to genotoxic stress. -
PARP1 Inhibitor
PARP1-IN-33 is a potent inhibitor of PARP1, exhibiting an IC50 of 0.41 nM. This compound demonstrates significant cytoprotective effects on retinal cells, with an EC50 of 0.02 nM in inhibiting MTS activity in H2O2-induced human retinal pigment epithelial cells. PARP1-IN-33 is valuable for research applications aimed at understanding retinal oxidative stress and developing therapeutic strategies for retinal diseases. -
Poly(ADP-ribose) Polymerase Inhibitor
PD128763 is a selective inhibitor of poly(ADP-ribose) polymerase (PARP). This compound enhances the cytotoxic effects of Streptozotocin, making it a valuable tool for studying cellular mechanisms in leukemia. PD128763 is suitable for research applications focused on PARP-related pathways and therapeutic strategies in cancer treatment. -
PARP-1 Inhibitor
A-620223 is a potent inhibitor of PARP-1, exhibiting a Ki of 8 nM and an EC50 of 3 nM in whole cell assays. This compound demonstrates significant in vivo efficacy in murine models, particularly in the B16F10 melanoma model when used in combination with Temozolomide and in the MX-1 breast xenograft model with Cisplatin. A-620223 is suitable for research applications focusing on melanoma and breast cancer therapy. -
PARP Inhibitor
Saruparib is a potent and selective PARP inhibitor, primarily targeting PARP1 with an IC50 value of 3 nM and PARP2 with an IC50 of 1400 nM. This orally active compound demonstrates significant anti-proliferative effects and is particularly effective in inhibiting the growth of cells exhibiting deficiencies in DNA repair mechanisms. Saruparib is commonly utilized in research focused on cancer treatment strategies, particularly in the context of homologous recombination repair-deficient tumors. -
PARP1 Inhibitor
Fluzoparib is a highly potent oral inhibitor of PARP1, demonstrating an IC50 of 1.46 ± 0.72 nM in cell-free enzymatic assays. This compound selectively targets homologous recombination repair (HR)-deficient cells while sensitizing both HR-deficient and HR-proficient cells to cytotoxic agents. With favorable pharmacokinetic properties in vivo, Fluzoparib is an important reagent for studying BRCA1/2-mutant relapsed ovarian cancer and related therapeutic strategies. -
PARP14 Inhibitor
RBN012759 is a potent and selective inhibitor of PARP14, exhibiting an IC50 of less than 3 nM. It demonstrates 300-fold selectivity for monoPARPs and 1000-fold selectivity for polyPARPs. RBN012759 has been shown to diminish pro-tumor macrophage activity and trigger inflammatory responses in tumor explants, making it a valuable tool for research in cancer biology and immune modulation. -
PARP Inhibitor
Basroparib is a selective inhibitor of tankyrase (TNKS1/TNKS2) with IC50 values of 29.94 nM and 3.68 nM, respectively, and exhibits limited activity against PARP1 (IC50 > 10 μM). This compound stabilizes AXIN1/2 proteins and effectively disrupts the Wnt/β-catenin signaling pathway, leading to inhibition of tumor cell proliferation and induction of apoptosis. Basroparib is particularly relevant for research in colorectal cancer (CRC) models bearing KRAS mutations, such as G12V/G12D, and demonstrates potential to overcome resistance to MEK inhibitors, providing synergistic antitumor effects. -
PARP Inhibitor
Benzamide is a potent inhibitor of poly(ADP-ribose) polymerase (PARP), demonstrating significant neuroprotective effects. It has been shown to protect against neurotoxicity induced by glutamate and methamphetamine in vitro. In vivo studies indicate that Benzamide can mitigate methamphetamine-induced dopamine depletions in mice without acute effects on striatal dopamine metabolism or body temperature regulation. Its dual role in neuroprotection and PARP inhibition makes it a valuable tool in neuropharmacology research. -
PARP10 Inhibitor
OUL232 is a potent inhibitor of poly(ADP-ribose) polymerase 10 (PARP10) and other mono-ADP-ribosyl transferases including PARP7, PARP11, PARP12, PARP14, and PARP15. With an IC50 of 7.8 nM, OUL232 represents the most effective PARP10 inhibitor characterized to date and is the first reported inhibitor targeting PARP12. This compound is valuable for studying the biological roles of PARP10 and PARP12 in cellular processes and may facilitate research into therapeutic strategies involving these targets. -
HDAC6 Inhibitor
