Catalog No.
Product Name
Application
Product Information
Citations
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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. -
PARP14 PROTAC Degrader
RBN012811 is a selective PROTAC degrader that targets PARP14, facilitating its degradation through a ternary complex with cereblon by binding at the NAD+ site. With an IC50 of 10 nM, RBN012811 efficiently reduces endogenous PARP14 levels in various cell lines and primary human macrophages. This reduction is associated with decreased IL-10 production and IFN-β mRNA, alongside an increase in phosphorylated STAT1, thereby enhancing inflammatory signaling and inhibiting interferon-induced ADPr condensate formation. RBN012811 also influences viral replication dynamics, promoting HSV1 replication while diminishing VSV replication, making it valuable for research in cancer biology and viral infections. -
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. -
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. -
ATR PROTAC Degrader
PROTAC ATR degrader-2 is a selective degrader targeting the ATR protein. It effectively induces degradation of ATR in acute myeloid leukemia (AML) cell lines MV-4-11 and MOLM-13, demonstrating DC50 values of 22.9 nM and 34.5 nM, respectively. This compound has an IC50 of 29.6 nM against ATR, while exhibiting minimal activity against ATM and PI3K. PROTAC ATR degrader-2 promotes apoptosis, causes DNA damage, and upregulates p53 expression, thereby inhibiting cancer cell proliferation. This reagent is suitable for research applications focused on understanding mechanisms in acute myeloid leukemia. -
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. -
SIRT6 PROTAC Degrader
SZU-B6 is a SIRT6-protein-targeting chimeric degrader that achieves a DC50 of 45 nM and 154 nM in SK-HEP-1 and Huh-7 cell lines, respectively. It effectively inhibits the proliferation of SK-HEP-1 cells with an IC50 of 1.51 μM and suppresses colony formation in both SK-HEP-1 and Huh-7 cells. Additionally, SZU-B6 induces apoptosis and causes a cell cycle arrest in the G2/M phase in SK-HEP-1 cells, demonstrating notable antitumor efficacy in mouse models. This compound serves as a valuable tool for studying the functional roles of SIRT6 in cancer research. -
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-PK Inhibitor
IC 86621 is a potent inhibitor of DNA-dependent protein kinase (DNA-PK) with an IC50 of 120 nM, acting as a selective and reversible ATP-competitive inhibitor. This compound impedes DNA-PK mediated repair of DNA double-strand breaks (DSB), displaying an EC50 of 68 µM. IC 86621 enhances antitumor activity in the presence of DSBs without inducing cytotoxicity and provides protection against apoptosis in T cells from rheumatoid arthritis. Its applications extend to cancer research and the study of immune responses in autoimmune disorders. -
PARP10/PARP15 Inhibitor
PARP10/15-IN-2 is a potent dual inhibitor of PARP10 and PARP15, exhibiting IC50 values of 0.15 µM and 0.37 µM, respectively. This compound has demonstrated the ability to penetrate cellular membranes and effectively rescue cells from apoptosis. PARP10/15-IN-2 serves as a valuable tool for research into cell survival mechanisms and the modulation of PARP-related signaling pathways. -
HDAC/JAK/BRD4 Inhibitor
HDAC/JAK/BRD4-IN-1 is a potent inhibitor targeting histone deacetylases (HDAC), Janus kinases (JAK), and bromodomain-containing protein 4 (BRD4). This compound demonstrates significant anti-proliferative effects and promotes apoptosis in MDA-MB-231 breast cancer cells. Additionally, HDAC/JAK/BRD4-IN-1 exhibits promising anticancer activity in vivo, making it a valuable tool for research in cancer therapeutics and the study of epigenetic and signaling pathways. -
Topoisomerases Inhibitor
Pyrazoloacridine is a potent inhibitor of topoisomerases 1 and 2, functioning as an intercalating agent with notable anti-cancer activity. This compound demonstrates cytotoxicity in K562 myeloid leukemia cells, exhibiting an IC50 of 1.25 μM following a 24-hour treatment. Pyrazoloacridine is primarily utilized in cancer research to explore mechanisms of tumor cell proliferation and resistance. -
DNA Alkylator
