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Catalog No.
Product Name
Application
Product Information
Citations
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RNA Polymerase Inhibitor
MRL-436 is an RNA polymerase inhibitor that exhibits significant antibacterial activity against Rifampicin-resistant strains. Its mechanism of action involves targeting residue 622 of the RNA polymerase β' subunit and the RNAP ω subunit. This compound is particularly valuable for research involving antibiotic resistance and the study of bacterial transcription mechanisms. -
SIRT1/3 Inhibitor
SPC-180002 is a dual inhibitor of SIRT1 and SIRT3, exhibiting IC50 values of 1.13 μM and 5.41 μM, respectively. This compound disrupts redox homeostasis through reactive oxygen species (ROS) generation, resulting in enhanced stability of the p21 protein and consequential mitochondrial dysfunction. SPC-180002 effectively inhibits cell cycle progression and reduces cancer cell proliferation, while also activating the Nrf2 signaling pathway, making it a valuable tool for cancer research and studies on metabolic dysregulation. -
SIRT2/Hsp70 Inhibitor
YM-08 is a selective inhibitor of SIRT2 and Hsp70, exhibiting an IC50 of 19.9 μM for SIRT2. This compound effectively penetrates the blood-brain barrier, making it a valuable tool for studying neurodegenerative diseases and cellular stress responses. Its dual inhibitory activity allows for investigation into SIRT2 and Hsp70's roles in various biological processes and potential therapeutic applications. -
HSP70/SIRT2 Inhibitor
HSP70/SIRT2-IN-2 is a dual inhibitor targeting SIRT2 and HSP70, demonstrating an IC50 of 45.1±5.0 μM for SIRT2. This compound exhibits significant antitumor activity, making it a valuable tool for cancer research. Its ability to simultaneously inhibit these two proteins positions HSP70/SIRT2-IN-2 as a useful candidate for studies focused on tumor progression and potential therapeutic strategies. -
HDAC1/HDAC2 Inhibitor
MRLB-223 is a selective inhibitor of HDAC1 and HDAC2, demonstrating potent activity against tumor cells. It induces histone hyperacetylation and activates the intrinsic apoptotic pathway, leading to tumor cell apoptosis and degradation of Bcr-Abl in a caspase-dependent manner. Notably, MRLB-223 mediates p53-independent cell death in Bcr-Abl-expressing myeloid cells and shows efficacy in animal models of Eμ-myc lymphoma. This compound is valuable for research focusing on the mechanisms of lymphomagenesis and therapeutic strategies for Eμ-myc lymphoma. -
ATR Inhibitor
ART0380 is a potent and selective ATR kinase inhibitor that targets the ATR-ATRIP complex. With an IC50 of 51.7 nM, ART0380 effectively inhibits ATR-dependent Chk1 serine 345 phosphorylation, leading to cell cycle disruption and DNA damage. This compound exhibits significant antitumor activity in preclinical models featuring various ataxia-telangiectasia mutated (ATM) gene alterations. ART0380 is applicable for cancer research, particularly in studies related to colorectal and prostate cancer. -
RNA-dependent RNA-polymerases Inhibitor
GS-443902 trisodium is a potent inhibitor of RNA-dependent RNA polymerases (RdRp), specifically targeting respiratory syncytial virus (RSV) and hepatitis C virus (HCV) RdRp with IC50 values of 1.1 μM and 5 μM, respectively. As the active triphosphate metabolite of Remdesivir (GS-5734), this compound is essential for research focused on viral replication mechanisms and the development of antiviral therapies. Its ability to effectively inhibit RdRp activity makes it a valuable tool for studies in virology and drug discovery. -
mtDNA Synthesis Inhibitor
Alovudine (3'-Fluoro-3'-deoxythymidine) is an inhibitor of mitochondrial DNA (mtDNA) synthesis and serves as a marker for DNA synthesis. This compound demonstrates reduced susceptibility to inflammatory changes compared to traditional markers, making it a more reliable biomarker in pancreatic cancer studies. Additionally, Alovudine exhibits significant anti-orthopoxvirus and anti-leukemic activities, providing valuable insights for ongoing research in virology and oncology. -
