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) 是一种可透过血脑屏障的选择性的 S-腺苷-蛋氨酸脱羧酶 (S-adenosyl-methionine decarboxylase) 抑制剂,可破坏多胺的生物合成。Mitoguazone 是一种具有抗肿瘤活性的合成多羰基衍生物,可抑制 HIV DNA 整合到单核细胞和巨噬细胞中的细胞 DNA 中,诱导细胞凋亡 (apoptosis)。Mitoguazone 具可用于预防急性白血病,霍奇金淋巴瘤和非霍奇金淋巴瘤。
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.
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.
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.
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.