Catalog No.
Product Name
Application
Product Information
Citations
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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. -
HDAC1/CDK7 Inhibitor
HDAC1/CDK7-IN-1 is a dual inhibitor targeting HDAC1 and CDK7, exhibiting IC50 values of 893 nM and 248 nM, respectively. This compound effectively inhibits the proliferation of cancer cell lines, including MDA-MB-231, MCF-7, A549, and HCT-116. Additionally, HDAC1/CDK7-IN-1 induces cell cycle arrest and apoptosis specifically in HCT-116 cells, while also disrupting their migratory capacity. These properties make it a valuable tool for cancer research, particularly in exploring therapeutic strategies that target epigenetic regulation and cell cycle dynamics. -
HDAC Inhibitor
WMJ-J-09 is a potent HDAC inhibitor with sub-nanomolar activity, exhibiting IC50 values of 7.5 nM against HDAC1 and 3.9 nM against HDAC6, along with notable activity towards HDAC2, HDAC3, and HDAC8. This compound effectively disrupts the cell cycle and promotes apoptosis in cancer cells through the LKB1-AMPK-p38MAPK-p63-survivin signaling pathway. By inhibiting HDAC enzyme activity, WMJ-J-09 leads to the acetylation of critical proteins, thus contributing to the regulation of cell death in cancer models, such as HCT116 and FaDu cells. -
HDAC Inhibitor
TH-6 is a potent inhibitor of histone deacetylases (HDACs), demonstrating IC50 values of 0.115 µM for HDAC1, 0.135 µM for HDAC2, 0.242 µM for HDAC3, 0.138 µM for HDAC6, and 2.120 µM for HDAC8. This compound effectively inhibits cell migration and invasion while promoting apoptosis and inducing cell cycle arrest in the G2/M phase. TH-6 exhibits significant anti-tumor activity, making it a valuable tool for cancer research and therapeutic studies. -
Topoisomerase II Inhibitor
Topoisomerase II inhibitor 11 is a potent inhibitor of topoisomerase II, exhibiting an IC50 of 2.89 μM. It demonstrates significant antiproliferative activity, achieving 92.46% inhibition in the renal cancer cell line A498 with an IC50 of 3.5 μM. This compound induces cell cycle arrest at the G2/M phase, ultimately leading to inhibited cell proliferation and pro-apoptotic effects, making it an important tool for cancer research. -
HDAC Inhibitor
HDAC-IN-36 is a potent HDAC (histone deacetylase) inhibitor that targets HDAC6 with an IC50 of 11.68 nM. This compound demonstrates significant biological activity by promoting apoptosis, enhancing autophagy, and inhibiting cellular migration. HDAC-IN-36 is applicable in cancer research, particularly in studies focusing on anti-tumor and anti-metastatic mechanisms in breast cancer. -
HDAC Inhibitor
Trichostatin C is an HDAC inhibitor that plays a crucial role in modulating gene expression by preventing the deacetylation of histones. This compound exhibits significant anticancer activity, inducing apoptosis and causing cell cycle arrest in the G2/M phase, making it particularly effective against lung cancer and urothelial bladder cancer. Additionally, Trichostatin C promotes differentiation in Friend leukemic cells and demonstrates antifungal properties, highlighting its potential in various research applications related to cancer biology and fungal infections. -
DNA Synthesis Inhibitor
(rel)-Oxaliplatin is a DNA synthesis inhibitor that functions through the formation of DNA crosslinks, thereby obstructing DNA replication and transcription. This compound induces apoptosis in cancer cells, making it a valuable tool for studying cancer biology and treatment mechanisms. It is widely utilized in cancer research to explore therapeutic strategies targeting DNA repair pathways. -
Purine Nucleoside Analog
2'-O-Methyl-5-iodouridine is a purine nucleoside analog that exhibits significant antitumor activity, particularly against indolent lymphoid malignancies. Its mechanism of action involves the inhibition of DNA synthesis and the induction of apoptosis, making it a valuable tool in cancer research. This compound can be utilized in studies aimed at understanding the biochemical pathways of cancer and the development of novel therapeutic strategies. -
JMJD3/HDAC1/HDAC6 Inhibitor
JMJD3/HDAC-IN-1 is a dual inhibitor targeting both Jumonji domain-containing protein demethylase 3 (JMJD3) and histone deacetylases HDAC1 and HDAC6. With an IC50 value of 16 nM for HDAC1, this compound induces hypermethylation of histone H3K27 and hyperacetylation of H3K9, promoting apoptosis through cleavage of caspase-7 and PARP. JMJD3/HDAC-IN-1 demonstrates significant anti-cancer activity by inhibiting cell cloning, migration, and invasion, making it valuable in cancer research and therapeutic studies. -
