across

Dersimelagon (MT-7117) is an orally active, selective agonist for the melanocortin 1 receptor (MC1R), demonstrating EC50 values of 8.16 nM (h), 3.91 nM (cm), 1.14 nM (m), and 0.251 nM (r) across species such as human, cynomolgus monkey, mouse, and rat, respectively. It exhibits strong affinity for human MC1R and MC4R, with Ki values of 2.26 nM and 32.9 nM, respectively. This compound is applied in the study of skin pigmentation.

Ionomycin is an calcium ionophore and an antibiotic that binds calcium ions (Ca2+). It is produced by the bacterium Streptomyces conglobatus.It is used in research to raise the intracellular calcium level (Ca2+) and as a research tool to understand Ca2+ transport across biological membranes. Ionomycin promotes apoptosis and induces the activation of protein kinase C (PKC).

λ-Cyhalothrin (Icon) is a type II synthetic pyrethroid insecticide featuring a high-efficiency, broad-spectrum formula with an α-cyano group. It is employed across various applications for controlling a wide array of pests. As a neurotoxin, λ-Cyhalothrin acts on sodium channels in neuron membranes within the central nervous system.

MEG hemisulfate (Mercaptoethylguanidine hemisulfate) acts as a highly potent and selective suppressor of inducible NO synthase (iNOS), demonstrating EC50 values of 11.5 μM for iNOS, 110 μM for ecNOS, and 60 μM for bNOS in tissue homogenates. It is notably effective as a peroxynitrite scavenger and blocks peroxynitrite-triggered oxidative mechanisms. Furthermore, this compound offers protective benefits across various experimental inflammation prototypes, such as ischemia/reperfusion injury, hemorrhagic shock, periodontitis, inflammatory bowel disease, and both endotoxic and septic shock.

PXS-5153A is an effective, selective, and fast-acting inhibitor of lysyl oxidase like 2/3 enzymes with enzymatic activity almost entirely blocked within 15 minutes. PXS-5153A could reduce crosslinks and ameliorates fibrosis.

CFM-2, a potent and selective non-competitive antagonist of AMPAR (AMPAR), exhibits anticonvulsant activity across various seizure models.

LUF6096 (CF-602) is a potent allosteric enhancer of the adenosine A3 receptor, exhibiting the capability to enhance agonist binding allosterically while demonstrating low orthosteric affinity across adenosine receptors. It displays protective effects in myocardial ischemia/reperfusion injury.

C-Myc Inhibitor 7, serving as both a c-Myc inhibitor and a multi-target protein degrader, effectively degrades proteins c-MYC, CK1α, GSPT1, and IKZF1/2/3 across various tumor cell types. It holds potential for research into diseases associated with high c-Myc expression, including cancer, cardiovascular and cerebrovascular conditions, and viral infections.

Repinotan HCl (Bay-x-3702) is an orally active, selective and potent 5-HT1A receptor agonist across the blood-brain barrier and is an aminomethylbenzidine derivative.Repinotan HCl has potent neuroprotective effects and can be used in studies of ischemic stroke and traumatic brain injury.

FINO2 is a potent ferroptosis-inducing compound that inhibits GPX4 activity. It functions as a stable oxidant, effectively oxidizing ferrous iron and demonstrating stability across varying pH levels. Furthermore, FINO2 induces widespread lipid peroxidation.

Emedastine (LY188695) is a second generation, selective histamine H1 receptor antagonist with anti-allergic activity. Emedastine reversibly and competitively blocks histamine by binding to H1 receptors, thus blocking its downstream activity. As a result this agent interferes with mediator release from mast cells either by inhibiting calcium ion influx across mast cell/basophil plasma membrane or by inhibiting intracellular calcium ion release within the cells. In addition, emedastine may also inhibit the late-phase allergic reaction mediated through leukotrienes or prostaglandins, or by producing an anti-platelet activating factor effect. Upon ocular administration, emedastine causes a dose-dependent inhibition of histamine-stimulated vascular permeability in the conjunctiva. Emedastine does not affect adrenergic, dopamine, or serotonin receptors.

Surfactin is a potent cyclic lipopeptide biosurfactants that mediates flux of mono-and divalent cations, such as calcium, across lipid bilayer membranes, with anti-bacterial, anti-fungal, antimycoplasma and hemolytic effects.

sn-Glycero-3-phosphocholine (Choline glycerophosphate) is a natural choline compound found in the brain and in milk. It is also a parasympathomimetic acetylcholine precursor which may have a potential for the treatment of Alzheimer's disease and dementia. sn-Glycero-3-phosphocholine rapidly delivers choline to the brain across the blood–brain barrier and is a biosynthetic precursor of the acetylcholine neurotransmitter. It is a non-prescription drug in most countries due to its Generally Recognised As Safe (GRAS) status [1]. Studies have investigated its efficacy for cognitive disorders including stroke and Alzheimer's disease. An Italian multicentre clinical trial on 2, 044 patients suffering from recent stroke were supplied Glycerylphosphorylcholine in doses of 1, 000 mg/day for 28 days and 400 mg three times per day for the five ensuing months. The trial confirmed the therapeutic role of alpha-GPC on the cognitive recovery of patients based on four measurement scales, three of which reached statistical significance [2].

Nigericin is an antibiotic derived from Streptomyces hygroscopicus that acts as a K+/H+ ionophore, promoting K+/H+ exchange across mitochondrial membranes. Nigericin can be an NLRP3 activator that causes the release of IL-1β as a NALP3-dependent manner. N

R-(+)-Cotinine ((+)-Cotinine), a metabolite of Nicotine, demonstrates minimal activity across numerous pharmacological targets. However, it is capable of enhancing the acetylcholine (Ach)-evoked current in human α7 nicotinic acetylcholine receptors (nAChRs) [1].

