DNA/RNA Synthesis Inhibitor

Antiproliferative agent-64 (Compound 76) is an inhibitor for eukaryotic translation initiation factor 4E (eIF4E), that block the secondary structure of mRNA, thereby inhibiting protein translation. Antiproliferative agent-64 inhibits the 5' untranslated region (5'UTR) of c-Myc (c-myc 5'UTR) with an EC₅₀ of 1.2 nM, inhibits 5'UTR encoding tubulin (tub 5'UTR) with an EC₅₀ of 40 nM. Antiproliferative agent-64 inhibits the proliferation of MDA-MB-231 with an EC₅₀ of 7 nM.

DNA Gyrase-IN-16 (Compound 9) is the inhibitor for DNA gyrase with an IC₅₀ of 1.609 μM. DNA Gyrase-IN-16 exhibits antibacterial activity, inhibits S. aureus and MRSA with MIC of 3.125 μM and 3.125 μM.

Rifamdin is a derivative of Rifampicin (HY-B0272). Rifamdin is an anti-tuberculosis agent. Rifamdin exerts its antibacterial effect by inhibiting the synthesis of bacterial RNA.

Dynemicin A is a potent antitumor antibiotic. Dynemicin A is a DNA synthesis inhibitor with an IC₅₀ of 2.2 ng/mL. Dynemicin A undergoes bioreductive epoxide ring opening and Bergman cyclization to generate a highly reactive benzenoid diradical, which specifically induces double-strand DNA cleavage. Dynemicin A can be used for research on bacterial infections, leukemia, and melanoma.

APX2014 is a Ref-1/APE1 inhibitor that inhibits Ref-1-induced transcription factor-DNA binding, thereby reducing the activation level of NF-κB and the expression of downstream pro-angiogenic targets. APX2014 blocks endothelial cell proliferation, lumen formation, migration and choroidal sprouting to exert anti-angiogenic activity. APX2014 activates the ISR pathway, promotes the death of pancreatic cancer cells and cancer-associated fibroblasts, and induces apoptosis in the absence of PRDX1. APX2014 inhibits the growth of pancreatic cancer spheroids, reduces the volume/weight of xenograft tumors, and decreases Ki-67 levels by targeting PRDX1. APX2014 can be used in research related to macular degeneration, retinopathy and pancreatic ductal adenocarcinoma.

FIT-039 (Standard) is the analytical standard of FIT-039. This product is intended for research and analytical applications. FIT-039 is a selective, ATP-competitive and orally active CDK9 inhibitor with an IC50 of 5.8 μM for CKD9/cyclin T1. FIT-039 does not inhibit other CDKs and other kinases. FIT-039 inhibits replication of HSV-1 (IC50 of 0.69 μM), HSV-2, human adenovirus, and human CMV. FIT-039 is a promising antiviral agent for inhibiting drug-resistant HSVs and other DNA viruses.

3′-Azido-2′,3′-dideoxy-CTP (AZddCTP) is a cytidine analog containing a 3-azido group. As a chain terminator, 3′-Azido-2′,3′-dideoxy-CTP can be incorporated into the nascent DNA chain by HIV reverse transcriptase. 3′-Azido-2′,3′-dideoxy-CTP terminates DNA synthesis due to the lack of a 3'-hydroxyl group, thereby inhibiting viral replication. 3′-Azido-2′,3′-dideoxy-CTP has IC₅₀ values of 15.6 μM and 160.8 μM for WT HIV and AZT^R HIV. 3′-Azido-2′,3′-dideoxy-CTP has antiviral activity.

Enitociclib (Standard) is the analytical standard of Enitociclib (HY-103019). This product is intended for research and analytical applications. Enitociclib ((+)-BAY-1251152; (+)-VIP152) is a selective CDK9 inhibitor (IC₅₀=3 nM) that inhibits transcriptional elongation by blocking Ser2/Ser5 phosphorylation of RNA polymerase II. Enitociclib specifically depletes key short-lived proteins such as c-MYC, MCL-1 and induces tumor cell apoptosis. Enitociclib also interferes with the production of enhancer RNAs (eRNA) and enhancer-promoter interactions, and downregulates oncogene expression at the epigenetic level. Enitociclib exerts synergistic effects with agents including Bortezomib (HY-10227), Lenalidomide (HY-A0003), Pomalidomide (HY-10984), Venetoclax (HY-15531) and Paclitaxel (HY-B0015), and even reverses paclitaxel resistance. Enitociclib serves as a vital research tool for various malignancies such as double-hit diffuse large B-cell lymphoma, multiple myeloma and pancreatic ductal adenocarcinoma.

Beaucage reagent (Standard) is the analytical standard of Beaucage reagent (HY-100951). This product is intended for research and analytical applications. Beaucage reagent is found to be potent in causing DNA cleavage.

Cyslopentenyl cytosine triphosphoric is an active metabolite of the antitumor nucleoside analogue cyclopentenyl cytosine (CPEC) within cells. Cyslopentenyl cytosine triphosphoric can inhibit CTP synthetase and deplete the pools of cytidine nucleotides. Cyslopentenyl cytosine triphosphoric can be used for the research of cancer, such as leukemia.

REV7/REV3L-IN-1 (Standard) is the analytical standard of REV7/REV3L-IN-1 (HY-100468). This product is intended for research and analytical applications. REV7/REV3L-IN-1 is a REV7/REV3L interaction inhibitor with an IC₅₀ of 78 μM. REV7/REV3L-IN-1 binds directly to REV7 and inhibits its interaction with REV3L. REV7/REV3L-IN-1 inhibits interstrand crosslink repair in cells. REV7/REV3L-IN-1 chemosensitizes cancer cells to Cisplatin (HY-17394). REV7/REV3L-IN-1 can be used in cervical cancer research.

