DNA Damage

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  1. RAD51 inhibitor

    Bractoppin is a potent and selective inhibitor of phosphopeptide recognition by the BRCA1 tBRCT domain.
  2. HDAC1 and HDAC3 inhibitor

    Suberoyl bis-hydroxamic acid (Suberohydroxamic acid; SBHA) is a competitive and cell-permeable HDAC1 and HDAC3 inhibitor with ID50 values of 0.25 μM and 0.30 μM, respectively.
  3. fluorescent probe

    DAPI Dihydrochloride is a cell-permeable fluorescent probe used to stain DNA and chromosomes, with a preference for adenine and thymine rich DNA.
  4. broad-spectrum seed treatment nematicide

    Tioxazafen is a disubstituted oxadiazole and a broad-spectrum seed treatment nematicide. Tioxazafen is designed to provide consistent broad-spectrum control of nematodes in corn, soy, and cotton.
  5. EG1

    Pax2 inhibitor

    EG1 is a specific Paired box 2 (Pax2) inhibitor that targets the DNA binding domain and inhibits embryonic kidney development.
  6. SIRT1/SIRT3 inhibitor

    4'-bromo-Resveratrol is a potent inhibitor of the deacetylases sirtuin 1 (SIRT1) and 3 (SIRT3).

  7. eIF4A Inhibitor

    Zotatifin is a highly selective inhibitor of eIF4A, targeting the assembly of the eIF4F initiation complex. With an IC50 of 2 nM, it promotes eIF4A binding to specific mRNA recognition motifs in the 5’-UTRs. Zotatifin exhibits significant antiviral properties, effectively reducing the infectivity of SARS-CoV-2 by inhibiting the biogenesis of its NP protein (IC90 = 37 nM) and also induces apoptosis in cancer cells. This compound is valuable for studies related to viral infections and translational control mechanisms.
  8. Fluorometric HDAC Substrate

    Boc-Lys(Ac)-AMC is a cell-permeable fluorometric substrate for histone deacetylases (HDACs). When cleaved by HDAC enzymes, it releases a fluorescent signal with excitation and emission maxima at 355 nm and 460 nm, respectively. This compound is valuable for studying HDAC activity in various biological contexts and can be utilized in high-throughput screening assays to evaluate enzyme inhibitors.
  9. PARP1 Degrader

    iRucaparib-AP6 is a potent PROTAC compound that selectively targets PARP1 for degradation. This non-trapping degrader inhibits both the catalytic activity and scaffolding functions of PARP1, effectively disrupting its role in DNA repair pathways. iRucaparib-AP6 is useful in studying the biology of PARP1 and its implications in cancer research, particularly in understanding resistance mechanisms to PARP inhibitors.
  10. VUBI1 Analogue

    VUBI1 analogue-1 is an analogue of VUBI1, functioning as a selective activator of the SOS1 pathway with a Kd of 44 nM. This compound is valuable for studying SOS1 activation mechanisms and provides a basis for the synthesis of (4S)-PROTAC SOS1 degrader-1. Its applications include investigations into targeted degradation and modulation of cellular pathways involving SOS1, offering insights into cellular signaling and potential therapeutic strategies.
  11. PROTAC PARP1 Degrader

    PROTAC PARP1 Degrader functions as a targeted protein degradation agent that specifically targets PARP1 through the MDM2 E3 ligase. This compound effectively induces PARP1 cleavage and promotes apoptosis in cancer cells, making it valuable for research in cancer therapies. The structure includes the MDM2 ligand, the PARP1 ligand, and a PEG-based linker, facilitating efficient delivery and degradation of the target protein.
  12. RNA RIBOTAC Degrader

    Dovitinib-RIBOTAC TFA is a targeted RNA RIBOTAC degrader that specifically binds to and degrades pre-miR-21. This compound demonstrates significant anti-tumor activity and effectively inhibits breast cancer metastasis. It serves as a valuable tool for research involving RNA-targeted degradation and its implications in cancer biology.
  13. SIRT2 Inhibitor

    SIRT2-IN-8 is a selective inhibitor of SIRT2 (Sirtuin 2), a member of the sirtuin family of proteins implicated in various cellular processes. This compound exhibits strong inhibition of SIRT2 activity, making it a valuable tool for investigating the role of SIRT2 in neurodegenerative diseases, particularly Huntington's and Parkinson's diseases. Its use in research can contribute to a better understanding of the molecular mechanisms underlying these conditions and aid in the development of therapeutic strategies.
  14. HDAC Inhibitor

