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Catalog No.
Product Name
Application
Product Information
Citations
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RAD51 inhibitor
Bractoppin is a potent and selective inhibitor of phosphopeptide recognition by the BRCA1 tBRCT domain. -
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. -
SIRT1/SIRT3 inhibitor
4'-bromo-Resveratrol is a potent inhibitor of the deacetylases sirtuin 1 (SIRT1) and 3 (SIRT3).
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DNA gyrase/topoisomerase inhibitor
Zoliflodacin (ETX0914;AZD0914) is a novel spiropyrimidinetrione bacterial DNA gyrase/topoisomerase inhibitor. -
polymerase inhibitor
ERDRP-0519 is an orally available inhibitor of polymerase that shows efficacy against a lethal morbillivirus infection in a large animal model. -
ATR inhibitor
Gartisertib (VX-803, ATR inhibitor 2) is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM.
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NAD+ competitive inhibitor of PARP7
RBN-2397 is a potent, accross species and orally active NAD+ competitive inhibitor of PARP7 (IC50<3 nM). -
DNA replication inhibitor
Enocitabine is a nucleoside analog, and is a potent DNA replication inhibitor, and a DNA chain terminator. -
HDAC6 inhibitor
Tubastatin A is a potent HDAC6 inhibitor with an IC50 value of 15 nM. -
pan-HDAC inhibitor
Quisinostat dihydrochloride (JNJ-26481585 dihydrochloride) is an orally available, potent pan-HDAC inhibitor with IC50s of 0.11 nM, 0.33 nM, 0.64 nM, 0.46 nM, and 0.37 nM for HDAC1, HDAC2, HDAC4, HDAC10 and HDAC11, respectively. Quisinostat dihydrochloride has a broad spectrum antitumoral activity. -
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. -
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. -
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. -
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. -
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. -
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. -
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). -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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.
