Metabolism

ICMT-IN-24 (compound 63) is an inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), exhibiting potent activity with an IC50 value of 0.19 μM [1].

Cholesterol 24-hydroxylase-IN-2 is a potent inhibitor of cholesterol 24-hydroxylase (CH24H or CYP46A1), exhibiting an IC50 value of 5.4 nM, and has potential

G43-C3-TEG is a glycosyl-transferase inhibitor that diminishes biofilm formation by inhibiting the synthesis of extracellular polysaccharides (EPS) [1].

Anticancer agent 122, a potent inhibitor of human lactate dehydrogenase A (h LDHA), exhibits significant anticancer activities, rendering it suitable for use in

RORγt agonist 2 is a potent agonist of RORγt.

SREBP/SCAP-IN-2 (compound 13) acts as a selective inhibitor of SREBP/SCAP [1].

4-epiMinocycline, recognized as a primary degradation product and a probable impurity in minocycline commercial formulations, is derived from minocycline, a broad-spectrum tetracycline antibiotic notable for its extended serum half-life. Besides treating acne, especially in older patients, minocylvania exhibits significant anti-inflammatory and neuroprotective effects.

5α-Androstan-3β-ol, a steroidal androgen, demonstrates selective interaction with cellular components, showing affinity for the androgen receptor (AR) with an IC50 of 1.7 µM and activating the pregnane X receptor (PXR) in HepG2 cells with an EC50 of 0.8 µM. It selectively inhibits the hydroxylase activities of 16α- and 6β-hydroxylase over 16β- or 7α-hydroxylase, with IC50 values of 70 and 110 µM, compared to >150 µM for the latter enzymes, indicating a specificity in its enzyme inhibition profile. Additionally, administration of this compound at a dosage of 30 mg/kg results in a decrease in testis weight and sperm production in mice, highlighting its biological effects on male reproductive parameters.

Branched fatty acid esters of hydroxy fatty acids (FAHFAs) have emerged as significant regulators of metabolic processes, influenced by dietary changes such as fasting and high-fat diets, and are linked to improved insulin sensitivity in mice. These compounds typically feature a fatty acid chain, either C-16 or C-18 in length (for example, palmitoleic, palmitic, oleic, or stearic acid), esterified to a hydroxy fatty acid of similar length. A specific FAHFA, 12-POHSA, involves the esterification of palmitoleic acid to the 12th carbon of stearic acid. Notably, 12-POHSA levels are markedly higher in the serum of AG4OX mice, which exhibit enhanced glucose tolerance due to overexpression of the Glut4 glucose transporter in adipose tissue. Given the capacity of FAHFAs to enhance glucose tolerance, stimulate insulin secretion, and exert anti-inflammatory actions, 12-POHSA holds potential as a bioactive lipid implicated in managing metabolic syndrome and inflammation.

C24:1 1-Deoxyceramide (m18:1/24:1(15Z)) is a lipid molecule that can be used in life science related research. The CAS number of C24:1 1-Deoxyceramide (m18:1/24:1(15Z)) is 1246298-58-7.

TAS2R14 agonist is a potent partial agonist of TAS2R14, displaying an EC50 value of 116.6 ± 23.6 nM [1].

S07-1066, an aldo-keto reductase 1C3 (AKR1C3) inhibitor, enhances doxorubicin (DOX) cytotoxicity by selectively inhibiting AKR1C3-mediated reduction of DOX and

ICMT-IN-44 (compound 23) serves as an ICMT inhibitor with an IC50 value of 0.167 μM [1].

ICMT-IN-41 (compound 20) serves as a potent inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), demonstrating an IC50 value of 0.069 μM [1].

1-O-Hexadecyl-2-arachidonoyl-sn-glycero-3-PC undergoes acylation through the action of CoA-independent transacylase, transforming lyso-PAF C-16 into this compound. It serves as the predominant precursor in the biosynthesis of PAF C-16 via the remodeling pathway.

5-PAHSA, a FAHFA formed through the formal condensation of the carboxy group of palmitic acid with the hydroxy group of 5-hydroxystearic acid, serves as a human metabolite, possesses anti-inflammatory and hypoglycemic properties, and is categorized as a long-chain fatty acid. This compound, deriving from hexadecanoic acid and octadecanoic acid, is the conjugate acid of a 5-PAHSA(1-).

Diflumidone sodium is a non-steroidal agent with anti-inflammatory activity.

Aladotrilat is an inhibitor of neutral endopeptidase. Its prodrug is aladrotril.

ICMT-IN-45 (compound 24) serves as an ICMT inhibitor, demonstrating an IC50 value of 0.132 μM [1].

IDH889: Brain-penetrant, mutant-specific IDH1 inhibitor; selective for IDH1 R132* mutations. IC50: 0.02μM (R132H), 0.072μM (R132C), 1.38μM (wild-type).