RNA Polymerase II/III Inhibitor
β-Amanitin is a cyclic peptide toxin that specifically targets and inhibits RNA Polymerase II and III, crucial enzymes in eukaryotic transcription. By obstructing these polymerases, β-Amanitin effectively halts protein synthesis, making it a valuable reagent in research focused on gene expression and transcription regulation. Additionally, its ability to induce cytotoxicity positions β-Amanitin as a potential component in antibody-drug conjugates (ADCs) for targeted therapeutic applications. -
RSV Polymerase Inhibitor
JNJ-8003 is a highly potent, orally active non-nucleoside inhibitor of respiratory syncytial virus (RSV) polymerase, exhibiting an IC50 of 0.29 nM. It specifically targets the L protein of the polymerase complex, effectively blocking the transcription and replication of the viral genome by inhibiting RNA-dependent RNA polymerase (RdRp) activity, with an IC50 of 0.67 nM. In vitro studies demonstrate subnanomolar efficacy, and it has shown significant effectiveness in mouse and neonatal lamb models. JNJ-8003 is a valuable reagent for investigating RSV biology and developing antiviral therapies. -
Topoisomerase Inhibitor
Hycanthone is a potent topoisomerase inhibitor that functions as a thioxanthenone DNA intercalator. It effectively inhibits RNA synthesis and the activity of DNA topoisomerases I and II, leading to a reduction in nucleic acid biosynthesis. Additionally, Hycanthone demonstrates significant inhibition of apurinic endonuclease-1 (APE1) through direct protein binding, with a binding affinity (KD) of 10 nM. This compound is recognized as a bioactive metabolite of Lucanthone and is noted for its anti-schistosomal properties, making it valuable in related research applications. -
DNA Polymerase β Inhibitor
Prunasin is a specific inhibitor of DNA Polymerase β, showing an IC50 value of 98 μM in rat models. As an orally active cyanogenic glucoside and a principal metabolite of Amygdalin, Prunasin exhibits notable anti-inflammatory and anti-fibrotic properties. This compound is valuable for research into conditions such as liver fibrosis, facilitating investigations into therapeutic strategies targeting DNA repair and fibrotic processes. -
Topoisomerase Inhibitor
Netropsin dihydrochloride is a potent topoisomerase inhibitor that functions as a minor-groove binder. It effectively inhibits the catalytic activity of isolated topoisomerases, disrupting the stabilization of cleavable complexes associated with topoisomerase I and II in the nucleus. Additionally, netropsin dihydrochloride exhibits notable antibacterial and antiviral properties, making it valuable for various research applications, including studies on DNA topology and therapeutic interventions against microbial infections. -
Telomerase Inhibitor
Braco-19 trihydrochloride is a potent telomerase inhibitor that disrupts telomerase capping and catalytic activity. By acting as a G-quadruplex binding ligand, Braco-19 stabilizes G-quadruplex formation at the 3' telomeric DNA overhang, leading to rapid cellular senescence or selective cell death. Additionally, Braco-19 demonstrates efficacy as an inhibitor of HAdV virus replication, making it a valuable tool for research in cancer biology and virology. -
Polθ/PARP Inhibitor
Polθ/PARP-IN-1 is a potent dual inhibitor targeting DNA polymerase theta (Polθ) and poly (ADP-ribose) polymerase (PARP), exhibiting IC50 values of 45.6 nM and 5.4 nM, respectively. This compound demonstrates significant antiproliferative activity by inducing apoptosis and cell cycle arrest at the G2/M phase, leading to DNA damage. Polθ/PARP-IN-1 is applicable in cancer research and may contribute to therapeutic strategies targeting tumorigenesis. -
DNA Polymerase Inhibitor