HDAC6-IN-53 is a potent inhibitor of histone deacetylase 6 (HDAC6) with an IC50 of 19.65 nM. This compound effectively suppresses collagen expression induced by TGF-β1, demonstrating therapeutic potential in the treatment of idiopathic pulmonary fibrosis (IPF). Additionally, HDAC6-IN-53 has shown efficacy in a mouse model of pulmonary fibrosis induced by Bleomycin. It is a valuable reagent for studying the molecular mechanisms underlying idiopathic pulmonary fibrosis and related pulmonary diseases. -
HDAC PROTAC Inhibitor
JPS016 is a class I histone deacetylase (HDAC) PROTAC inhibitor that targets HDAC1, HDAC2, and HDAC3 for ubiquitination and proteasomal degradation via VHL E3 ligase recruitment. This compound demonstrates significant anticancer activity by reducing the viability of colon cancer cells and inducing apoptosis. Additionally, JPS016 activates the PINK1/Parkin-mediated mitochondrial autophagy pathway, enhancing cardiomyocyte viability, alleviating mitochondrial damage, and decreasing mitochondrial ROS production. It is valuable for research into colon cancer and sepsis-related cardiac dysfunction. -
HDAC Inhibitor
STR-V-53 is a histone deacetylase (HDAC) inhibitor with a low nanomolar IC50. By inhibiting HDAC activity, STR-V-53 increases histone acetylation, leading to altered gene expression. This compound exhibits significant anti-tumor properties, inhibiting proliferation and promoting apoptosis in cancer cells. It serves as a valuable research tool for studying epigenetic regulation and potential therapeutic strategies in oncology. -
HDAC Inhibitor
HDAC-IN-56 is a potent, orally active inhibitor of class I histone deacetylases (HDACs), demonstrating IC50 values of 56.0 ± 6.0 nM for HDAC1, 90.0 ± 5.9 nM for HDAC2, and 422.2 ± 105.1 nM for HDAC3, with minimal activity against HDAC4-11. This compound effectively increases intracellular levels of acetylated histone H3 and P21, leading to G1 cell cycle arrest and apoptosis in tumor cells. HDAC-IN-56 is utilized in cancer research to investigate its therapeutic potential and mechanisms involving HDAC inhibition. -
A2A Receptor/HDAC Inhibitor
IHCH-3064 is a dual-target compound that inhibits the Adenosine A2A Receptor and histone deacetylase (HDAC). It demonstrates potent binding affinity for the A2A receptor (Ki = 2.2 nM) and selectively inhibits HDAC1 with an IC50 of 80.2 nM. This compound exhibits significant antiproliferative activity against various tumor cell lines in vitro, making it a valuable tool for tumor immunotherapy research applications. -
HDAC6 Inhibitor
HDAC6-IN-50 is a potent HDAC6 inhibitor with an IC50 of 35 nM. This compound is valuable in the investigation of neurodegenerative disorders, particularly in the context of Parkinson's disease (PD) and Alzheimer's disease (AD). HDAC6-IN-50 facilitates research on the epigenetic regulation involved in these diseases, contributing to the understanding of their pathogenesis and potential therapeutic strategies. -
HDAC6 Inhibitor
ITF5924 is a potent and highly selective inhibitor of HDAC6, exhibiting an IC50 of 7.7 nM. This compound demonstrates over 104-fold selectivity for HDAC6 compared to other HDAC subtypes. The unique difluoromethyl-1,3,4-oxadiazole (DFMO) moiety allows ITF5924 to function as a slow-binding substrate analog, undergoing an enzyme-catalyzed ring-opening reaction that forms a stable and long-lasting enzyme-inhibitor complex. ITF5924 is valuable for studies exploring the role of HDAC6 in various cellular processes and disease states, making it an essential tool for epigenetic research. -
HDAC1 Inhibitor
HDAC1-IN-8 is a selective inhibitor of histone deacetylase 1 (HDAC1) with an IC50 of 11.94 µM. It exhibits significant antiproliferative activity and has been shown to induce cell cycle arrest at both G1 and G2/M phases. Additionally, HDAC1-IN-8 promotes autophagy and demonstrates anticancer potential, making it a valuable tool for research in lung cancer and other malignancies. -
HDAC3 Inhibitor
HDAC3-IN-1 is a potent and selective inhibitor of histone deacetylase 3 (HDAC3), exhibiting an IC50 value of 5.96 nM. This compound effectively modulates gene expression through the inhibition of histone deacetylation, making it a valuable tool for studying epigenetic regulation and cellular signaling pathways. HDAC3-IN-1 is applicable in research areas such as cancer biology, neurodegenerative disorders, and potential therapeutic development for various diseases involving epigenetic dysregulation. -
HDAC Inhibitor
