integration

Unesbulin (PTC596) is an orally active, selective inhibitor of B-cell-specific Moloney murine leukemia virus integration site 1 (BMI-1).

HIV-1 integrase inhibitor 8 is an inhibitor of HIV-1 integrase, a critical enzyme necessary for the integration step in HIV replication [1].

CELT-327 is a potent, selective fluorescent hA2B/A3 adenosine receptor antagonist, exhibiting K_i values of 35.6 nM at A2B and 45.7 nM at A3 receptors. It efficiently labels HCT116 cells expressing A2B adenosine receptors in a dose-dependent manner, demonstrating rapid, uniform spread and integration of fluorescence within cell monolayers. In live HCT116 spheroids, it achieves consistent staining throughout, penetrating even the deepest layers. As a fluorescent adenosine receptor probe, CELT-327 is ideal for applications in fluorescence binding assays, live cell imaging, flow cytometry, and fluorescence polarization assays, serving as an effective alternative to GPCR radiolabeling ligands. Its excitation and emission peaks are at 589 nm and 616 nm, respectively, making it suitable for TR-FRET assays as an acceptor dye, particularly in combination with the CoraFlor1 TR-FRET donor.

L-731988 functions as an anti-HIV agent by inhibiting strand transfer, blocking integration, and hindering the replication of HIV-1 within cells.

Integrase-LEDGF p75 allosteric inhibitor 1 is an orally active inhibitor that targets integrase-LEDGF p75 (IN-LEDGF p75), impeding HIV-1 DNA integration and exhibiting antiviral effects against the HIV-1 recombinant molecular clone NL432 with an EC50 of 3.9 nM.

4-Thiouracil is a photoactivatable probe designated for site-specific applications in detecting RNA structures and nucleic acid-nucleic acid contacts. Upon illumination with ultraviolet light exceeding 300 nm and in the presence of oxygen, it serves as an energy donor, facilitating the generation of singlet oxygen through triplet-triplet energy transfer. This process enables the highly reactive oxygen species to interact with 4-thiouracil, leading to the formation of uracil and uracil-6-sulfonate; the latter exhibits fluorescence around a wavelength of approximately 390 nm. Additionally, 4-Thiouracil functions as a substrate for T. gondii uracil phosphoribosyltransferase, allowing the synthesis of 4-thiouridine monophosphate for subsequent integration into RNA.

Glucagon significantly impacts protein and amino acid metabolism. It hinders the integration of amino acids into the proteins of the liver, muscle, and pancreas, augmenting nitrogen excretion and stimulating hepatic urea synthesis. Additionally, it elevates hepatic transaminase and urea cycle enzyme levels. Glucagon also enhances hepatic amino acid uptake, facilitating their conversion into liver glycogen, and reduces blood amino acid concentrations [1].

DSPE-PEG(2000)-TCO is a PEGylated derivative of 1,2-distearoyl-sn-glycero-3-phosphoethanolamine (DSPE) that features a trans-cyclooctene (TCO) moiety capable of reacting with tetrazine to facilitate bioorthogonal conjugation in lipid nanoparticles (LNPs). This compound's integration of the TCO group endows it with significant utility in biomedical research, particularly in the bioconjugation of lipid nanoparticles.

CID-1304264 is an HIV-1 Rev pre-integration inhibitor.

GS-9160 is a novel and potent inhibitor of human immunodeficiency virus type 1 (HIV-1) integrase (IN) that specifically targets the process of strand transfer. It is an authentic inhibitor of HIV-1 integration, since treatment of infected cells results in an elevation of two-long terminal repeat circles and a decrease of integration junctions.

BMIM-TFSI (compound8) is an HIV-1 integrase inhibitor that effectively suppresses both the 3'-processing (3'-P) and strand transfer (ST) steps of the integration process. It is applicable in HIV-1 research.

VPM peptide functions as a protease-cleavable dithiol cross-linker. It is capable of integration into the PEG-diacrylate (PEG-DA) macromer backbone, resulting in the formation of PEG hydrogel.

N3-PEG3-vc-PAB-MMAE, a drug-linker conjugate designed for Antibody-Drug Conjugates (ADC), features the integration of monomethyl auristatin E (MMAE), a tubulin inhibitor, via a 3-unit polyethylene glycol (PEG) linker. This compound demonstrates significant antitumor activity.

CCT036477 is a selective inhibitor of wingless-type MMTV integration site family dependent transcription. CCT036477reduces the transcriptional activity of the T-cell factor and lymphoid enhancer factor transcription factor family at the ß-catenin level.

Mitoguazone (Methyl-GAG) is a selective S-adenosyl-methionine decarboxylase inhibitor that penetrates the blood-brain barrier and disrupts polyamine biosynthesis. Mitoguazone is a synthetic polycarbonyl derivative with anti-tumor activity that inhibits the integration of HIV DNA into cellular DNA in monocytes and macrophages, inducing apoptosis. Mitoguazone can be used to prevent acute leukemia, Hodgkin lymphoma and non-Hodgkin lymphoma.

GS-9822 is a novel LEDGIN, an inhibitor that targets the binding pocket of LEDGF p75 which is a cellular cofactor that substantially contributes to HIV integration site selection, displaying a block-and-lock phenotype in cell culture.

Hyaluronic Acid Methacryloyl (HAMA) with a molecular weight of 150 kDa is a biocompatible methacrylated derivative of hyaluronic acid. HAMA is utilized as an ink for 3D printing hydrogels, exhibiting rapid photoreactive responses, quick gelation speeds, and stable hydrogel properties. Under ultraviolet light exposure, HAMA efficiently induces gelation in conjunction with phenyl-2,4,6-trimethylbenzoylphosphinate (LAP). The integration of HAMA with tissue-specific extracellular matrix (ECM) materials, such as pancreatic ECM (pECM), is poised to become a vital source material for organ-like tissue cultivation.

PolQi2 is a Polθ inhibitor that suppresses the helicase activity of Polθ. It can be combined with AZD7648 to enhance HDR-mediated integration and editing accuracy.