3,4-Dihydroxybenzylamine hydrobromide is a DNA polymerase inhibitor that exhibits cytotoxic effects in melanoma cells. This compound demonstrates significant growth inhibitory activity across various melanoma cell lines, with efficacy correlated to the levels of tyrosinase activity. Its unique mechanism makes it a valuable tool for investigating cellular processes related to DNA replication and repair in cancer research. -
DNA Synthesis Inhibitor
Cytarabine triphosphate trisodium is a competitive inhibitor of DNA synthesis, functioning as an active metabolite of Cytarabine. It is used primarily in research to assess the chemosensitivity of leukemic blasts to Cytarabine by measuring intracellular levels. This compound plays a critical role in studies related to leukemia treatment and the evaluation of drug efficacy in cancer therapies. -
MTH1 Inhibitor
BAY-707 is a potent and selective inhibitor of MTH1 (NUDT1) that functions through a substrate-competitive mechanism with an IC50 of 2.3 nM. This compound exhibits a favorable pharmacokinetic profile compared to other MTH1 inhibitors and demonstrates good tolerability in mouse models. Although BAY-707 has shown effective inhibition of MTH1, it does not exhibit significant anticancer activity in either in vitro or in vivo studies, making it suitable for research into MTH1 function and related pathways. -
RNA/DNA Synthesis Inhibitor
Sodium Camptothecin is a plant-derived alkaloid that functions primarily as an RNA and DNA synthesis inhibitor. It exhibits potent antitumor activity by effectively inhibiting the replication of adenoviruses, leading to significant disruption of viral DNA integrity. This compound is valuable for research applications focused on viral replication mechanisms and cancer therapy investigations. -
Topoisomerase II Inhibitor
F-14512 is a topoisomerase II inhibitor that selectively targets cancer cells via the polyamine transport system. By enhancing the interaction of polyamines with DNA, F-14512 effectively inhibits topoisomerase II, leading to significant DNA damage and subsequent cellular cytotoxicity, particularly in cells exhibiting high PTS activity. This compound has demonstrated potent antitumor efficacy in the MX1 breast tumor xenograft model, making it a valuable tool for researching breast cancer and exploring mechanisms of drug resistance in oncological studies. -
Viral DNA Polymerase Inhibitor
Foscarnet trisodium hexahydrate is a viral DNA polymerase inhibitor that reversibly suppresses viral replication. It is primarily utilized as an antiherpesvirus agent, demonstrating efficacy in the treatment of cytomegalovirus retinitis. This compound is valuable for researchers studying viral infections and developing antiviral therapies. -
Poly(A) polymerase Inhibitor
2'-Deoxyadenosine 5'-diphosphate disodium (dADP disodium) acts as an inhibitor of bacterial poly(A) polymerase. This compound is particularly useful in the synthesis of deoxyadenosine oligonucleotides when utilized with Escherichia coli polynucleotide phosphorylase and other related enzymes. Its role in inhibiting poly(A) polymerase makes it valuable for studies in RNA metabolism and gene regulation research. -
DNA Polymerase Inhibitor
ddATP trisodium solution (100 mM) serves as a chain-elongating inhibitor of DNA polymerase. As an active metabolite of 2',3'-dideoxyinosine, it is primarily utilized in the Sanger method for DNA sequencing. Additionally, this reagent is valuable for studying viral infections and other applications in molecular biology research. -
DENV Polymerase Inhibitor
NITD-2 is a selective inhibitor of dengue virus (DENV) polymerase, specifically targeting the RNA-dependent RNA polymerase (RdRp) to impede RNA elongation. This compound exhibits potent antiviral activity against DENV, making it a valuable tool for research focused on understanding dengue virus replication and developing therapeutic strategies. Its limited ability to penetrate cell membranes can be an important consideration for in vitro experimental design. -
DNA/RNA Synthesis Inhibitor
