DNA/RNA Synthesis Inhibitor

GSK 299423 is an antibiotic agent.GSK299423 shows potent inhibition of supercoiling by DNA gyrase from S. aureus(IC₅₀=14 nM）and Escherichia coli(IC₅₀=100 nM.

Usnic acid is a secondary metabolite of lichens with a unique dibenzofuran skeleton. Usnic acid inhibits DNA/RNA synthesis and has antibacterial activity. Usnic acid induces cell cycle arrest and apoptosis and has anticancer activity. Usnic acid inhibits RANKL-mediated osteoclast formation and function by reducing the transcriptional and translational expression of NFATc1. Usnic acid has antioxidant and anti-inflammatory activities by inhibiting lipid peroxidation and myeloperoxidase.

SET-12 is an antiparasitic agent with high activity and selectivity against the Leishmania amazonensis. SET-12 exhibits excellent activity against the pre-flagellated form of the Leishmania amazonensis, with an IC₅₀ of 10.89 μM and a selectivity index (SI) of up to 12.1. SET-12 is also effective against the non-flagellated form within cells, with an IC₅₀ of 3.81 μM and a further increased selectivity index (SI) to 34.5. SET-12 causes signs of parasite cell apoptosis, including mitochondrial damage and accumulation of ROS.

Trifluridine (Standard) is the analytical standard of Trifluridine. This product is intended for research and analytical applications. Trifluridine (Trifluorothymidine) is an irreversible and orally active thymidylate synthase inhibitor, and thereby suppressing DNA synthesis. Trifluridine is an antiviral molecule used for research of HSV, rhabdovirus and orthopoxvirus infection. Trifluridine induces cell apoptosis and autophagy. Trifluridine is also an anticancer agent used in studies of metastatic colorectal cancer, gastrointestinal tumors.

T2AA hydrochloride is a non-peptide small molecule PCNA inhibitor T2 amino alcohol (T2AA) that lacks thyroid hormone activity. T2AA hydrochloride inhibits the interaction of PCNA/PIP-box peptide (IC50=~1 μM) and the interaction of PCNA with full-length p21 protein.

Ibezapolstat hydrochloride is a first-in-class, orally active DNA polymerase IIIC (pol IIIC) inhibitor, with a K_i of 0.325 μM for the DNA pol IIIC from C. difficile. Ibezapolstat hydrochloride is developed for the research of C. difficile infection(CDI).

Viquidacin (NXL 101) is an antibiotic with inhibitory activity against topoisomerase IV and DNA gyrase. Viquidacin exhibits antibacterial activity against gram positive bacterial by inhibiting the supercoiling, decatenation and relaxation in strains Staphylococcus aureus and Escherichia coli in micromolar levels. Viquidacin inhibits S. aureus wildtype and mutants with MIC of 2-128 mg/L.

Pazufloxacin (mesylate) (Standard) is the analytical standard of Pazufloxacin mesylate (HY-B0724A). This product is intended for research and analytical applications. Pazufloxacin mesylate is an orally active fluoroquinolone antimicrobial agent. Pazufloxacin mesylate inhibits DNA gyrase with IC₅₀ values of 0.88 μg/mL (E. coli) and 1.9 μg/mL (P. aeruginosa). Pazufloxacin mesylate exhibits broad-spectrum antimicrobial activity, with MIC₉₀ values ranging from 0.025 to 100 μg/mL against Gram-positive and Gram-negative bacteria, non-fermenting bacteria, Legionella spp., and anaerobic bacteria. Pazufloxacin mesylate is indicated for research on systemic infections, lung infections, urinary tract infections, and Legionella pneumonia.

Isomalathion is an isomer and impurity of Malathion (HY-B0943). Isomalathion inhibits Carboxyesterase and AChE, with an IC₅₀ value of 3.2 μM against bovine acetylcholinesterase. Isomalathion moderately reduces CYP1A2 transcript levels, increases CYP2B6 transcript levels, and induces dose-dependent DNA damage. Malathion is an organophosphorus insecticide.

Abyssinone V is a prenylated flavonoid with predicted anti-viral activity. Abyssinone V can be isolated from the stem bark of Erythrina melanacantha. Abyssinone V possesses good pharmacodynamics properties. Abyssinone V is predicted to be antivirals including anti-herpes (HSV) agent, with mechanisms comprising inhibition of polymerase, ATPase and membrane integrity.

