antiprion

TCS PrP Inhibitor 13 (5-(4-Nitrophenyl)-2-Phenyl-4H-Pyrazol-3-One) is an antiprion agent inhibiting protease-resistant prion protein (PrP-res) accumulation.

l-Atabrine dihydrochloride displays antiprion activity. l-Atabrine dihydrochloride is a less active enantiomer of quinacrine.

1-(4-Methoxyphenyl)-3-methyl-1H-pyrazol-5(4H)-one (Compound 2) exhibits antiprion activity in ScN2a and F3 cells, with IC50 values of 13 nM and 25 nM, respectively.

Icerguastat (Sephin1) Carbonate, a Guanabenz derivative lacking α2-adrenergic activity, is a selective inhibitor of the phosphatase regulatory subunit PPP1R15A (R15A). It inhibits the dephosphorylation of eIF2α, thereby prolonging the protective response. Additionally, Icerguastat Carbonate exhibits antiprion activity.

Chloroguanabenz (acetate) is an antiprion agent derived from guanabenz, an α2-adrenergic receptor agonist. It inhibits prion formation in vitro in both yeast and mammalian models. Additionally, Chloroguanabenz (acetate) reduces levels of the truncated huntingtin protein derivative Htt48 in HEK293T cells and is used for studying Huntington's disease.

Radotinib (IY-5511) dihydrochloride is an orally bioavailable and brain-penetrant selective tyrosine kinase Bcr-Abl1 inhibitor with an IC50 of 34 nM. It exhibits antiprion and antitumor activities by inhibiting tumor cell proliferation, inducing cell cycle arrest, and triggering apoptosis. Radotinib dihydrochloride is applicable in research on chronic myeloid leukemia, multiple myeloma, other tumors, and prion-related neurodegenerative diseases.

IND81 is an antiprion agent that works by extending the lives of prion-infected animals.

IND45193, an antiprion agent, acts by reducing PrP(Sc) levels in dividing and stationary-phase cells.

Chloroguanabenz is an antiprion agent and a derivative of the α2-adrenergic receptor agonist guanabenz . It inhibits prion formation in yeast and mammalian cell-based assays. Chloroguanabenz reduces the levels of both soluble and aggregated forms of the truncated Huntingtin derivative Htt48 in an HEK293T cellular model of Huntington's disease.

6-Amino-8-trifluoromethylphenanthridine (6A-8tFP) is an antiprion agent and a derivative of 6-aminophenanthridine. It inhibits the protein folding activity of the ribosome (PFAR) at a concentration of 150 μM and directly competes with protein substrates for the ribosomal active site.

6-Aminophenanthridine is an antiprion agent. It inhibits prion formation in yeast- and mammalian-based screening assays when used alone and, to a greater extent, when used in combination with the α2-adrenergic receptor agonist guanabenz . 6-Aminophenanthridine (300 μM) inhibits protein folding activity of the ribosome (PFAR) by directly competing with protein substrates for the active site and decreases the yield of refolded protein without affecting the refolding rate. It prevents progressive wing position defects in a Drosophila model of oculopharyngeal muscular dystrophy (OPMD) when larvae are raised on medium containing doses ranging from 300 to 400 μM and in adults following dietary administration of 1-3 mM doses. 6-Aminophenanthridine also reduces muscle degeneration and decreases the number of nuclear inclusions in thoracic muscle in a Drosophila model of OPMD.

Quinoprazine, a powerful inhibitor of Vaccinia virus DNA synthesis (IC50 = 10 μM), exhibits notable antimalarial activity against Plasmodium berghei. Additionally, it demonstrates significant antiprion potency, effectively reducing levels of PrPSc [1]-[5].

BiCAPPA is a bivalent anti-prion ligand. BiCAPPA reduces the levels of the infectious conformation of prion protein (PrPSc) in cells infected with yaws, with an EC50 value of 0.32 μM.