STh, also known as Escherichia coli heat-stable toxin, is a 19 amino acid polypeptide containing three disulfide bridges. It serves as an antigen of significance in the quest for a comprehensive enterotoxigenic Escherichia coli (ETEC) vaccine.
Closthioamide is a potent inhibitor of bacterial DNA gyrase and highly active against MRSA, Ec, VRE, and Mv (MICs: 0.58 μM, 9.00 μM, 0.58 μM and 72.03 μM).
DBCO-PEG4-Desthiobiotin is a polyethylene glycol (PEG) derivative utilized as a linker for the synthesis of proteolysis-targeting chimeras (PROTACs)[1].
N-Desthiobiotin-N-bis(PEG4-t-butyl ester) is a PEG-based linker compound employed for the synthesis of PROTACs, which are bifunctional molecules designed for targeted protein degradation[1].
Amine-PEG3-Desthiobiotin is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.
Amine-PEG4-Desthiobiotin is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.
Transthyretin-IN-1 (Compound 1d) is a potent inhibitor of transthyretin (TTR) fibril formation, making it a valuable tool for investigating Alzheimer’s disease [1].
Bisthianostat, also known as CF367 or CF367;-C, is a novel Orally Efficacious Pan-HDAC Inhibitor. Bisthianostat selectively binds to and inhibits HDACs, which inhibits deacetylation of histone proteins and leads to the accumulation of highly acetylated histones. This may result in an induction of chromatin remodeling, the inhibition of tumor oncogene transcription, and the selective transcription of tumor suppressor genes. This prevents cell division, induces cell cycle arrest and apoptosis. This may inhibit the proliferation of susceptible tumor cells. HDACs, upregulated in many tumor cell types, are a family of enzymes that deacetylate histone proteins.
Arsthinol is an antiprotozoal agent which may have anti-cancer activity. It was found that arsthinol, a trivalent organoarsenic compound (dithiarsolane), has been active in vitro on leukemia cell lines and offers a better therapeutic index than arsenic trioxide, as estimated by the ratio LD50 IC50. Arsthinol induced growth inhibition of NB4 cells at lower concentration (IC50 (concentration inhibiting growth by 50%) = 0.78 + - 0.08 micromol l after 24 h) than As(2)O(3) (IC50 = 1.60 + - 0.23 micromol l after 24 h) or melarsoprol (IC50 = 1.44 + - 0.08 micromol l after 24 h). Arsthinol-cyclodextrin complex demonstrated to have was more effective than arsenic trioxide (As2O3) and melarsoprol on the U87 MG cell line. Importantly, in the in vivo study, significant antitumor activity against heterotopic xenografts was observed after i.p. administration.