6-Hydroxy-DOPA (Standard) is the analytical standard of 6-Hydroxy-DOPA. This product is intended for research and analytical applications. 6-Hydroxy-DOPA is a selective and effective allosteric inhibitor of the RAD52 ssDNA binding domain. 6-Hydroxy-DOPA can be used for the research of cancer.

Levofloxacin-d₃ ((-)-Ofloxacin-d₃) hydrochlorideis deuterium labeled Levofloxacin (hydrochloride). Levofloxacin ((-)-Ofloxacin) hydrochloride is an orally active antibiotic and is active against both Gram-positive and Gram-negative bacteria. Levofloxacin hydrochloride inhibits the DNA gyrase and topoisomerase IV. Levofloxacin hydrochloride can be used for chronic periodontitis, airway inflammation and BK Viremia research. Levofloxacin hydrochloride shows anti-orthopoxvirus activity.

DNA Gyrase-IN-15 (Compound 11) is an antimicrobial agent and inhibitor of DHPS and DNA gyrase, with IC₅₀s of 1.73 and 0.07 µM, respectively. DNA Gyrase-IN-15 shows antimicrobial activity against Enterococcus faecalis (MIC of 15.62 µg/mL), Acinetobacter baumannii, Enterobacter species (MIC of 7.81 µg/mL), Pseudomonas aeruginosa, Klebsiella pneumoniae and Staphylococcus aureus. DNA Gyrase-IN-15 also shows antibiofilm activity against Enterococcus faecalis.

Gemifloxacin (mesylate) (Standard) is the analytical standard of Gemifloxacin (mesylate). This product is intended for research and analytical applications. Gemifloxacin mesylate (SB-265805S; LB-20304a) is an orally active broad-spectrum quinolone antibacterial antibiotic. Gemifloxacin mesylate inhibits DNA synthesis by inhibiting DNA gyrase and Topoisomerase IV activities. Gemifloxacin mesylate has potent antibacterial activities against gram-positive bacteria in vitro efficacy study, particularly Streptococci and Staphylococci. Gemifloxacin mesylate has been used in the research of respiratory tract infections.

LMed 99 is an antiviral agent. LMed 99 inhibits viral RNA synthesis and reduces viral protein expression in a time-dependent manner. LMed 99 potently inhibits Influenza A virus replication. LMed 99 can be used in the research of Influenza A virus infections (H1N1, H5N1).

2-Fluoroadenine is a toxic purine bases. 2-Fluoroadenine has toxicity in nonproliferating and proliferating tumor cells. 2-Fluoroadenine can be used for researching anticancer.

Cyclothialidine E inhibits escherichia coli DNA helicases with an IC₅₀ of 0.7 μM.

ASO-5005 is a 20-mer Gapmer antisense oligonucleotide modified with locked nucleic acids (LNA), featuring a full phosphorothioate backbone, which targets BCL2 mRNA and BCL2L1 mRNA. ASO-5005 downregulates Bcl-2 expression via an RNase H-dependent mechanism, with its sequence fully complementary to BCL2 mRNA; it simultaneously downregulates Bcl-xL expression via an RNase H-dependent mechanism, with three mismatches between its sequence and BCL2L1 mRNA, while LNA modification enhances its activity against this mismatched target. ASO-5005 induces Apoptosis by activating Caspase-3 and cleaving ICAD. ASO-5005 does not significantly regulate the expression of Bcl-W, Survivin, Akt, or p53 in tumor cells. ASO-5005 can be used for research on breast cancer and non-small cell lung cancer.

Kukoamine B, a spermine alkaloid, is a potent dual LPS and CpG DNA inhibitor with K_d values of 1.23 µM and 0.66 µM, respectively. Kukoamine B exerts anti-inflammatory, anti-diabetic, anti-oxidant, anti-osteoporotic and neuroprotective effects. Kukoamine B has the potential for the study of sepsis. .

CPO 4 is a DNA-targeting antibacterial agent. CPO 4 intercalates into DNA to form a CPO 4-DNA complex, thereby blocking DNA replication. CPO 4 disrupts the metabolic activity of bacteria. CPO 4 induces intracellular protein leakage in bacteria. CPO 4 can be used for the research of drug-resistant bacterial infections.