    HC-Toxin is a potent histone deacetylase (HDAC) inhibitor with an IC50 of 30 nM. This cyclic tetrapeptide effectively induces apoptosis in tumor cells, demonstrating significant anticancer activity. Its mechanism of action makes it valuable for research in cancer therapy and the modulation of gene expression.
  15. HIV Reverse Transcriptase Inhibitor

    β-Rubromycin is a selective inhibitor of HIV-1 reverse transcriptase, exhibiting a Ki of 0.27 μM. Additionally, it demonstrates potent telomerase inhibition with an IC50 of 3 μM. β-Rubromycin effectively inhibits the proliferation of K-562 and HeLa cell lines, showing IC50 values of 19.5 µM and 22.7 µM, respectively, making it a valuable tool for research in HIV and telomerase-related studies.
  16. DNA Stain

    7-Aminoactinomycin D (7-AAD) is a cell-impermeant fluorescent DNA stain that primarily targets and binds to GC-rich regions of DNA. This compound is often utilized in flow cytometry and fluorescence microscopy to assess cell viability and apoptosis. Additionally, 7-AAD exhibits antibacterial properties, expanding its utility in various biological research applications.
  17. SIRT Inhibitor

    Nicotinamide is a form of vitamin B3 or niacin. Nicotinamide Hydrochloride inhibits SIRT2 activity (IC50: 2 μM). Nicotinamide also inhibits SIRT1. Nicotinamide increases cellular NAD+, ATP, ROS levels. Nicotinamide inhibits tumor growth and improves survival. Nicotinamide also has anti-HBV activity.
  18. Alkaloid

    Berberine (Natural Yellow 18) is an alkaloid isolated from the Chinese herbal medicine Huanglian, as an antibiotic. Berberine (Natural Yellow 18) induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Berberine (Natural Yellow 18) has antineoplastic properties. 

  19. Pre-mRNA Splicing Inhibitor

    Herboxidiene (GEX1A) is a potent phytotoxic polyketide from Streptomyces sp. A7847 with a diverse range of activities, including herbicidal, anti-cholesterol, anti-tumor effects. Herboxidiene inhibits the pre-mRNA splicing process by binding to spliceosome-associated protein (SAP) 155, a subunit of SF3b, in the splicesome.
  20. Cyanotoxin

    Cylindrospermopsin, a cyanotoxin, is a polycyclic uracil derivative containing guanidine and sulfate groups, which can inhibit protein synthesis and covalently modify DNA or RNA. Cylindrospermopsin induces hepatocellular hypertrophy, renal cellular hypertrophy, intracellular reactive oxygen species (ROS), DNA strand breaks, mitochondrial hyperpolarisation, ultrastructural damage, and altered gene expression in liver, kidney, and intestinal cells. Cylindrospermopsin can be used in research including hepatocellular carcinoma and water quality testing.
  21. Fluorochrome

    Propidium Iodide (PI) is a nuclear staining agent that stains DNA. Propidium Iodide is an analogue of ethidine bromide that emits red fluorescence upon embedding in double-stranded DNA. Propidium Iodide cannot pass through living cell membranes, but it can pass through damaged cell membranes to stain the nucleus. Propidium Iodide has a fluorescence wavelength of 493/617 nm and a wavelength of 536/635 nm after Mosaic with DNA. Propidium Iodide is commonly used in the detection of apoptosis (apoptosis) or necrosis (necrosis), and is often used in flow cytometry analysis.
  22. Antibiotic

    Erythromycin is a macrolide antibiotic that targets bacterial 50S ribosomal subunits, effectively inhibiting RNA-dependent protein synthesis by obstructing transpeptidation and translocation reactions. This compound demonstrates a broad spectrum of antimicrobial activity against various bacteria, making it valuable in microbiological research. Additionally, erythromycin has been shown to possess antitumor and neuroprotective properties, contributing to its usefulness in diverse areas of biomedical research.
  23. Skin Depigmenting Agent