Topoisomerase Inhibitor
Cholesteryl hemisuccinate is a topoisomerase inhibitor with notable hepatoprotective and anticancer properties. It effectively mitigates acetaminophen-induced hepatotoxicity by preventing hepatic apoptosis and necrosis. Additionally, cholesteryl hemisuccinate interferes with DNA replication and repair mechanisms by inhibiting DNA polymerase and DNA topoisomerase, ultimately leading to reduced tumor growth. This compound is suitable for applications in cancer research and liver protection studies. -
Topoisomerase II Inhibitor
Etoposide phosphate is a selective inhibitor of topoisomerase II, instrumental in disrupting DNA re-ligation processes. As the phosphate ester proagent of etoposide, it exhibits potent anti-cancer activity by inducing cell cycle arrest, apoptosis, and autophagy in cancer cells. This compound is primarily employed in cancer research to explore mechanisms of action and potential therapeutic strategies in oncology. -
HDAC3/p-STAT3 Inhibitor
1-Stearoyl-sn-glycero-3-phosphocholine is an inhibitor of histone deacetylase 3 (HDAC3) and the phosphorylation of signal transducer and activator of transcription 3 (p-STAT3). This compound has demonstrated the ability to induce apoptosis and exhibits significant anticancer activity in chronic myelogenous leukemia (CML) K562 cells. It serves as a valuable tool for researchers investigating the therapeutic potential of HDAC inhibitors in cancer treatment. -
SIRT7 Inhibitor
SIRT7 Inhibitor 97491 is a selective inhibitor of the SIRT7 enzyme, exhibiting an IC50 of 325 nM and effectively reducing its deacetylase activity in a dose-dependent manner. This compound enhances tumor suppression by stabilizing the p53 protein through acetylation at lysine residues K373 and K382. Additionally, SIRT7 Inhibitor 97491 promotes apoptosis via the caspase signaling pathway, making it a valuable tool for cancer research and studies focused on elucidating the role of SIRT7 in tumor progression. -
eIF4A Inhibitor
CR-1-31-B is a synthetic rocaglate that serves as a potent inhibitor of the eukaryotic translation initiation factor eIF4A. By disrupting the interaction between eIF4A and RNA, CR-1-31-B impedes the initiation phase of protein synthesis. This compound has been shown to affect the association of Plasmodium falciparum eIF4A with RNA and induce apoptosis in neuroblastoma and gallbladder cancer cells, making it a valuable tool for studying mechanisms of protein synthesis and cancer biology. -
Topoisomerase II Inhibitor
ICRF-193 is a potent inhibitor of DNA Topoisomerase II, disrupting DNA synthesis and inducing apoptosis in cancer cells. This compound exhibits significant anti-cancer and anti-inflammatory activities, making it valuable for research in oncology and inflammation. Additionally, ICRF-193 demonstrates cardioprotective properties against anthracycline-induced toxicity in cardiomyocytes. It is particularly relevant for studies focusing on acute promyelocytic leukemia, as well as broader investigations into cancer, infection, inflammation, and cardiovascular conditions. -
Fluorescent Tag
Ethidium bromide is a fluorescent intercalating agent widely used in molecular biology as a nucleic acid stain. It inserts between DNA base pairs, allowing visualization of DNA and RNA under ultraviolet (UV) light during techniques such as agarose gel electrophoresis. Due to its high sensitivity and strong fluorescence, Ethidium bromide is a standard tool for nucleic acid detection, though it is handled with caution because of its mutagenic properties. -
RNA Aptamers Probe
DFHBI-1T is a membrane-permeable fluorescent probe activated by RNA aptamers, with excitation/emission maxima at 472/507 nm. It specifically binds to aptamers such as Spinach, Spinach2, iSpinach, and Broccoli, resulting in bright fluorescence with low background signal. DFHBI-1T is commonly used for live-cell imaging of RNA. -
HDAC inhibitor
Nullscript is an inactive analog of Scriptaid and serves as a negative control for Scriptaid, a representative histone deacetylase (HDAC) inhibitor. Despite its inactivity as an HDAC inhibitor, Nullscript inhibits the growth of *Cryptosporidium parvum* with an IC₅₀ value of 2.1 μM. -
HDAC6-UBD antagonist
SGC-UBD253 is a potent antagonist of the HDAC6 ubiquitin-binding domain (UBD). It is suitable for use in cancer research. -
HDAC1/DNA Methyltransferase Inhibitor