NT376 is a potent and selective inhibitor of class-IIa Histone deacetylases (HDAC), demonstrating an IC50 value of 32 nM in HT-29 cells. It exhibits significant biological activity that supports its role in cancer research and the investigation of central nervous system disorders, including Alzheimer's and Huntington's diseases. NT376 serves as a valuable tool for studying the epigenetic regulation of gene expression and potential therapeutic pathways in these conditions. -
HDAC6 Inhibitor
HDAC6-IN-66 is a potent and selective inhibitor of histone deacetylase 6 (HDAC6), exhibiting an IC50 of 1.8 nM. This compound effectively induces acetylation of α-tubulin while preferentially impacting histone H3. HDAC6-IN-66 serves as a valuable tool for cancer research, facilitating studies on the role of HDAC6 in oncogenic processes and potential therapeutic interventions. -
HDAC6 Inhibitor
HDAC6-IN-9 is a potent and selective inhibitor of HDAC6, demonstrating IC50 values of 4.2 nM for HDAC6 and significantly lower values for HDAC1, HDAC3, HDAC8, and HDAC10. This compound exhibits notable anti-proliferative activity, making it a valuable tool for research in cancer biology and therapeutic development. Its selectivity enables investigations into the specific roles of HDAC6 in cellular processes and disease states. -
HDAC Inhibitor
HDAC-IN-45 is a small molecule inhibitor targeting histone deacetylases (HDACs), specifically demonstrating significant inhibition of HDAC1, HDAC2, and HDAC3 with IC50 values of 0.108 µM, 0.585 µM, and 0.563 µM, respectively. This compound exhibits pronounced anticancer activity and forms a hydrogen bond with the Y303 residue, which may contribute to its mechanism of action. HDAC-IN-45 is valuable for cancer research, particularly in studies focused on epigenetic regulation and therapeutic interventions in tumorigenesis. -
HDAC Inhibitor
4-Iodo-SAHA is an orally active inhibitor of class I and class II histone deacetylases (HDACs), demonstrating EC50 values of 1.1, 0.95, 0.12, 0.24, 0.85, and 1.3 μM across the Skbr3, HT29, U937, JA16, and HL60 cell lines, respectively. This compound exhibits significant potential for tumor growth inhibition and is valuable for cancer research applications, including the investigation of epigenetic regulation and therapeutic interventions in HDAC-related malignancies. -
HDAC Inhibitor
HDAC-IN-26 is a highly selective inhibitor of class I histone deacetylases (HDACs), exhibiting an EC50 value of 4.7 nM. This compound plays a crucial role in modulating gene expression by preventing the deacetylation of histones, thereby facilitating an open chromatin state. HDAC-IN-26 is valuable for research applications involving cancer biology, neurodegenerative diseases, and epigenetic regulation. -
BChE/HDAC6 Inhibitor
BChE/HDAC6-IN-1 is a selective dual inhibitor targeting both butyrylcholinesterase (BChE) and histone deacetylase 6 (HDAC6), with IC50 values of 4 nM and 8.9 nM, respectively. This compound demonstrates significant potential in ameliorating cognitive impairment in an Aβ1–42-induced mouse model, making it a valuable tool in Alzheimer's disease research. Its ability to modulate both cholinergic and epigenetic pathways positions BChE/HDAC6-IN-1 as a promising candidate for studies focused on neurodegenerative disorders. -
HDAC2 Inhibitor
HDAC2-IN-1 is a competitive inhibitor of histone deacetylase 2 (HDAC2), demonstrating an IC50 of 0.5 μM. This orally active compound exhibits additional inhibitory effects on HDAC1 and HDAC8, with IC50 values of 1.61 μM and 0.98 μM, respectively. Its ability to penetrate the blood-brain barrier positions HDAC2-IN-1 as a valuable tool for investigating the role of HDACs in neurodegenerative diseases and other neurological disorders. -
HDAC6 Inhibitor
HDAC6-IN-52 is a potent inhibitor of histone deacetylase 6 (HDAC6), demonstrating a complete inhibition at 10 μM. This compound is significant in the context of central nervous system diseases, particularly neurodegenerative disorders such as Alzheimer’s disease and progressive supranuclear palsy. HDAC6-IN-52 is valuable for research investigating the therapeutic potential of HDAC6 modulation in neurological conditions. -
HDAC Inhibitor
HDAC-IN-20 is a potent inhibitor of histone deacetylases (HDACs), offering oral bioavailability. It exhibits significant anti-cancer activity, making it a valuable tool for investigating tumor biology and exploring epigenetic regulation in cancer research. This compound facilitates the study of HDAC's role in oncogenesis and therapeutic responses, thereby contributing to the understanding of cancer treatment strategies. -
