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.

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

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.

AP-C1 is a potent inhibitor of cGMP-dependent protein kinase II (cGKII), exhibiting a pIC50 value of 6.5, but only weakly inhibits cGKII-dependent anion secretion [1].

AP-18 is a potent and selective TRPA1 inhibitor. AP-18 inhibits activation of TRPA1 induced by 50 μM Cinnamaldehyde with an IC50 of 3.1 μM and 4.5 μM for human and mouse TRPA1, respectively. AP-18 could reverse complete Freund's adjuvant (CFA)-induced mechanical hyperalgesia in mice. AP-18 could attenuate Yo-Pro uptake induced by 30 μM AITC in a concentration-dependent manner (IC50= 10.3 μM).

KCa2 (small conductance Ca2+-activated potassium) channel negative allosteric modulator (IC50 = 1.1 μM). Increases the EC50 of Ca2+ on KCa2.3 channels by ~3-fold. Prolongs atrial effective refractory period (AERP) in rats. Reduces atrial fibrillation (AF) duration and prolongs atrial refractoriness without affecting ventricular refractory period in an animal AF model. Diness et al (2017) Termination of vernakalant-resistant atrial fibrillation by inhibition of small-conductance Ca2+-activated K+ channels in pigs. Circ.Arrhythm.Electrophysiol. 10 e005125 PMID:29018164 |Simó-Vicens et al (2017) A new negative allosteric modulator, AP14145, for the study of small conductance calcium-activated potassium (KCa2) channels. Br.J.Pharmacol. 174 4396 PMID:28925012

Tat-Gap 19, a peptide inhibitor of connexin43 (Cx43) hemichannels, is derived from the HIV-1 Tat protein transduction domain fused with a nine-amino acid sequence from Cx43 residues 128-136. This compound, at a concentration of 10 µM, effectively suppresses glutamate-induced ATP release in primary rat hepatocytes, indicating inhibition of Cx43 hemichannel activity. Furthermore, Tat-Gap 19 demonstrates therapeutic potential by significantly reducing infarct volume in a mouse cerebral ischemia-reperfusion injury model following middle cerebral artery occlusion (MCAO) at a dosage of 25 mg/kg. Moreover, its intraperitoneal administration at 1 mg/kg per day ameliorates fibrosis and decreases the area of hepatic stellate cells, the precursors to myofibroblasts, expressing α-smooth muscle actin (α-SMA), in a model of thioacetamide-induced liver damage. Additionally, it enhances superoxide dismutase (SOD) activity in hepatic cells from the treated mice, indicating its antioxidative benefits.

SAAP 148, an antimicrobial peptide, effectively combats various multidrug-resistant bacteria in vitro and, in vivo, reduces skin colony-forming units (CFUs) in mouse models of A. baumannii or methicillin-resistant S. aureus (MRSA) infections at concentrations ranging from 0.125-2% w/w.

PACAP 1-38 acetate is a pituitary adenylate cyclase activating polypeptide (PACAP) analogue. PACAP 1-38 acetate binds to PACAP type I receptor(IC50 = 4 nM) and PACAP type II VIP2 receptor(IC50 = 1 nM) but not to PACAP type II, VIP1 receptor.

SAAP 148 is an antimicrobial and antibiofilm agent that demonstrates inhibitory activity against antibiotic-resistant pathogens, with an LC50 of 0.8-12.8 μM.

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.

15(S)-HpETE is a product of arachidonic acid formed in the 15-lipoxygenase pathway and inhibits angiogenesis. 15(S)-HpETE can upregulate the expression of CD31, E-selectin, and gene selectin in cells.

T-5224 is a transcription factor c-Fos/AP-1 inhibitor that specifically inhibits the DNA-binding activity of c-Fos/c-Jun without affecting other transcription factors.

E3330 is a potent and selective APE1(Ref-1) inhibitor, which suppressed NF-kappa B DNA-binding activity.

IMM-H007 is a novel lipid-lowering agent, increasing abca1 protein expression

Dehydroglyasperin D exhibits anticancer, anti-inflammatory, anti-obesity, antioxidant and anti-aldose reductase effects, it inhibits the proliferation of HT-29 human colorectal cancer cells through direct interaction with phosphatidylinositol 3-kinase; it also mediates suppression of both COX-2 expression and the MLK3 signalling pathway through direct binding and inhibition of MLK3. Dehydroglyasperin D shows strong ferric reducing activities and effectively scavenged DPPH, ABTS(+), and singlet oxygen radicals.

Kukoamine A possesses anticancer, cytoprotective, antioxidant, and anti-inflammatory activities, it also has neuroprotective effects through inhibiting oxidative stress and apoptosis after whole-brain irradiation (WBI) in rats.

3-O-Methylgallic acid (3,4-Dihydroxy-5-methoxybenzoic acid) reduces cell proliferation in Caco-2 cells (IC50 = 24.1 μM) more effectively than anthocyanins and may offer protection against colon cancer after its formation in the gut. It inhibits transcription factors NF-κB, AP-1, STAT-1, and OCT-1, which are known to be activated in colorectal cancer.