Metabolism

DHODH-IN-22: potent, selective DHODH inhibitor, orally active, IC50: 0.3 nM, for AML research.

LNP Lipid-8 (11-A-M), an ionizable lipid, is utilized in lipid nanoparticles (LNP) for siRNA delivery to T cells without ligand targeting. When loaded with GFP siRNA (siGFP), it significantly silences the GFP gene in a mouse model [1].

SH-BC-893: Oral anti-cancer sphingolipid analog, prevents ceramide-related mitochondrial issues, and tackles diet-related obesity.

CJ-463, a selective uPA blocker, shows strong anti-tumor effect, especially at 100mg/kg, potentially treating lung cancer.

DPM-1001 trihydrochloride: Potent PTP1B inhibitor, IC50 100 nM, oral, non-competitive, anti-diabetic.

α-Glucosidase-IN-11 is a highly permeable competitive inhibitor of α-glucosidase (IC50: 0.56 μM).

Bemfivastatin hemicalcium (PPD 10558), an orally active HMG-CoA reductase inhibitor, serves as a lipid-lowering agent.

M5N36: selective Cdc25C inhibitor, IC50: 0.15µM A, 0.19µM B, 0.06µM C; halts cell growth, boosts p-CDK1/2.

ATX inhibitor 15, an indole-based carbamate, has a 2.17 nM IC50 against ATX, suppresses pro-fibrotic genes, and protects against mouse lung fibrosis.

Lithium benzoate, an aromatic alcohol present in numerous plants, commonly serves as an additive in food, beverages, cosmetics, and various other products. This compound exhibits antibacterial and antifungal properties, functioning effectively as a preservative [1].

Hypusine is an N-terminal amino alcohol derivative of Lys occurring in bovine brain &

VT-1598 tosylate is a selective, orally active antifungal compound that targets CYP51. It demonstrates efficacy against C. auris.

5α-Androst-16-en-3-one, a mammalian pheromone present in boar saliva, plays a crucial role in facilitating social and sexual interactions by acting as a volatile chemical cue. It is utilized to prime sows in estrus for mating or artificial insemination, underscoring its significance in reproductive behavior. Additionally, this compound is detected in human sweat and urine, where it is involved in studies concerning receptor-mediated odorant detection and the genetic foundations of anosmias, thereby broadening its scope of relevance beyond the animal kingdom.

CP-113818 is a potent inhibitor of cholesterol acyltransferase (ACAT) and can be used to study Alzheimer's disease.

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

5,6-dehydro Arachidonic acid, an arachidonic acid analog with a 5,6 acetylene, inhibits 5-LO; Ki=15 μM in RBL cells, IC50=10 μM in guinea pig leukocytes.

Dasatinib analog-1 (compound 5826) demonstrates inhibition of CYP3A4 activity, presenting a K_i value of 5.4 μM, and effectively prevents the formation of glutathione adducts [1].

IDH1 Inhibitor 7 is an IDH1 inhibitor with an IC 50 of less than 100 nM .

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.

ICMT-IN-22 (compound 62) acts as an ICMT inhibitor with an IC50 value of 0.63 μM [1].