ap-1

AP-1/NF-κB activation inhibitor 1 is a potent inhibitor of AP-1 and NF-κB mediated transcriptional activation (IC50 = 1 μM), without blocking basal transcription driven by the β-actin promoter. It has a similar inhibitory effect on the production of IL-2 and IL-8 levels in stimulated cells [1].

AP-1, a miniaturized proteolysis-targeting chimera (PROTAC) incorporating an anaplastic lymphoma kinase (ALK) ligand connected to (±)-thalidomide via an ultrashort linker, effectively degrades ALK fusion proteins such as NPM-ALK in Karpas-299 cells and EML4-ALK and ALKF1174L in SN-N-SH and NCI H3122 cells, respectively. Concentrations ranging from 10 to 300 nM are sufficient for its action, which is hindered by the proteasome inhibitor MG-132. Demonstrating selectivity, AP-1 exhibits cytotoxicity towards ALK-dependent Karpas-299 cells with an IC50 value of 0.1265 nM, while showing significantly less toxicity to non-ALK-dependent THP-1 cells (IC50 = 2,704 nM). Furthermore, it effectively reduces tumor volume in NCI H3122 mouse xenograft models at doses of 25, 50, and 100 mg/kg.

NFAT:AP-1 inhibitor-10 is a novel inhibitor of the NFAT:AP-1:DNA interaction on the ARRE-2 element, binding to DNA in a sequence-selective manner and inhibiting the transcription of the Il2 gene and several other cyclosporin A-sensitive cytokine genes important for the effector immune response.

AcrAP1 (AP1-Z1) is an antimicrobial peptide found in the venom of the Arabian scorpion (Androctonus crassicauda). It exhibits antibacterial properties, effectively inhibiting the growth of both Gram-positive and Gram-negative bacteria, as well as yeasts. AcrAP1 also displays antitumor activity by promoting apoptosis in cancer cells and inhibiting angiogenesis, making it a potential candidate for cancer treatment research.

Ortho-methyl 4-AP-1-ethyl Carbamate is used as a precursor for the synthesis of ortho-methylfentanyl.

TRAP-1 (XJZ-06-462) is a p53 transcription activator that effectively activates mutant p53 and triggers the transcription of p53 target genes. In the p53Y220C pancreatic cell line, TRAP-1 rapidly upregulates p21 and other p53 target genes. TRAP-1 also inhibits cell proliferation, exhibiting IC50 values of 3.94 μM and 0.531 μM in BxPC-3 and A549 cell lines, respectively. Additionally, TRAP-1 modulates autophagy in lung cancer cells and provides protection against oxidative stress and apoptosis.

VAP-1-IN-3 (compound 136) is a potent inhibitor of amine oxidase vascular adhesion protein-1 (VAP-1), demonstrating an IC50 value of 0.13 μM against VAP-1 isolated from bovine plasma. It is applicable for inflammation research.

nociceptin/orphanin FQ (NOP) receptor antagonist

AP-102 is a bioactive chemical.

NAP-1 is a compound with anesthetic activity.1 It increases paired-pulse inhibition in the CA1 region of rat hippocampal brain slices when used at a concentration of 100 μM. NAP-1 also induces loss of righting reflex in tadpoles (EC50 = 0.53 μM).References NAP-1 is a compound with anesthetic activity.1 It increases paired-pulse inhibition in the CA1 region of rat hippocampal brain slices when used at a concentration of 100 μM. NAP-1 also induces loss of righting reflex in tadpoles (EC50 = 0.53 μM). References

SSAO/VAP-1 Inhibitor 1 is a potent compound aimed at inhibiting SSAO/VAP-1, a protein involved in facilitating the translocation of Glucose Transport 4 (GLUT 4) to the cell membrane in adipocytes, thus playing a crucial role in glucose regulation. Additionally, in endothelial cells, this enzyme is responsible for mediating the adherence and infiltration of leukocytes, contributing to inflammatory responses. Given these mechanisms, SSAO/VAP-1 Inhibitor 1 holds considerable potential for research into treatments for inflammation, inflammation-related conditions, diabetes, and diabetes-associated diseases[1].

CAP-1 is an inhibitor of HIV-1 capsid formation.

BMAP-18 is a biologically active peptide, a truncated derivative of BMAP-27, which is part of the Cathelicidin family of peptides known for their potent bactericidal properties against pathogens such as Staphylococcus aureus, Streptococcus uberis, and Escherichia coli. Unlike the full-length BMAP-27, which can be cytotoxic to human erythrocytes and neutrophils at concentrations higher than required for its antimicrobial effect, BMAP-18 offers increased cell selectivity due to its reduced hemolytic activity while maintaining effective antimicrobial function.

SMAP-18, an 18-amino acid residue peptide amide, is a biologically active truncated variant of Sheep myeloid antimicrobial peptide-29 (SMAP-29). It retains potent antimicrobial activity against Pseudomonas strains, other Gram-negative bacteria, and multidrug-resistant pathogens. Notably, SMAP-18 exhibits increased cell selectivity relative to the parent peptide SMAP-29 due to its reduced hemolytic activity while maintaining its antimicrobial efficacy.

HAP-1, a synovial-targeted transduction peptide, selectively mediates the internalization of protein complexes into synovial cells of human and rabbit origin. When fused with the antimicrobial peptide (KLAK)2, HAP-1 forms the proapoptotic peptide DP2 [1].

ZAP-180013 is an inhibitor of zeta-chain-associated protein kinase 70 (ZAP70,IC50 : 1.8 μM).

CAP-100 is a monoclonal antibody targeting CCR7. It neutralizes the ligand binding site and signaling of CCR7. This compound effectively inhibits migration, extravasation, homing, and survival in chronic lymphocytic leukemia (CLL) samples induced by CCR7. CAP-100 can mediate potent tumor cell killing through host immune mechanisms and exhibits favorable toxicity profiles in related hematopoietic cell subsets. It is involved in research on antitumor activity and diseases like chronic lymphocytic leukemia (CLL).

TRAP-14 amide is a protease-activated receptor (PAR) activating peptide and acts as a PAR agonist, with an EC50 of 24 μM. It induces significant platelet aggregation via ADP and MMP-2 dependent pathways and is insensitive to Aspirin. Additionally, TRAP-14 amide effectively increases the surface expression of glycoprotein (GP) Ib and GPIIb/IIIa, as well as the release of ADP.

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

INI-43, an inhibitor of Nuclear Import-43, shows a significant cytotoxic effect on various cervical and oesophageal cancer cell lines by targeting Kpnβ1 and interferes with the nuclear localization of Kpnβ1 and known Kpnβ1 cargoes, NFAT, NFκB, AP-1 and NF

Farudodstat (ASLAN003) is an orally active and potent inhibitor of DHODH (Human Dihydroorotate Dehydrogenase) with antitumor activity, showing potential as a first-in-class candidate in AML [Acute Myeloid Leukemia].

Vaginatin, a compound isolated from Laserpitium zernyi, has anticancer activity, inhibits AP-1 pro-inflammatory factor, and can be used in cancer research.10 FTHF disodium (10) has been shown to be effective in the study of cancer.

SR 11302 is an inhibitor of activator protein-1 (AP-1).

SL327 is a selective inhibitor for MEK1/2 with IC50 of 0.18 μM/0.22 μM; able to transport through the blood-brain barrier.