DNA/RNA Synthesis Inhibitor

Hydroxycitric acid is an orally active, multi-target, multi-bioactive organic acid. activates Nrf2 and its downstream molecule GPX4, increases glutathione levels, and thereby inhibits ferroptosis. Hydroxycitric acid activates the Nrf2/Keap1 and ACLY/NF-κB signaling pathways, upregulates the activities of antioxidant enzymes such as superoxide dismutase, reduces MDA content, thereby alleviating oxidative stress and renal tubular epithelial cell apoptosis, and improves pulmonary vascular and right ventricular remodeling. Hydroxycitric acid activates both the AMPK and mTORC1/S6K pathways, triggers the unfolded protein response, arrests the cancer cell cycle, and induces DNA fragmentation.

L82 is a selective and uncompetitive DNA ligase 1 (DNA Lig1) inhibitor (hLig1 IC₅₀=12 μM). L82 shows anti-proliferative activity to breast cancer cells.

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.

Sodium pyrophosphate (Disodium pyrophosphate) is an orally active reverse transcriptase ribonuclease H inhibitor. Sodium pyrophosphate forms soluble complexes with iron from ferric pyrophosphate to promote intestinal iron absorption. Sodium pyrophosphate increases the β-sheet content of oxidatively damaged myofibrillar protein gels and enhances the gastric digestibility and antioxidant activity of their digestion products. Sodium pyrophosphate prevents the degradation of RNA-DNA hybrids, inhibits antisense complementary DNA synthesis, induces phage DNA leakage, and causes random mutations in temperate phages.

Chromomycin A3 is an inhibitor that selectively binds to GC-rich DNA sequences. Chromomycin A3 targets the DNA minor groove after forming a dimer with Mg²⁺. Chromomycin A3 inhibits DNA replication and transcription, blocks the binding of Sp1 transcription factor to target gene promoters, downregulates the expression of anti-apoptotic proteins such as FLIP, Mcl-1, and XIAP, and induces S-phase cycle arrest and caspase-dependent apoptosis in tumor cells. Chromomycin A3 can antagonize oxidative stress induced by glutathione depletion and neuronal apoptosis induced by Camptothecin (HY-15660). Chromomycin A3 can be used in basic research on malignant tumors such as cholangiocarcinoma, and is a potential chemosensitizer and GC-rich region probe.

Neobavaisoflavone, a flavonoid, is isolated from the seeds of Psoralea corylifolia. Neobavaisoflavone exhibits anti-inflammatory, anti-cancer and anti-oxidation activities. Neobavaisoflavone inhibits DNA polymerase at moderate to high concentrations. Neobavaisoflavone also inhibits platelet aggregation.

X5050 is a REST inhibitor, with an EC₅₀ of 2.1 μM.

TH588 is first-in-class nudix hydrolase family inhibitor that potently and selectively engage and inhibit the MTH1 (IC₅₀= 5 nM).

DHICA (5,6-Dihydroxyindole-2-carboxylic acid) is an eumelanin building block, GPR35 agonist and melanin synthesis intermediate. DHICA activates GPR35, triggering dynamic mass redistribution and β-arrestin translocation. DHICA interacts with DNA and interferes with Fpg activity. DHICA promotes the generation of single-strand breaks in plasmid DNA. DHICA increases the activity and expression levels of SOD and Catalase. DHICA is applicable to research related to skin cancer and colon 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.

DHX9-IN-1 is an inhibitor of ATP-dependent RNA helicase A (DHX9). Its EC₅₀ value is 1.41 μM. DHX9-IN-1 has anti-tumor activity and can be used in colorectal cancer research.

Zoliflodacin (ETX0914;AZD0914) is a novel spiropyrimidinetrione bacterial DNA gyrase/topoisomerase inhibitor. Zoliflodacin has potent in vitro antibacterial activity against Gram-positive and Gram-negative organisms, including S. aureus with the MIC₉₀ of 0.25 μg/mL.

2'-O-Methylcytidine is an orally active 2'-substituted nucleoside as a inhibitor of HCV replication with antiviral activity. 2'-O-Methylcytidine inhibits RNA-dependent RNA polymerase (NS5B)-catalyzed RNA synthesis in vitro, in a manner that is competitive with substrate nucleoside triphosphate.

Rhodizonic acid disodium (Sodium rhodizonate dibasic) is a transition metal-dependent pro-oxidant and lead detection agent that induces reactive oxygen species generation, DNA damage, and inhibits Aconitase activity. Rhodizonic acid disodium generates superoxide anion radicals in an iron (II)-dependent manner, leading to aconitase inactivation. Rhodizonic acid disodium also triggers hydroxyl radical-mediated DNA strand breaks and 8-OHdG formation via copper ion reduction. Rhodizonic acid disodium reacts with lead to form a scarlet precipitate, with the color intensity proportional to lead content, enabling qualitative or quantitative analysis of lead. Rhodizonic acid disodium can also be used for real-time visualization of the dynamic process of lead sequestration in the plant rhizosphere and evaluation of the effects of environmental factors such as soil type on the stability of lead-sequestering structures.

Bleomycin A5 (Pingyangmycin) is a glycopeptide antibiotic with multiple biological activities, which can be isolated from Streptomyces. Bleomycin A5 exerts cytotoxic effects by binding to Fe²⁺ to form a complex, inducing single-strand and double-strand DNA breaks, and inhibiting DNA replication. Bleomycin A5 inhibits Drp1-mediated mitochondrial fission and suppresses PINK1/Parkin pathway-mediated mitophagy, ultimately triggering mitochondria-mediated cellular apoptosis. Bleomycin A5 can be used in cancer research.

Isopimpinellin, an orally active compound isolated from Glomerella cingulata. Isopimpinellin blocks DNA adduct formation and skin tumor initiation by 7,12-dimethylbenz[a]anthracene. Isopimpinellin possesses anti-leishmania effect.

2'-O-Methylguanosine is a modified nucleoside produced in tRNAs by the action of tRNA guanosine-2’-O-methyltransferase. 2'-O-Methylguanosine results in apoptotic changes of cells.

L82-G17 is an uncompetitive DNA ligase I (Lig I)-selective inhibitor. L82-G17 inhibits the third step of the ligation reaction, phosphodiester bond formation. L82-G17can be used as a probe of the catalytic activity.

Vidarabine (Ara-A) is a Purine nucleoside derivative and Antiviral agent. The triphosphate derivative of Vidarabine competitively inhibits DNA polymerase, incorporates into the terminus of elongating DNA molecules, and interferes with the early steps of viral DNA synthesis. Vidarabine inhibits the replication of herpes simplex virus, varicella-zoster virus, cytomegalovirus, Epstein-Barr virus and vaccinia virus, reduces viral shedding, and accelerates skin healing. Vidarabine is metabolized to arabinosyl hypoxanthine, causes minimal impairment of corneal wound healing in rabbit models, and is associated with recurrence of herpes simplex encephalitis. Vidarabine can be used in the research of herpetic keratoconjunctivitis, herpes simplex encephalitis, herpetic uveitis, and chronic active hepatitis associated with hepatitis B virus.

Gemcitabine (Standard) is the analytical standard of Gemcitabine. This product is intended for research and analytical applications. Gemcitabine (LY 188011) is a pyrimidine nucleoside analog antimetabolite and an antineoplastic agent. Gemcitabine inhibits DNA synthesis and repair, resulting in autophagyand apoptosis.