    Monobenzone is a potent skin depigmenting agent that primarily targets the enzyme ribonucleotide reductase (RNR) by inhibiting its regulatory subunit, RRM2. It effectively induces depigmentation, making it a valuable compound in vitiligo research. Additionally, Monobenzone demonstrates significant anti-leukemic properties, inhibiting the proliferation and DNA synthesis of acute myeloid leukemia (AML) cells, and promoting cell cycle arrest and apoptosis. These dual functionalities position Monobenzone as a critical reagent in both dermatological and oncology studies.
  24. PDE Inhibitor

    Theophylline, a potent phosphodiesterase (PDE) inhibitor, primarily targets PDE3, leading to relaxation of airway smooth muscle and enhanced bronchodilation. This compound also functions as an adenosine receptor antagonist and exhibits anti-inflammatory properties by elevating IL-10 levels and inhibiting NF-κB translocation into the nucleus. Additionally, Theophylline has been shown to induce apoptosis in certain cell types. Its applications are particularly relevant in the research of asthma and chronic obstructive pulmonary disease (COPD).
  25. Topoisomerase IV Inhibitor

    Ciprofloxacin is a potent topoisomerase IV inhibitor that demonstrates significant antibacterial activity as a fluoroquinolone antibiotic. It induces both mitochondrial and nuclear DNA damage, leading to mitochondrial dysfunction and increased reactive oxygen species (ROS) production. Ciprofloxacin exhibits anti-proliferative properties and triggers apoptotic pathways, making it a valuable tool for research applications focused on bacterial infections, oxidative stress, and cancer biology.
  26. Anti-microbial Agent/Kir3.2 Blocker

    3,6-Diaminoacridine hemisulfate is an acridine compound that functions primarily as a broad-spectrum antimicrobial agent and a Kir3.2 potassium channel blocker. Its mechanism involves insertion into bacterial DNA, thereby disrupting replication and transcription, which ultimately leads to bacterial lysis. Additionally, this compound is utilized in research to investigate the neurological phenotype associated with Down syndrome. Due to its ability to penetrate the stratum corneum and accumulate in the cell nucleus, prolonged exposure warrants caution due to potential oncogenic effects.
  27. Topoisomerase I Inhibitor

    Irinotecan hydrochloride is a potent inhibitor of topoisomerase I, an enzyme crucial for DNA replication and transcription. This compound exhibits significant anti-tumor activity, primarily in the treatment of colorectal cancers. Its mechanism involves the stabilization of the enzyme-DNA complex, leading to apoptosis in cancer cells. Irinotecan hydrochloride is widely utilized in cancer research to elucidate cellular response mechanisms and to develop novel therapeutic strategies.
  28. DNA Dye

    DAPI (4',6-Diamidino-2-phenylindole) is a fluorescent DNA dye that selectively binds to the AT base pairs in the minor groove of double-stranded DNA, enhancing fluorescence intensity approximately 20-fold upon binding. This property makes DAPI suitable for applications in fluorescence microscopy, allowing for quantification of DNA based on fluorescence intensity. Additionally, DAPI's ability to penetrate intact cell membranes enables its use in staining both live and fixed cells. DAPI also acts as an inhibitor of acid-sensing ion channel 3 (ASIC3), potentially contributing to research in chronic pain treatment (Ex/Em = 356/451 nm).
  29. DNA Structure Probe

    2-Aminopurine is a fluorescent analog of guanosine and adenosine, functioning as a DNA structure probe. Its insertion into oligonucleotides results in significant fluorescence quenching due to stacking interactions with adjacent natural bases. This property makes 2-Aminopurine an invaluable tool for investigating nucleic acid structure and dynamics in various research applications.
  30. Fluorescent Dye

    CellTracker Blue CMF2HC Dye is a fluorescent dye primarily used for visualizing and tracking live cells. It emits a blue fluorescence when excited at wavelengths between 450-460 nm, making it suitable for applications such as two-channel nucleic acid sequencing. Additionally, this dye facilitates the rapid assessment of microbial antibiotic sensitivity, providing valuable insights for microbiological research.
  31. DNA Fluorescent Dye

    Methyl Green is a non-intercalating fluorescent dye that targets DNA by selectively binding to the major groove. It exhibits high affinity, resistance to photobleaching, and stable fluorescence emission, making it suitable for various applications. Methyl Green can be utilized for fluorescent labeling of nuclei in embryonic tissues or cells, as well as for DNA staining and assessing cell activity in gel electrophoresis. Its fluorescence peaks are observed at 633 nm and 677 nm, enabling direct measurement through microscopy and flow cytometry.
  32. Topoisomerase IIα Inhibitor