Psammaplin A, a marine-derived metabolite, is a potent inhibitor of HDAC1 (IC50: 45 nM), DNA methyltransferases (IC50: 18.6 nM), and aminopeptidase N (IC50: 18 μM). It also suppresses DNA topoisomerase and farnesyl protein transferase activities. As a PPARγ activator, Psammaplin A induces apoptosis and exhibits antitumor, anti-inflammatory, and anti-angiogenic properties. Additionally, it demonstrates antibacterial activity against Gram-positive bacteria by inhibiting DNA synthesis and DNA -
SAHH inhibitor
Adenosine dialdehyde is a purine nucleoside analogue and a potent inhibitor of S-adenosylhomocysteine hydrolase (SAHH), with a Ki of 3.3 nM. By inhibiting SAHH, it disrupts methylation-dependent processes, contributing to its demonstrated anti-tumor activity in vivo. Adenosine dialdehyde is a valuable tool in cancer research, particularly in studies targeting epigenetic regulation and methylation pathways. -
DNA polymerase theta (Polθ) inhibitor
RP-6685 is a potent, selective, and orally active inhibitor of DNA polymerase theta (Polθ), with an IC50 of 5.8 nM as measured by the PicoGreen assay. It exhibits significant antitumor efficacy in mouse xenograft models. Additionally, RP-6685 contains an alkyne functional group, making it a useful click chemistry reagent capable of undergoing copper-catalyzed azide-alkyne cycloaddition (CuAAC) with azide-containing molecules, enabling its application in chemical biology and drug discovery research. -
DHX9 inhibitor
ATX968 (example 31) is an orally active, potent, and selective inhibitor of ATP-dependent RNA helicase A (DHX9), with an EC50 of 0.054 μM in circBRIP1-expressing models. It demonstrates robust and durable tumor growth inhibition or regression in mouse xenograft studies using microsatellite instability-high (MSI-H) and mismatch repair-deficient (dMMR) colorectal cancer cell lines, highlighting its potential for targeted cancer therapy. - L-Asparaginase (L-ASNase) is a deamidating enzyme that catalyses the hydrolysis of L-asparagine and L-glutamine, and can be used for the research of acute lymphoblastic leukemia. L-Asparaginase depletes L-asparagine from plasma resulting in inhibition of RNA and DNA synthesis with the subsequent blastic cell apoptosis.
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Polθ DNA polymerase inhibitor
ART899 is a highly specific allosteric inhibitor of the DNA polymerase domain of polymerase theta (Polθ). It effectively enhances the radiosensitivity of tumor cells and demonstrates good tolerability when combined with fractionated radiation therapy. ART899 significantly reduces tumor growth compared to radiation alone, making it a promising candidate for combination cancer radiotherapy strategies. -
DNA Alkylator
Illudin S is a natural sesquiterpene compound with potent cytotoxic, anti-tumor, and antiviral activities. It exhibits genotoxic effects and disrupts cell cycle progression by blocking the G1-S phase transition in human leukemia cells. Illudin S is of interest in cancer research due to its ability to target rapidly proliferating cells. -
DNA gyrase inhibitor/Hsp90 antagonist
Novobiocin (Albamycin) is a potent and orally active antibiotic that functions as a DNA gyrase inhibitor and a heat shock protein 90 (Hsp90) antagonist. It holds potential for research into highly β-lactam-resistant pneumococcal infections and has demonstrated antiviral activity against orthopoxviruses. -
PARG inhibitor
COH34 is a potent and selective inhibitor of poly(ADP-ribose) glycohydrolase (PARG), with an IC50 of 0.37 nM. It binds to the catalytic domain of PARG (Kd = 0.547 μM), prolonging PARylation at sites of DNA damage and trapping DNA repair factors, thereby interfering with the DNA damage response. -
Endoplasmic Reticulum Stress Inhibitor
Tauroursodeoxycholate (Tauroursodeoxycholic acid; TDUCA) dihydrate is an inhibitor of endoplasmic reticulum (ER) stress that significantly downregulates pro-apoptotic molecules, including caspase-3 and caspase-12. Additionally, it suppresses ERK signaling, contributing to its cytoprotective and anti-apoptotic effects. -
DNA polymerase inhibitor
Aphidicolin is a tetracyclic diterpenoid antibiotic produced by the mold Cephalosporium aphidicola, known for its potent and selective inhibition of DNA polymerase α and δ. By interfering with these polymerases, Aphidicolin blocks DNA synthesis and prevents mitotic cell division, making it a valuable tool for studying cell cycle regulation and DNA replication. In addition to its antiproliferative properties, Aphidicolin inhibits viral DNA synthesis and demonstrates antiviral activity against herpes simplex virus and orthopoxviruses. It also enhances apoptosis induced by arabinosyl nucleosides in human promyelocytic leukemia cells, suggesting potential in combination therapies for cancer and viral infections. Aphidicolin is widely used in research involving DNA replication stress, antiviral mechanisms, and cell cycle synchronization. -
