pap 1

PAP-1 (5-(4-Phenoxybutoxy)psoralen) is a selective, orally active Kv1.3 blocker with an EC50 of 2 nM.

PAP-IN-1 (compound 28) is a binuclear metallohydrolase inhibitor specific to purple acid phosphatases (PAPs), with a Ki value of 168 nM against mammalian PAP and a Kic value of 0.17 μM targeting porcine PAP. This compound plays a significant role in anti-osteoporotic drug development research [1].

Pap12-6, an antibacterial peptide originating from the first twelve N-terminal amino acids of papiliocin found in P. xuthus larvae, exhibits activity against a range of eight Gram-negative bacteria (e.g., E. coli, P. aeruginosa, S. syphimurium with MIC50s=4-8 µM) and Gram-positive bacteria (e.g., S. aureus, methicillin-resistant S. aureus 3126, B. subtilis, and S. epidermidis with MIC50s=4-8 µM), without compromising the viability of human erythrocytes, mouse RAW 264.7 macrophages, human HaCaT keratinocytes, or human HEK293 kidney cells at 25 µM. It causes membrane depolarization in E. coli at 4 and 8 µM and, upon preincubation at 10 µM, decreases nitrite (NO2-), Tnf-α, and Il-6 secretion in LPS-stimulated RAW 264.7 macrophages. In a murine model, Pap12-6 enhances survival rates and diminishes colony forming units (CFUs) in several organs upon E. coli infection at 10 mg/kg and 1 mg/kg doses, respectively. Additionally, at a 1 mg/kg dose, it lowers serum aspartate aminotransferase (AST) and alanine transaminase (ALT) levels, as well as blood urea nitrogen levels in E. coli-induced sepsis, indicating its therapeutic potential for bacterial infections without affecting host cell viability.

Pap12-6 is a 12-peptide derived from the antimicrobial peptide Papiliocin, which originates from the larvae of the yellow-patterned butterfly. It exhibits potent antibacterial activity by penetrating and disrupting bacterial membranes. Additionally, Pap12-6 exerts anti-inflammatory effects through the TLR4-mediated NF-κB signaling pathway.

SARS-CoV-2 RdRp-IN-1 (Compound PAP-2) is a potent inhibitor of SARS-CoV-2 RdRp with an EC50 value of 1.11 μM. This compound interacts directly with SARS-CoV-2 RdRp, effectively resisting exonuclease (ExoN) activity, and demonstrates broad-spectrum antiviral activity against coronaviruses.

Compound 35 (PAP-IN-2) is a purple acid phosphatase (PAP) inhibitor with an inhibition constant (Ki) of 186 nM, potentially useful in the development of anti-osteoporotic compounds [1].