    Topoisomerase II-IN-24 is a selective inhibitor of Topoisomerase IIα, exhibiting an IC50 of 41.67 μM. This compound has been shown to effectively inhibit the proliferation of cancer cells while inducing G2/M phase arrest and promoting apoptosis. Topoisomerase II-IN-24 is valuable for research focusing on cancer biology, particularly in the study of colon cancer.
  33. HDAC3 Inhibitor

    HDAC3-IN-2 is a potent inhibitor of histone deacetylase 3 (HDAC3), with an IC50 value of 14 nM. This pyrazinyl hydrazide compound exhibits cytotoxicity against triple-negative breast cancer cell lines, demonstrating an IC50 of 0.55 μM for 4T1 cells and 0.74 μM for MDA-MB-231 cells. In in vivo studies using tumor-bearing mouse models, HDAC3-IN-2 effectively enhances histone acetylation levels at H3K9, H3K27, and H4K12 while promoting apoptosis through increased caspase-3, caspase-7, and cytochrome c levels, alongside a decrease in proliferation markers such as Bcl-2, CD44, EGFR, and Ki-67.
  34. PARP1 Inhibitor

    PARP-1-IN-2 is a potent inhibitor of PARP1, exhibiting an IC50 value of 149 nM. This compound demonstrates significant anti-proliferative effects on the A549 human lung adenocarcinoma epithelial cell line and induces apoptosis in these cells. Its favorable ADME profile suggests high permeability across the blood-brain barrier, making it a valuable tool for research in cancer biology and therapeutic applications targeting PARP1-related pathways.
  35. Topoisomerase I/II Inhibitor

    Topoisomerase I/II Inhibitor 8 is a dual-target inhibitor that effectively disrupts the function of both Topoisomerase I and II, leading to DNA damage. This compound activates PARP-1, which in turn stimulates the necroptotic pathway via RIPK1, RIPK3, and MLKL signaling. Exhibiting significant anticancer properties, Topoisomerase I/II Inhibitor 8 induces cell death in cancer cells, presenting a promising approach to overcome drug resistance in cancer therapies.
  36. PARP1 Inhibitor

    4,4′-Secalonic acid D is a potent inhibitor of PARP1, a key enzyme in the DNA repair pathway. This compound promotes the accumulation of reactive oxygen species (ROS) and DNA damage, leading to the activation of the caspase-3/GSDME pathway, which triggers apoptosis and pyroptosis in tumor cells. 4,4′-Secalonic acid D exhibits significant anti-tumor activity, making it a valuable tool for cancer research and therapeutic investigations.
  37. HDAC1/6 Inhibitor

    HDAC1/6-IN-3 is a potent inhibitor of histone deacetylases 1 and 6 (HDAC1 and HDAC6). It demonstrates strong inhibitory activity, with IC50 values of 1.1 nM for HDAC1 and 2.7 nM for HDAC6. This compound effectively induces cell cycle arrest in the G0/G1 phase and promotes both apoptosis and pyroptosis in HepG2 cells. Additionally, HDAC1/6-IN-3 exhibits significant antitumor effects in the HepG2 xenograft model and is valuable for research focused on various types of cancer, including liver, lung, colon, and breast cancers.
  38. Topoisomerase I Inhibitor

    Topoisomerase I Inhibitor 2 targets DNA topoisomerase I (Top1) with high specificity, effectively inhibiting its activity and leading to DNA damage. This compound not only induces apoptosis but also disrupts the G2/M phase of the cell cycle, thereby exhibiting significant anti-tumor effects. Its properties make it a valuable tool for cancer research and therapeutic studies focused on DNA damage response mechanisms.
  39. PARP-1 Inhibitor

    PARP-1-IN-3 is a potent inhibitor of PARP-1, with IC50 values of 0.25 nM for PARP-1 and 2.34 nM for PARP-2. This benzamide derivative effectively induces apoptosis and leads to G2/M phase cell cycle arrest. PARP-1-IN-3 is valuable for research applications focused on cancer mechanisms and therapeutic strategies.
  40. 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.
  41. 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.
  42. 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.
  43. 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.
  44. 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.
  45. 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.
  46. 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.
  47. 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.
  48. 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.
  49. 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.
  50. 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.

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