POLRMT inhibitor
IMT1 is a first-in-class, specific, and noncompetitive inhibitor of human mitochondrial RNA polymerase (POLRMT). It induces a conformational change in POLRMT, preventing substrate binding and inhibiting transcription in a dose-dependent manner in vitro. IMT1 decreases deoxynucleoside triphosphate levels and citric acid cycle intermediates, leading to significant depletion of cellular amino acid levels. IMT1 holds potential for the treatment of diseases associated with mitochondrial transcription disorders. -
DNA Repair/Replicase Modulator
N-Nitrosodiethylamine (Diethylnitrosamine, DEN) is a highly potent hepatocarcinogenic dialkylnitrosamine found in tobacco smoke, water, cheddar cheese, cured and fried foods, and various alcoholic beverages. It induces alterations in nuclear enzymes involved in DNA repair and replication, contributing to its carcinogenicity. DEN causes tumors across multiple animal species, primarily affecting the nasal cavity, trachea, lung, esophagus, and liver. -
WRN inhibitor
HRO761 (Werner syndrome RecQ helicase-IN-1, example 42) is a potent and selective inhibitor of the Werner syndrome RecQ DNA helicase (WRN), an essential enzyme involved in DNA replication, repair, and genome stability. Inhibition of WRN has shown synthetic lethality in cancers with microsatellite instability (MSI) or deficient DNA mismatch repair (dMMR), making HRO761 a promising candidate for targeted cancer therapy. It is being explored in preclinical cancer research to evaluate its efficacy in selectively killing WRN-dependent tumor cells while sparing normal cells. -
PolΘ inhibitor
PolQi2 is a selective inhibitor of DNA polymerase theta (Polθ), specifically targeting its N-terminal helicase domain to suppress the alternative end-joining (alt-EJ) DNA repair pathway. By inhibiting Polθ, PolQi2 enhances the precision and integration efficiency of CRISPR/Cas9-mediated gene editing across diverse genomic loci and cell lines. Furthermore, when used in combination with DNA-PK inhibitors, PolQi2 significantly reduces off-target effects associated with Cas9 activity. These properties make PolQi2 a valuable tool for improving the fidelity and efficiency of gene editing applications in both basic research and potential therapeutic contexts. -
RNA pol III inhibitor
ML-60218 is a broad-spectrum RNA polymerase III (Pol III) inhibitor with IC₅₀ values of 32 μM in *Saccharomyces cerevisiae* and 27 μM in human cells. It inhibits Pol III–mediated transcription, which is essential for the synthesis of small RNAs such as tRNAs and 5S rRNA. ML-60218 has been shown to disrupt pre-assembled viroplasms and prevent the formation of new ones, indicating its antiviral potential. Notably, this activity occurs independently of de novo transcription of host cellular RNAs, suggesting a direct effect on viral replication machinery. ML-60218 is a valuable tool for studying Pol III function and holds potential for antiviral research. -
POLRMT inhibitor
IMT1B (LDC203974) is an orally bioavailable, noncompetitive, and selective allosteric inhibitor of mitochondrial RNA polymerase (POLRMT). By targeting POLRMT, IMT1B disrupts mitochondrial DNA (mtDNA) transcription and impairs mitochondrial gene expression, leading to reduced mitochondrial function. This mechanism contributes to its potent anti-tumor effects, particularly in cancer cells that are highly dependent on mitochondrial metabolism. IMT1B holds promise as a therapeutic agent for targeting mitochondrial vulnerabilities in tumors. -
glutamine amidotransferase inhibitor
Azaserine (CI-337) is a glutamine analog and competitive inhibitor of glutamine amidotransferase, an enzyme involved in nucleotide biosynthesis. It exhibits both antibiotic and antitumor properties by disrupting glutamine-dependent metabolic processes essential for cell proliferation. Azaserine demonstrates antibacterial activity and has shown antitumor effects in various cancer models. However, it has also been reported to possess tumorigenic potential under certain conditions, warranting cautious evaluation. -
HDAC11 inhibitor
Elevenostat (JB3-22) is a selective histone deacetylase 11 (HDAC11) inhibitor with an IC₅₀ of 0.235 µM. It exhibits antitumor activity by inducing apoptosis in multiple myeloma cells and shows potential as a therapeutic agent in hematologic malignancies. Additionally, Elevenostat has been shown to inhibit the maturation of mouse oocytes, suggesting a role for HDAC11 in reproductive biology and offering a tool for studying epigenetic regulation in oocyte development.
