regenerating

Pentamidine dihydrochloride (MP-601205 dihydrochloride) is an aromatic diamidine agent effective against various microorganisms, including protozoa (Trypanosoma brucei, Leishmania spp., and Babesia spp.) and fungi (Pneumocystis jirovecii). It is a potent and selective inhibitor of protein tyrosine phosphatases and phosphatase of regenerating liver. Pentamidine dihydrochloride inhibits the parasite Leishmania infantum with an IC50 of 2.5 μM.

Costunolide (Costus lactone) has anti-inflammatory and anti-oxidant properties and mediates apoptosis.

Thienopyridone is a potent and selective inhibitor of phosphatase of regenerating liver (PRL) phosphatase [IC50 values of 173 nM for PRL-1, 277 nM for PRL-2, and 128 nM for PRL-3], and induces p130Cas cleavage and apoptosis with anticancer effects.

Y-33075 (Y-39983 free base) is a ROCK inhibitor that lowers intraocular pressure (IOP), increases blood flow to the optic nerve head (ONH), and increases the number of RGCs (retinal ganglion cells) in the body with regenerating axons.

ESI1 is a small molecule inhibitor of epigenetic silencing. This compound induces the formation of nuclear aggregates of the key lipid metabolism regulator SREBP1 2, thereby concentrating transcription co-activators to drive lipid cholesterol biosynthesis. Additionally, ESI1 promotes myelin regeneration in demyelination animal models and facilitates de novo myelination on regenerating CNS axons, reversing age-related cognitive decline.

PRL-3 Inhibitor I (BR-1) is a phosphatase of regenerating liver 3 (PRL-3) inhibitor which blocks the migration and invasion of metastatic cancer cells.

17-phenyl trinor PGE2 ethyl amide is derived from 17-phenyl trinor PGE2, a synthetic analog of PGE2 that acts as an agonist of EP1 and EP3 receptors in mice (Ki = 14 and 3.7 nM, respectively) and EP1, EP3, and EP4 in rats (Ki = 25, 4.3, and 54 nM, respectively). 17-phenyl trinor PGE2 causes contraction of guinea pig ileum at a concentration of 11 μM and is 4.4 times more potent than PGE2 as an antifertility agent in hamsters. Modification of the C-1 carboxyl group to an ethyl amide serves to increase lipid solubility, thereby improving uptake into tissues and further lowering the effective concentration. Ethyl amide groups are then removed by amidases, regenerating the active free acid.

PRL-IN-1 (compound 43), a phosphatase of regenerating liver (PRL) inhibitor, directly targets and binds the PRL1 trimer interface, thereby inhibiting PRL1 trimerization. This compound demonstrates potent anticancer activities [1].

Ursolic aldehyde can inhibit phosphatase of regenerating liver-3, with the IC(50) value of 50 +/- 0.3 mu M.