(S)-Seco-Duocarmycin SA is a potent DNA alkylator that binds to DNA, leading to cytotoxic effects in tumor cells. This compound exhibits significant antitumor activity, with an IC50 of 10 pM, and induces a concentration-dependent increase in apoptotic cell death. Additionally, (S)-Seco-Duocarmycin SA is capable of causing substantial cell cycle arrest in the S and G2/M phases. Its mechanism of action makes it a valuable cytotoxic agent for antibody-drug conjugates in cancer research applications. -
PARP/PI3K Inhibitor
PARP/PI3K-IN-1 is a potent inhibitor of both PARP and PI3K, exhibiting pIC50 values of 8.22 for PARP-1, 8.44 for PARP-2, and varying activity against PI3K isoforms with values of 8.25 for PI3Kα, 6.54 for PI3Kβ, 8.13 for PI3Kδ, and 6.08 for PI3Kγ. This compound demonstrates significant anticancer activity and is suitable for research applications targeting a variety of oncological disorders. Its dual inhibition may provide insights into therapeutic strategies for cancer treatment. -
Sirtuin Inhibitor
Sirt1/2-IN-2 is a dual inhibitor targeting SIRT1 and SIRT2, exhibiting IC50 values of 1.8 μM and 2.4 μM, respectively. This compound effectively prevents the deacetylation of p53 while promoting acetylation of p53 and α-tubulin. Sirt1/2-IN-2 demonstrates pro-apoptotic properties and exhibits anti-proliferative effects on human leukemia cell lines, making it a valuable tool in cancer research and therapeutic studies targeting the sirtuin family. -
HDAC1-3 Inhibitor
HDAC-IN-53 is a selective inhibitor of histone deacetylases 1-3, demonstrating IC50 values of 47 nM, 125 nM, and 450 nM for HDAC1, HDAC2, and HDAC3, respectively. This compound exhibits minimal off-target effects, as it does not inhibit class II HDACs (IC50 > 10 μM). HDAC-IN-53 promotes caspase-dependent apoptosis and has been shown to inhibit the growth of human tumor xenografts in nude mice, as well as murine tumors in immune-competent mice bearing MC38 colon cancer. It serves as a valuable tool for studying cancer biology and potential therapeutic strategies targeting HDAC pathways. -
HDAC6 Inhibitor
QTX125 TFA is a potent and highly selective inhibitor of Histone Deacetylase 6 (HDAC6). This compound demonstrates exceptional selectivity for HDAC6 over other isoforms, making it a valuable tool for studying the role of HDAC6 in various biological processes. QTX125 TFA has shown promising antitumor effects, indicating its potential for use in cancer research and therapeutic applications targeting HDAC6-related pathways. -
HDAC Inhibitor
CRA-026440 hydrochloride is a potent, broad-spectrum histone deacetylase (HDAC) inhibitor, exhibiting Ki values against recombinant HDAC isoenzymes of 4 nM for HDAC1, 14 nM for HDAC2, 11 nM for HDAC3, 15 nM for HDAC6, 7 nM for HDAC8, and 20 nM for HDAC10. This compound demonstrates significant antitumor and antiangiogenic activities, making it relevant for studies in cancer biology. Additionally, CRA-026440 hydrochloride possesses an alkyne functional group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), facilitating its use in click chemistry applications for bioconjugation studies. -
PARP1 Inhibitor
KU-0058948 is a potent inhibitor of PARP1, exhibiting an IC50 value of 3.4 nM. This compound induces cell cycle arrest and apoptosis in primary myeloid leukemic cells as well as established myeloid leukemic cell lines. It is suitable for research applications focused on cancer biology and the exploration of PARP1's role in cellular processes. -
DNA Synthesis Inhibitor
Fludarabine triphosphate is a potent inhibitor of DNA synthesis, primarily targeting DNA primase. This nucleotide analog effectively inhibits DNA primase with an IC50 value of 2.3 μM and a Ki of 6.1 μM, obstructing the formation of primer RNA and ultimately disrupting DNA synthesis. Additionally, Fludarabine triphosphate also inhibits ribonucleotide reductase and DNA polymerase, leading to cellular apoptosis. It is utilized in various research applications to study mechanisms of DNA replication and the effects of nucleotide analogs on cell viability. -
Topoisomerase II Inhibitor
Etoposide phosphate disodium is a selective inhibitor of topoisomerase II, acting as a potent anti-cancer agent. This phosphate ester prodrug of etoposide effectively prevents the re-ligation of DNA strands, leading to cell cycle arrest, apoptosis, and autophagy in cancer cells. It is utilized in cancer research for its ability to induce programmed cell death and its therapeutic implications in chemotherapy. -
HDAC1/2 and CDK2 Inhibitor
