TLR7 8 agonist 4 hydroxy-PEG10-acid hydrochloride (compound 9) is a drug-linker conjugate used in antibody-drug conjugates (ADCs) with high efficacy against tumors. It consists of TLR7 8 agonist 4, a potent TLR7 8 agonist, linked to the ADC linker hydroxy-PEG10-acid which can be cleaved.
TMB 8 is a non-competitive antagonist of nicotinic acetylcholine receptors (nAChRs) with IC50 values of 390 and 350 nM, respectively, for human muscle-type and α3β4 subunit-containing ganglionic nAChRs expressed in TE671 RD or SH-SY5Y cells. It inhibits nicotine-induced dopamine release from rat brain synaptosomes (IC50 = 480 nM). TMB 8 also reduces calcium availability in smooth and skeletal muscle, blocking the contractile response in isolated rabbit aortic strip when used at a concentration of 50 μM and inhibiting calcium influx and efflux in isolated guinea pig ileum when used at a concentration of 65 μM. It has been used in the study of intracellular calcium dynamics, particularly in smooth muscle. TMB 8 also inhibits protein kinase C (PKC) activity in a dose-dependent manner.
8-Hydroxyguanine, generated through the oxidative degradation of DNA by the hydroxyl radical, serves as an indicator of oxidative stress in biological systems.
Two Rho-associated kinases (ROCK), ROCK-I and ROCK-II, act downstream of the G protein Rho to regulate cytoskeletal stability. The ROCKs play important roles in diverse cellular functions including cell adhesion and proliferation, smooth muscle contraction, and stem cell renewal. Glycyl-H-1152 is a selective and potent ROCK inhibitor (IC50 = 11.8 nM for ROCK-II). It is a glycylated isoquinoline compound derived from the therapeutically-important ROCK inhibitor HA-1077 (Fasudil) and exhibits better specificity. Thus, it poorly inhibits Ca2+/calmodulin-dependent kinase type II, protein kinase (PK) G, and Aurora A (IC50 = 2.57, 2.35, and 3.26 μM, respectively) as well as PKA or PKC (IC50 ≥ 10 μM for each). The potency of Glycyl-H-1152 is superior to that of other ROCK inhibitors, including Y-27632 (Ki = 220 nM) and HA-1077 (IC50 = 158 nM).
H-D-Phe-Pip-Arg-pNA hydrochloride, a chromogenic substrate, mimics the N-terminal segment of the A alpha chain of fibrinogen, the native substrate of thrombin. It displays specificity towards thrombin and is employed for quantifying antithrombin-heparin cofactor (AT-III). The utilization of H-D-Phe-Pip-Arg-pNA hydrochloride in the AT-III assay enables a sensitive, accurate, and straightforward measurement process.
GNE-617 hydrochloride is a potent and competitive inhibitor of nicotinamide phosphoribosyltransferase (IC50: 5nM). GNE-617 hydrochloride reduces the NAD levels in a > 95% reduction in both NAPRT1-deficient and NAPRT1-proficient cell lines and exerts (EC50
Taltobulin hydrochloride is a synthetic analogue of the tripeptide hemiasterlin, is a potent agent of antimicrotubule that circumvents P-glycoprotein-mediated resistance in vitro and in vivo.