magnitude

Venetoclax (ABT-199) is a Bcl-2 inhibitor (Ki<0.01 nM) with potent, selective, and orally active properties. Venetoclax has a 3-order-of-magnitude lower affinity for Bcl-xL and Bcl-W (Kis=48 245 nM). Venetoclax induces autophagy and apoptosis.

γ-Hexalactone (γ-caprolactone) belongs to the class of organic compounds known as gamma butyrolactones. Gamma butyrolactones are compounds containing a gamma butyrolactone moiety, which consists of an aliphatic five-member ring with four carbon atoms, one oxygen atom, and bears a ketone group on the carbon adjacent to the oxygen atom. Thus, Gamma-caprolactone is considered to be a fatty ester lipid molecule. Gamma-Caprolactone is a very hydrophobic molecule, practically insoluble (in water), and relatively neutral. Gamma-Caprolactone exists in all eukaryotes, ranging from yeast to humans. Outside of the human body, Gamma-caprolactone has been detected, but not quantified in, several different foods, such as potato, cereals and cereal products, pomes, alcoholic beverages, and fruits. This could make Gamma-caprolactone a potential biomarker for the consumption of these foods. 4-hydroxy-Hexanoic acid gamma-lactone is occasionally found as a volatile component of human urine. In some cases differences up to an order of magnitude are observed. 4-hydroxy-Hexanoic acid gamma-lactone has been found in the polar fraction of human blood. Biological fluids such as blood and urine have been shown to contain a large number of components, some of them volatiles (low boiling point) apparently present in all individuals, while others such are much more variable. Although some of these changes may have dietary origins, others seem to be characteristic of the individual.

MRS-1706 has Ki values of 1.39, 112, 157, and 230 nM for human A2B, A2A, A1, and A3 receptors respectively. MRS-1706 is an effective and selective adenosine A2B receptor inverse agonist.

N-acetyl Leukotriene E4 is an endogenous metabolite of Leukotriene E4, which is excreted mainly through bile, and is one to three orders of magnitude less active than Leukotriene E4, causing constriction of the airways.

1. Tiliroside (Tribuloside) shows anticarcinogenic activity. 2. Tiliroside shows hepatoprotective activity. 3. Tiliroside shows antioxidant and anti-inflammatory activity, can inhibit neuroinflammation in neurodegenerative disorders. 4. Tiliroside has anti-diabetic effect, are at least partially mediated through inhibitory effects on carbohydrate digestion and glucose uptake in the gastrointestinal tract. 5. Tiliroside and gnaphaliin are antioxidants against in vitro Cu(2+)-induced LDL oxidation in the same order of magnitude compared to that of the reference drug, probucol. 6. Tiliroside enhances fatty acid oxidation via the enhancement adiponectin signaling associated with the activation of both AMP-activated protein kinase and peroxisome proliferator-activated receptor α and ameliorates obesity-induced metabolic disorders.

PBS-1086 is a novel dual inhibitor of the canonical and noncanonical NF-κB pathways, increasing the magnitude and duration of initial EGFR inhibitor response in multiple NSCLC models, decreasing PDHK1 expression, and suppressing phosphorylation of the PDHK1 protein substrate PDHA1 in a panel of PTEN-deficient cell lines.

Covidcil-19 binds to the revised attenuator hairpin structure of the SARS-CoV-2 frameshifting element (FSE) with high affinity (Kd = 11 nM). It stabilizes the hairpin's folded state and reduces frameshifting efficiency in cells. Covidcil-19 inhibits viral propagation and reduces viral infectivity by > 3.5 orders of magnitude.

Cryptophycin analog 1, an ADC payload, exhibits anticancer activity and demonstrates cellular potency an order of magnitude greater than the approved ADC payloads MMAE and DM1 [1].

Selective NaV1.7 channel blocker. Shifts activation gating positively and decreases current magnitude. Displays 100-fold selectivity over other sodium channel subtypes.

Amyloid A proteins (H2N-Ala-Gly-Leu-Pro-Glu-Lys-Tyr-OH) are a family of apolipoproteins associated with high-density lipoprotein in plasma. Different isoforms of SAA are expressed constitutively at different levels or in response to inflammatory stimuli.