HDAC1/2 and CDK2-IN-1 is a dual inhibitor targeting HDAC1, HDAC2, and CDK2, with IC50 values of 70.7 μM, 23.1 μM, and 0.80 μM, respectively. This compound effectively disrupts the cell cycle and promotes apoptosis in tumor cells, demonstrating significant in vivo antitumor activity. It is suitable for research applications focused on cancer biology and therapeutic interventions targeting histone deacetylases and cyclin-dependent kinases. -
HDAC/MBLAC2 Inhibitor
Pracinostat dihydrochloride is a potent inhibitor of histone deacetylases (HDACs), demonstrating IC50 values in the range of 40-140 nM, making it a valuable tool in cancer research. In addition, it effectively inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2) with an EC50 below 10 nM, highlighting its potential use in studies related to epigenetic regulation and resistance mechanisms in cancer therapies. -
Topoisomerase II Inhibitor
Daunorubicin citrate is a potent inhibitor of topoisomerase II, exerting significant anti-tumor activity. This cytotoxic agent interferes with DNA and RNA synthesis, leading to reduced cancer cell viability and the induction of apoptosis and necrosis. As an anthracycline antibiotic, daunorubicin citrate is utilized in research related to various cancers, including leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, and Wilms' tumor, as well as studies on infectious diseases. -
Sirtuin Inhibitor
Sirt1/2-IN-3 is a dual inhibitor of the sirtuin family, specifically targeting SIRT1 and SIRT2 with IC50 values of 1.4 μM and 2.0 μM, respectively. This compound effectively prevents the deacetylation of p53, leading to increased acetylation of both p53 and α-tubulin. Sirt1/2-IN-3 has been demonstrated to induce apoptosis and exhibit anti-proliferative effects on human leukemia cell lines, making it a valuable tool for cancer research and the study of cellular aging mechanisms. -
SIRT Inhibitor
SIRT-IN-7 is a selective inhibitor targeting the SIRT family of proteins, specifically SIRT1, SIRT2, and SIRT3. This compound enhances the acetylation and activation of the tumor suppressor protein p53, leading to the inhibition of proliferation and the induction of apoptosis and autophagy in breast cancer cells. SIRT-IN-7 demonstrates significant anti-tumor activity, making it a valuable tool for research in cancer biology and therapeutic development. -
PARP-2 Inhibitor
PARP-2-IN-3 is a potent inhibitor of PARP-2, exhibiting an IC50 of 0.07 μM. This compound effectively induces apoptosis and necrosis in cancer cells, making it a valuable tool for cancer research. Additionally, PARP-2-IN-3 demonstrates favorable pharmacokinetic properties and oral bioavailability, supporting its potential use in therapeutic applications targeting PARP-2 related pathways. -
HDAC Inhibitor
HDAC-IN-73 is a potent histone deacetylase (HDAC) inhibitor targeting HDAC1 and HDAC6, with IC50 values of 0.17 µM and 0.49 µM, respectively. Its enhanced activity against HDAC6 demonstrates a nine-fold greater potency compared to PsA, making it a valuable compound in the field of cancer research. HDAC-IN-73 exhibits significant antiproliferative effects, induces apoptosis, and triggers G2/M cell cycle arrest, positioning it as a promising candidate for investigating therapies in colon cancer and other malignancies. -
HDAC Inhibitor
HDAC-IN-96 is a selective inhibitor of histone deacetylases 1 and 2 (HDAC1/2), exhibiting IC50 values of 457.1 nM and 433.7 nM, respectively. This compound demonstrates significant cytotoxicity against various hematological tumor cell lines, including RS4;11, K562, RPMI-8226, and U266, with IC50 values between 2.11 and 5.35 μM. HDAC-IN-96 has been shown to induce apoptosis and cause S phase arrest in cancer cells, making it a valuable tool for research in hematological malignancies such as acute lymphoblastic leukemia. -
Aurora A/Aurora B/HDAC1/HDAC2 Inhibitor
Aurora kinase/HDAC-IN-1 is a potent dual inhibitor targeting Aurora A, Aurora B, HDAC1, and HDAC2. This compound promotes histone H3 acetylation, inhibits Aurora A phosphorylation and downstream signaling, and induces apoptosis through G2/M cell-cycle arrest. It demonstrates significant antiproliferative activity in colorectal cancer cells, with an IC50 of 30.2 nM in HCT-116 cells, and effectively suppresses tumor growth in HCT-116 colorectal cancer xenograft mouse models. This reagent is valuable for research in cancer biology and therapeutic application development.