DHPS-IN-1 is a potent inhibitor of dihydropteroate synthase (DHPS), exhibiting a remarkable inhibitory potency with an IC50 of 0.014 μM. This compound effectively impedes DNA and RNA synthesis, demonstrating significant anti-melanoma activity. DHPS-IN-1 is relevant for research applications focused on understanding metabolic pathways in cancer and developing targeted therapies against melanoma. -
DNA/RNA Synthesis Inhibitor
3-Isomangostin is a potent inhibitor of the MutT homologue 1 (MTH1) with an IC50 value of 52 nM, impacting DNA and RNA synthesis. Derived from the shell of Garcinia mangostana L., it presents a valuable chemical tool for investigating anticancer mechanisms and developing novel therapeutic strategies against cancer. Its ability to inhibit MTH1 highlights its potential for applications in cancer research and drug discovery. -
DNA Polymerase α Inhibitor
NSC639828 is a potent inhibitor of DNA polymerase α, exhibiting an IC50 of 70 μM. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. NSC639828 can be utilized to investigate the role of DNA polymerase α in tumorigenesis and to explore potential therapeutic strategies in cancer treatment. -
RNA Synthesis Inhibitor
Nitracrine is an RNA synthesis inhibitor that covalently and reversibly binds to DNA, forming covalent adducts in vivo. As a 1-nitroacridine derivative, it exhibits potent hypoxia-selective cytotoxicity in vitro and serves as an effective antitumor agent. Nitracrine demonstrates cytotoxic effects against a wide range of cell types, making it a valuable tool for cancer research and therapeutic investigations. -
DNA Polymerase Inhibitor
Acyclovir triphosphate sodium is a potent inhibitor of viral DNA polymerase, functioning as a competitive analogue of deoxyguanosine triphosphate (dGTP). This compound also exhibits inhibitory activity against HIV-1 reverse transcriptase, leading to the termination of viral DNA synthesis. Acyclovir triphosphate sodium is valuable for research applications in virology and the study of antiviral mechanisms. -
DNA/RNA Synthesis Inhibitor
Methotrexate α-tert-butyl ester is an antimetabolite and antifolate compound that acts as a potent inhibitor of DNA and RNA synthesis. It demonstrates significant anti-tumor activity by effectively reducing tumor growth in HT1080 tumor-bearing mouse models. This compound is also utilized for its immunosuppressive and antineoplastic properties in various research applications. -
RNA Polymerase I Transcription Inhibitor
BMH-22 is a selective inhibitor of RNA polymerase I transcription, functioning independently of p53 pathways. This benzonaphthyridin compound induces reorganization of nucleolar marker proteins, indicative of nucleolar segregation, and destabilizes RPA194 through a proteasome-dependent mechanism. Additionally, BMH-22 effectively inhibits the synthesis of nascent rRNA and the expression of the 45S rRNA precursor. Its potent anticancer properties make it a valuable tool for studying cancer biology and RNA transcription regulation in various tumor models. -
RNA Polymerase Inhibitor
MMV688845 is an RNA polymerase inhibitor targeting nontuberculous mycobacteria (NTM) with demonstrated bactericidal activity against Mycobacterium abscessus. This compound exhibits potential anti-tuberculosis efficacy, making it a valuable tool for research in tackling mycobacterial infections. Its selective mechanism positions MMV688845 as a promising candidate for further exploration in antimicrobial studies and drug development. -
NS5B Polymerase/RdRp Inhibitor
Lomibuvir is a selective non-nucleoside inhibitor of the NS5B RNA-dependent RNA polymerase (RdRp) associated with Hepatitis C Virus (HCV). It targets the thumb pocket 2 of the NS5B polymerase with a binding affinity (Kd) of 17 nM and effectively inhibits HCV replication, demonstrated by an EC50 value of 5.2 nM in the 1b/Con1 subgenomic replicon model. Lomibuvir primarily interferes with the elongation phase of RNA synthesis, making it a valuable tool for studying HCV replication mechanisms and developing antiviral therapies. -
RNA Polymerases Inhibitor