4-Ethylcatechol is a ring-dihydroxylated metabolite of 4-Ethylphenol that leads to oxidative DNA damage.

4,8-DiMeIQx is an orally active mutagen, selective dopaminergic neurotoxicant, and DNA damaging agent. 4,8-DiMeIQx can be isolated from cooked beef, sausage, pork, and chicken. 4,8-DiMeIQx induces reverse mutations in *Salmonella typhimurium* TA98 in the presence or absence of S9 mix, and forms DNA adducts in vivo in rat liver. 4,8-DiMeIQx exhibits selective neurotoxicity toward dopaminergic neurons. 4,8-DiMeIQx shows no activity against non-dopaminergic neurons. 4,8-DiMeIQx can be used in studies related to Parkinson's disease and colorectal cancer.

Remdesivir O-desphosphate acetonide impurity (Standard) is the analytical standard of Remdesivir O-desphosphate acetonide impurity. This product is intended for research and analytical applications.

Methotrexate disodium (Standard) (Amethopterin disodium (Standard); CL14377 disodium (Standard); WR19039 disodium (Standard)) is the analytical standard of Methotrexate disodium (HY-14519A). This product is intended for research and analytical applications. Methotrexate disodium (Amethopterin disodium; CL14377 disodium; WR19039 disodium) is an orally active antifolate (Antifolate). Methotrexate disodium inhibits dihydrofolate reductase (DHFR), blocks tetrahydrofolate production, suppresses purine/pyrimidine synthesis and transmethylation, and causes intracellular accumulation of AICAR. Methotrexate disodium promotes extracellular adenosine release, regulates the cytokine network, and inhibits the alarmin function of HMGB1. Methotrexate disodium induces apoptosis and cytotoxicity, upregulates the expression of iNOS and COX-2, suppresses hippocampal neurogenesis, and induces pulmonary fibrosis. Methotrexate disodium is used in the research of various immune and inflammation-related diseases such as arthritis, psoriasis, systemic lupus erythematosus, as well as pulmonary fibrosis and breast cancer.

Amsacrine lactate (m-AMSA lactate) is a Topoisomerase II inhibitor. Amsacrine lactate intercalates into DNA. Amsacrine lactate induces Ca²⁺-mediated inactivation of ERK, and also downregulates AKT, promoting MCL1 downregulation mediated by GSK3β via reducing the phosphorylation level of GSK3β. Amsacrine lactate induces Apoptosis by activating Caspase-9 and Caspase-3. Amsacrine lactate blocks HERG potassium channels in the open/inactivated state. Amsacrine lactate induces chromosomal aberrations and sister chromatid exchanges, and inhibits the synthesis of RNA and DNA. Amsacrine lactate exhibits anti-leukemic activity. Amsacrine lactate causes cardiac repolarization disorders, QT interval prolongation, ventricular arrhythmias, and increases the risk of sudden cardiac death. Amsacrine lactate can be used in research related to acute myeloid leukemia, lymphoma and progressive malignancies.

Chebulinic acid (Standard) is the analytical standard of Chebulinic acid. This product is intended for research and analytical applications. Chebulinic acid is a potent natural inhibitor of M. tuberculosis DNA gyrase, also can inhibit SMAD-3 phosphorylation, inhibit H+ K+-ATPase activity.

Simeprevir (Standard) is the analytical standard of Simeprevir (HY-10241). This product is intended for research and analytical applications. Simeprevir (TMC435; TMC435350) is an oral, potent and highly specific hepatitis C virus (HCV) NS3/4A protease inhibitor with a K_i of 0.36 nM. Simeprevir inhibits HCV replication with an EC₅₀ of 7.8 nM. Simeprevir also potently suppresses SARS-CoV-2 replication and synergizes with Remdesivir. Simeprevir inhibits the main protease (Mpro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses.

Gangaleoidin is a FOXM1 inhibitor with an IC₅₀ of 2.8 μM. Gangaleoidin inhibits interaction between FOXM1’s DNA-binding domain and target DNA sequence, downregulates FOXM1 and downstream target gene CCNB1 at the transcriptional level. Gangaleoidin suppresses proliferation of FOXM1-overexpressing breast cancer cells. Gangaleoidin can be used for the research of breast cancer.

DNA Gyrase/ribosomes-IN-1 is a bacterial ribosome and DNA gyrase inhibitor, with IC₅₀ values of 1.11 μM and 3.31 μM, respectively. DNA Gyrase/ribosomes-IN-1 also inhibits CYP3A4, with an IC₅₀ of 18.5 μM, and exhibits stability in mouse plasma and liver microsomes. DNA Gyrase/ribosomes-IN-1 inhibits bacterial protein synthesis by interacting with ribosomal RNA and associated sites. DNA Gyrase/ribosomes-IN-1 suppresses bacterial DNA replication by interacting with the gyrase complex. DNA Gyrase/ribosomes-IN-1 restores activity against macrolide-resistant, erm-mediated Gram-positive pathogens and enhances activity against Gram-negative bacteria such as Haemophilus influenzae and Moraxella catarrhalis. DNA Gyrase/ribosomes-IN-1 can be used in research on community-acquired bacterial pneumonia.