Metabolism

PHD-IN-1 (compound 80) serves as a potent PHD2 inhibitor, exhibiting an IC50 value of ≤5 nM.

1-Isopropyltryptophan (1-IsoPT), an IDO1 inhibitor, suppresses the expression of IDO-1 and IDO-2 mRNA induced by IFN-γ stimulation [1].

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

BMS-986172 is an orally active, highly selective inhibitor of MGAT2, demonstrating inhibitory concentrations (IC50) of 4.6 nM for human MGAT2 (hMGAT2) and 20 nM

VU0364739, a selective phospholipase D2 (PLD2) inhibitor with an IC50 of 22 nM, effectively reduces cancer cell proliferation [1].

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

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

hCAIX-IN-16 (Compound 12d), an inhibitor of hCA IX, exhibits inhibition constants (K i) of 190.0 nM for hCA IX and 187.9 nM for hCA XII.

KD-026 (SLx 4090), a microsomal triglyceride transfer protein (MTP) inhibitor(IC50 = 8.0 nM), is used in type 2 diabetes studies.

Perindopril acyl-β-D-glucuronide is a metabolite of the ACE inhibitor perindopril [1].

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

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

Glycosidase-IN-2 is a glycosidase inhibitor with hypoglycemic activity.

GSK-8062 is an agonist of farnesoid X receptor (FXR).

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

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

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.

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