3'-Deoxyuridine-5'-triphosphate (3'-dUTP) is a nucleotide analogue that serves as an inhibitor of DNA-dependent RNA polymerases I and II. It competitively inhibits the incorporation of UTP into RNA, demonstrating potent biological activity with a Ki value of 2.0 μM. This compound is valuable for research applications involving transcription regulation and the study of RNA synthesis mechanisms. -
DNA Synthesis Inhibitor
Cytarabine triphosphate (Ara-CTP) is a competitive inhibitor of DNA synthesis, serving as an active metabolite of Cytarabine. This compound plays a crucial role in cellular mechanisms by disrupting normal DNA replication processes. Its intracellular levels are valuable for predicting the chemosensitivity of leukemic blasts to Cytarabine, making it a significant biomarker in the treatment of leukemia and related hematological disorders. -
DNA Synthesis Inhibitor
Cytembena is a potent inhibitor of DNA synthesis, primarily targeting replicative DNA processes, purine biosynthesis, and tetrahydrofolate formylase activity. Its biological activity demonstrates significant anti-cancer effects, particularly in the treatment of ovarian and breast cancer, as well as providing pain relief in cases of skeletal metastases. This compound is valuable in research applications focused on cancer therapeutics and the mechanisms of DNA replication and repair. -
Topoisomerase I Inhibitor
Irinotecan-d10 is a deuterated derivative of Irinotecan, a potent inhibitor of topoisomerase I. By binding to the topoisomerase I-DNA complex, it disrupts the religation of DNA strands, thereby inducing DNA damage and apoptosis in rapidly dividing cells. This reagent is useful in cancer research, particularly in studies aimed at understanding the mechanisms of action of topoisomerase inhibitors and their therapeutic potential in oncology. -
Topoisomerase Inhibitor
Amonafide L-malate is a topoisomerase II inhibitor that functions as a DNA intercalator. This compound induces apoptotic signaling by disrupting the interaction between topoisomerase II and DNA, leading to inhibited DNA replication and cell proliferation. Amonafide L-malate is utilized in cancer research to study mechanisms of apoptosis and the effects of topoisomerase inhibition on tumor cells. -
HDAC Inhibitor
HDAC-IN-37 is a potent inhibitor of histone deacetylases (HDACs), demonstrating IC50 values of 0.0551 μM for HDAC1, 1.24 μM for HDAC3, 0.948 μM for HDAC8, and 34.2 μM for HDAC6. This compound effectively increases histone acetylation through a slow-off binding mechanism. Additionally, HDAC-IN-37 disrupts the transition from the G1 phase to the S phase of the cell cycle and promotes early apoptosis in various cell types, making it a valuable tool for research in cancer biology and therapeutic development. -
c-Met/HDAC Inhibitor
c-Met/HDAC-IN-3 is a dual inhibitor targeting c-Met and histone deacetylase 1 (HDAC1), exhibiting IC50 values of 12.50 nM and 26.97 nM, respectively. This compound demonstrates significant biological activity by inducing apoptosis and causing cell cycle arrest at the G2/M phase. c-Met/HDAC-IN-3 serves as a valuable tool for research in cancer biology and therapeutic development, particularly in studies focused on synergistic inhibition of oncogenic pathways. -
PARP-1/2/TNKS1/2 Inhibitor
PARP1/2/TNKS1/2-IN-1 is an inhibitor targeting PARP-1, PARP-2, TNKS1, and TNKS2, with IC50 values of 0.25 nM, 1.2 nM, 13.5 nM, and 4.15 nM, respectively. This compound demonstrates significant antitumor activity and promotes apoptosis, making it a valuable tool for research focused on cancer biology and therapeutic strategies. Its dual inhibitory action can facilitate the exploration of cellular repair mechanisms and enhance the understanding of poly(ADP-ribose) polymerases in cancer treatment. -
HDAC6 Inhibitor
HDAC6-IN-4 is a potent and selective inhibitor of histone deacetylase 6 (HDAC6), exhibiting an IC50 value of 23 nM. This compound promotes apoptosis in cancer cells and demonstrates significant antitumor efficacy while exhibiting minimal toxicity. HDAC6-IN-4 is valuable for research in cancer biology, particularly in studies focused on epigenetic regulation and therapeutic development. -