HDAC6 Inhibitor
MPT0G413 is a selective HDAC6 inhibitor with an IC50 of 3.92 nM, demonstrating potent oral bioavailability and the ability to penetrate the blood-brain barrier. This compound effectively reduces tau protein phosphorylation and aggregation, thereby addressing cognitive deficits related to memory and learning. MPT0G413 is suitable for research applications in neurological disorders, including Alzheimer's disease. -
HDAC6 Inhibitor
NR160 is a selective inhibitor of histone deacetylase 6 (HDAC6), exhibiting an IC50 value of 30 nM. This compound demonstrates low cytotoxicity in leukemia cell lines and enhances the induction of apoptosis when used in conjunction with proteasome inhibitor Bortezomib, as well as chemotherapeutic agents Epirubicin and Daunorubicin. NR160 serves as a valuable tool for researchers investigating the therapeutic potential of HDAC6 inhibition in cancer treatment. -
PHD2/HDACs Inhibitor
PHD2/HDACs-IN-1 is a dual inhibitor targeting both PHD2 and various HDACs, demonstrating potent inhibitory activity with IC50 values of 1.15 μM for PHD2, 19.75 μM for HDAC1, 26.60 μM for HDAC2, and 15.98 μM for HDAC6. This compound showcases low toxicity and exhibits renoprotective effects, making it suitable for research related to cisplatin-induced acute kidney injury (AKI). Its ability to modulate epigenetic regulation and hypoxic signaling pathways positions it as a valuable tool in exploring the underlying mechanisms of renal stress responses. -
HDAC Inhibitor
YF479 is a potent inhibitor of histone deacetylases (HDACs), demonstrating significant biological activity in the modulation of gene expression. This compound impairs cell viability and suppresses both colony formation and tumor cell motility. Additionally, YF479 effectively inhibits breast tumor growth and metastasis, making it a valuable tool for research in breast cancer clinical trials. -
CYP17A1/HDAC6 Inhibitor
CYP17A1/HDAC6-IN-1 is a dual inhibitor targeting both CYP17A1 and HDAC6, exhibiting IC50 values of 0.284 μM and 0.6015 μM, respectively. This compound demonstrates significant anti-tumor activity, making it a valuable tool for research in cancer biology. Its ability to simultaneously inhibit these targets suggests potential applications in therapeutic strategies against malignancies driven by steroidogenesis and histone deacetylation. -
HDAC8 Inhibitor
HDAC8-IN-2 is a potent inhibitor of histone deacetylase 8 (HDAC8) with IC50 values of 0.27 μM for Schistosoma mansoni HDAC8 and 0.32 μM for human HDAC8. This compound demonstrates significant efficacy in killing schistosome larvae and markedly reduces the egg-laying capacity of adult worm pairs. These properties make HDAC8-IN-2 a valuable tool for research focused on schistosomiasis and histone deacetylation processes. -
HDAC3 Inhibitor
HDAC3-IN-4 is a selective inhibitor of histone deacetylase 3 (HDAC3) with an IC50 of 89 nM, demonstrating effective targeting of this enzyme. It promotes the degradation of PD-L1 through the modulation of cathepsin B (CTSB) activity in lysosomes, exhibiting a DC50 of 5.7 μM. HDAC3-IN-4 shows high selectivity for HDAC3 compared to other HDAC isoforms, including HDAC1, HDAC6, HDAC7, and HDAC8, making it a valuable tool for studying epigenetic regulation and potential immunotherapeutic approaches. -
HDAC Inhibitor
FITC-SAHA is a fluorescein-conjugated derivative of SAHA, serving as a potent inhibitor of histone deacetylases (HDACs). This compound effectively modulates histone acetylation, influencing gene expression and cellular processes. FITC-SAHA is primarily utilized in cancer research and studies related to Alzheimer's disease, facilitating the investigation of HDAC's role in these conditions. Its fluorescent labeling aids in the visualization and analysis of cellular and molecular interactions. -
PfHDAC1 Inhibitor
HDAC1-IN-4 is a potent inhibitor of Plasmodium falciparum histone deacetylase 1 (PfHDAC1), demonstrating significant antimalarial activity with an IC50 of less than 5 nM. This compound exhibits a favorable safety profile with reduced cytotoxicity. HDAC1-IN-4 serves as a valuable tool for investigating the role of histone deacetylases in malaria research and may provide insights for novel therapeutic strategies against Plasmodium falciparum infections.
