Metabolism

MSI-1436 is a selective, non-competitive the enzyme protein-tyrosine phosphatase 1B (PTB1B)inhibitor(IC50 of appr 1 μM)

UK 357903, a phosphodiesterase 5A (PDE5A) inhibitor, is used potentially for the treatment of erectile dysfunction.

5(S)-HETrE, made by 5-LO from mead acid, has unknown biological activity and metabolic fate.

Lp-PLA2-IN-9, a tetracyclic pyrimidinone, inhibits rhLp-PLA2 (pIC50: 10.1), promising for neurodegenerative research.

15-PGDH-IN-2 (Compound 2) is an inhibitor of 15-PGDH with an IC50 value of 0.274 nM. This compound is useful for research into hair loss, bone formation, gastric ulcer healing, and dermal wound healing [1].

1-Stearoyl-2-hydroxy-sn-glycero-3-PG, a lysophospholipid characterized by the presence of stearic acid (18:0) at the sn-1 position, finds application in the creation of micelles, liposomes, and various artificial membranes, including those utilized in lipid-based drug delivery systems.

PDE12-IN-3 is an inhibitor of phosphodiesterase 12 (PDE12) (pXC50 of 7.68),with antiviral activity.

DGAT1-IN-1 is a potent inhibitor of diacylglycerol O- acyltransferase type 1(DGAT1, IC50 of < 10 nM).

Efipladib is a phospholipase inhibitor. Efipladib decreases nociceptive responses without affecting PGE2 levels in the cerebral spinal fluid.

Fatty acid amide hydrolase (FAAH), an enzyme responsible for the hydrolysis and inactivation of fatty acid amides like anandamide and oleamide, has been identified as a target by the potent FAAH inhibitor PHOP. PHOP demonstrates remarkable inhibitory activity with K_i values as low as 0.094 nM for human FAAH and 0.2 nM for rat FAAH. Additionally, through a proteomics assay focusing on the serine hydrolase enzyme family, to which FAAH belongs, PHOP's selectivity was evaluated, presenting IC_50 values of 1.1 nM against FAAH, 1.4 nM against triacylglycerol hydrolase (TGH), and greater than 100 µM against an uncharacterized hydrolase (KIAA1363). This specificity profile of PHOP underscores its potential for yielding precise outcomes in studies involving complex biological systems.

Ilepatril, also known as AVE-7688, is a vasopeptidase inhibitor for the treatment of hypertension.

Me-Indoxam is an inhibitor of sPLA2. It has no effect on arachidonic acid release and platelet activating factor synthesis.

CAY10502 inhibits cPLA2α (85 kDa), crucial in inflammation/arachidonic cascade, with 4.3 nM IC50, reducing arachidonic acid in human platelets.

Prostaglandin B2 is a dehydration product of PGE2/PGA2 with weak TP receptor activity, raising rabbit pulmonary pressure at >5 ug/kg.

CETP-IN-3 is an inhibitor of the plasma glycoprotein cholesterol ester transfer protein (CETP), elevating HDL-C through inhibition of CETP.

NC1 is a potent allosteric inhibitor of lymphoid-specific PTPN22, a protein tyrosine phosphatase.

Nampt-IN-10 TFA, a NAMPT inhibitor, shows potency in A2780 (IC50: 5 nM) and CORL23 (IC50: 19 nM), suitable for ADC payloads.

TMP778 is an effective and selective RORγt inverse agonist (IC50: 7 nM in FRET assay).

ICMT-IN-1 (compound 75) is a potent ICMT inhibitor with an IC50 value of 0.0013 μM.

Tetrahydro-11-dehydrocorticosterone is an inhibitor of 11β-hydroxysteroid dehydrogenase [1].