HDAC Inhibitor
HDAC-IN-31 is a selective and orally active histone deacetylase (HDAC) inhibitor, exhibiting IC50 values of 84.90 nM for HDAC1, 168.0 nM for HDAC2, 442.7 nM for HDAC3, and greater than 10,000 nM for HDAC8. This compound induces apoptosis and triggers G2/M phase cell cycle arrest, demonstrating significant antitumor efficacy. HDAC-IN-31 is applicable in research focused on diffuse large B-cell lymphoma and other cancer studies. -
Topoisomerase/HDAC Inhibitor
Top/HDAC-IN-1 is a dual inhibitor targeting both topoisomerase and histone deacetylases (HDACs), demonstrating IC50 values of 18 nM for HDAC1, 230 nM for HDAC2, 790 nM for HDAC3, 87 nM for HDAC6, and 5250 nM for HDAC8. This compound exhibits significant antitumor activity against HCT116 cells, with an IC50 of 180 nM, effectively inducing apoptosis and promoting G2 cell cycle arrest. Top/HDAC-IN-1 serves as a valuable tool in cancer research, particularly for studies involving epigenetic modulation and cell proliferation. -
mTOR/HDAC6 Inhibitor
mTOR/HDAC6-IN-1 is a potent dual inhibitor targeting mTOR and HDAC6, exhibiting IC50 values of 133.7 nM and 56 nM, respectively. This compound is known to induce significant autophagy and apoptosis while suppressing cell migration. It holds potential for research applications in triple-negative breast cancer (TNBC) studies, offering insights into the interplay between these critical pathways in cancer progression. -
HDAC Inhibitor
HDAC-IN-59 is a potent inhibitor of histone deacetylases (HDACs), demonstrating significant biological activity in cancer research. This compound promotes the generation of reactive oxygen species (ROS), leading to DNA damage and the induction of apoptosis via the mitochondria-related pathway. Additionally, HDAC-IN-59 effectively disrupts the cell cycle at the G2/M phase, making it a valuable tool for studying the mechanisms of cell growth regulation and apoptosis in various cancer models. -
JAK/HDAC Inhibitor
JAK/HDAC-IN-2 is a dual-target inhibitor of Janus kinase (JAK) and histone deacetylase (HDAC), specifically inhibiting HDAC3/6 and JAK1/2 with nanomolar potency. This compound demonstrates proapoptotic activity by inhibiting histone deacetylation and STAT3 phosphorylation, contributing to its mechanism of action. JAK/HDAC-IN-2 exhibits significant antiproliferative effects in various hematological malignancies and solid tumors, making it a valuable tool for cancer research and therapeutic studies. -
c-Met/HDAC Inhibitor
c-Met/HDAC-IN-2 is a highly potent dual inhibitor targeting c-Met and histone deacetylases (HDACs), exhibiting IC50 values of 18.49 nM for HDAC1 and 5.40 nM for c-Met. This compound demonstrates significant antiproliferative effects against various cancer cell lines, notably inducing G2/M-phase cell cycle arrest and apoptosis in HCT-116 cells. c-Met/HDAC-IN-2 is a valuable tool for investigating mechanisms of anti-cancer resistance and exploring therapeutic strategies in oncology research. -
HDAC inhibitor
HDAC-IN-67 is a potent inhibitor of histone deacetylases HDAC1 and HDAC6, demonstrating IC50 values of 22 nM and 8 nM, respectively. This compound effectively inhibits cell proliferation and induces apoptosis in various cancer cell lines. Its significant antitumor activity makes HDAC-IN-67 a valuable tool for cancer research and a potential candidate for therapeutic development. -
PIM-1/HDAC Inhibitor
PIM-1/HDAC-IN-1 is a selective inhibitor of PIM-1 as well as histone deacetylases HDAC 1 and HDAC 6, exhibiting an IC50 of 343.87 nM for PIM-1 and 63.65 nM and 62.39 nM for HDAC 1 and HDAC 6, respectively. This compound demonstrates significant apoptotic activity in MCF-7 cell lines, inducing pre-G1 apoptosis and causing cell cycle arrest at the G2/M phase. PIM-1/HDAC-IN-1 is a valuable tool for research on cancer biology and the regulation of cell proliferation and apoptosis.
