Metabolism

H2-003 is a selective inhibitor of diacylglycerol acyltransferase 2 (DGAT2).

Pactimibe sulfate is a dual ACAT1/2 inhibitor with anti-atherogenic potential, reducing plasma cholesterol.

GPX4-IN-2 is a potent inhibitor of GPX4, exhibiting antiproliferative activity. It holds potential for cancer research applications.

4BAB (compound 29) is an irreversible inhibitor of glyoxalase I (GLO1) and exhibits anticancer activity.

11β-13,14-Dihydro-15-keto PGF2α, a PGD2 metabolite in the 15-hydroxy PGDH pathway, is formed in human males upon infusion or inhalation of tritiated PGD2, with peak plasma levels of both 11β-PGF2α and 11β-13,14-dihydro-15-keto PGF2α observed within 10 minutes. In human lung homogenates, PGD2 is metabolized firstly to 11β-PGF2α and subsequently to 11β-15-keto-PGF2α in the presence of NAD+, but not to 11β-13,14-dihydro-15-keto PGF2α. Conversely, guinea pig liver and kidney homogenates can metabolize PGD2 to 11β-13,14-dihydro-15-keto PGF2α via 11β-PGF2α, with both NAD+ and NADP+ being requisite for this conversion.

BMS-186511: An FT inhibitor targeting malignant cells in NF1, halting growth and spread without affecting related enzymes.

B 581 is an inhibitor that specifically blocks farnesylated.

DC271, a retinoid and RAR agonist, mimics the cellular effects of the endogenous ATRA and the synthetic EC23, by binding to retinoid protein machinery such as CRABPII to facilitate the translocation of ATRA into the nucleus [1].

15-beta PGF2α, a biochemical compound, serves as a pivotal mediator in diverse physiological processes.

L791943 is a selective, potent) inhibitor of Phosphodiesterase-4 (PDE4,IC50 of 4.2 nM).

RB 101 suppresses enkephalinase and aminopeptidases; biologically cleaved at disulfide to produce inhibitors of both aminopeptidase N and neutral endopeptidase.

CYP3A4-IN-2, a potent CYP3A4 inhibitor (IC50: 0.055 μM), is a hydrophobic ritonavir analog with immunosuppressive and antiviral properties.

cis-ent-Tadalafil (cis-ent-IC-351) is a potent and selective PDE5 inhibitor that lowers blood pressure.

Leukotriene C4 (14,15-LTC4) is an inflammatory mediator synthesized from arachidonic acid through the actions of 15- and 12-lipoxygenases (LOs), involving intermediates such as 15-HpETE and 14,15-LTA4. Unlike the majority of leukotrienes formed via the 5-LO pathway, 14,15-LTC4 is an eoxin predominantly produced by eosinophils, although mast cells and nasal polyps can also synthesize it. While its physiological roles are not well understood, 14,15-LTC4 exhibits limited contractile activity on guinea pig ileum and pulmonary parenchyma. However, it can increase vascular permeability in human endothelial cell monolayers in vitro with potency comparable to 5-LO-derived leukotrienes, contributing to plasma leakage characteristic of inflammation.

BMS-262084 is a potent selective β-lactam trypsin inhibitor with therapeutic potential in the treatment of asthma.

Pactimibe is a ACAT inhibitor. It has anti-atherosclerotic activity.

First potent oral dual IDO1/IDO2 inhibitor with antitumor properties; IC50: 28 nM (IDO1), 144 nM (IDO2).

Bemoradan is an inhibitor of the rolipram-insensitive cyclic AMP phosphodiesterase from canine heart tissue

Dieicosanoin is a diacylglycerol that incorporates arachidic acid, a saturated long-chain fatty acid featuring a 20-carbon backbone. This acid is derivable from sources such as peanut butter and anaerobic fungi [1] [2].