Phospholipase D (PLD), an enzyme within the phospholipase superfamily, is prevalent across bacteria, yeast, plants, animals, and viruses, serving roles in biochemical research. It catalyzes the hydrolysis of glycerophospholipids' phosphodiester bonds, generating phosphatidic acid and soluble choline. PLD is implicated in numerous disease-related pathways, such as diabetes, atherogenesis, obesity, tumorigenesis, immune responses, and neuroendocrine functions [1].

LSP-GR3, a novel splice modulating oligomer (SMO) consisting of chemically-modified RNA oligonucleotides, potently and specifically directs the alternative splicing of GluR to promote GluR3-flip expression across the central nervous system (CNS).

LM2I, a derivative of Spinosyn A (SPA), serves both as an argininosuccinate synthase (ASS1) enzyme activator and a tumor inhibitor through direct interaction with ASS1. It demonstrates notable antiproliferative effects across seven colorectal cancer cell lines and in colorectal cancer xenograft tumors. Furthermore, LM2I suppresses the growth of colorectal cancer cells by targeting the EGFR pathway [1].

Malonyl Coenzyme A (lithium) is a coenzyme A derivative that is utilized in fatty acid and polyketide synthesis and in the transport of α-ketoglutarate across the mitochondrial membrane. Malonyl Coenzyme A (lithium) is formed by the Acetyl CoA Carboxylase-mediated carboxylation of acetyl CoA. Malonyl Coenzyme A (lithium) is exclusively used as the extender unit in the synthesis of bacterial aromatic polyketides.

SAR441255 is a potent unimolecular peptide that acts as a GLP-1/GIP/GCG receptor triagonist, demonstrating balanced activation across all three target receptors. It has shown positive acute glucoregulatory effects in diabetic obese monkeys [1].

Spexin-2 (53-70), human, mouse, rat (NPQ 53-70), is a biologically active, non-amidated peptide derived from the prohormone proNPQ, conserved across mammalian species. It acts as a central modulator of cardiovascular and renal function, with observed effects in rats including a decrease in heart rate and an increase in urine flow rate.

EILDV (human, bovine, rat) is an active pentapeptide analog with a conserved tripeptide sequence LDV across human, bovine, and rat species, utilized in cell adhesion research [1].

Poloxamer 188, a nonionic linear copolymer possessing surfactant properties, demonstrates anti-thrombotic, anti-inflammatory, and cytoprotective activities across different tissue injury models.

RyR1(3614-3643) is a biologically active peptide representing the absolutely conserved CaM-binding domain of RyR1 across all vertebrates.

Aflatoxin Q1, a hydroxy metabolite of Aflatoxin B1 (AFB1)—a mycotoxin synthesized by Aspergillus flavus (A. flavus)—and aflatoxin B1 8,9-oxide are principal oxidative derivatives produced from Aflatoxin B1 in human liver microsomes across all substrate concentrations. The conversion of Aflatoxin B1 to Aflatoxin Q1 through 3 alpha-hydroxylation represents a critical detoxification route [1] [2].

Pep-1-Cysteamine, a chimeric cell-penetrating peptide (CPP), exhibits primary amphipathicity and facilitates the translocation of active proteins across biological membranes into cells [1].

The binding affinities of ganoderic acid DM and ganoderic acid Z (ΔGbind, -16.83 and-10.99 kcal mol-1) are comparable to that of current commercial drug oseltamivir (-23.62 kcal mol-1);Ganoderic acid DM is a potential source of anti-influenza ingredient, with novel binding pattern and advantage over oseltamivir, it has steric hindrance on the 150 cavity of N1 protein, and exerts activities across the H274Y and N294S mutations, is the attractive candidates of novel neuraminidase (NA) inhibitors.Ganoderic acid zeta has cytotoxicity in vitro against Meth-A and LLC cell lines.

PRMT4-IN-2 (compound 55) acts as a pan-inhibitor across various protein arginine methyltransferase (PRMT) isoforms, exhibiting inhibitory potencies with IC50 values of 92 nM for PRMT4, 436 nM for PRMT6, 460 nM for PRMT1, 823 nM for PRMT8, and 1.386 μM for PRMT3 [1].

Targefrin is a potent antagonist targeting EphA2, exhibiting a dissociation constant of 21 nM and an IC50 value of 10.8 nM for the EphA2-LBD. It promotes receptor internalization and degradation across multiple pancreatic cancer cell lines [1].

LAS190792 (AZD8999) is a dual-action chemical compound that simultaneously acts as a strong muscarinic antagonist and β2-adrenoceptor agonist. It exhibits significant potency across a range of receptors, with pIC50 values of 8.9 for M1, 8.8 for M2, 8.8 for M3, 9.2 for M4, 8.2 for M5, 7.5 for β1, 9.1 for β2, and 5.6 for β3. Its effectiveness across these receptors makes LAS190792 a viable candidate for bronchodilator applications [1].

HAIYPRH hydrochloride is a targeting ligand that specifically binds to the transferrin receptor (TfR) and facilitates the transport of nanocarriers across the blood-brain barrier [1].

KY-1044 (Alomfilimab; SAR 445256) is a fully human IgG1 monoclonal antibody that targets the inducible costimulatory receptor (ICOS). This compound selectively depletes cells with high ICOS expression through antibody-dependent cellular cytotoxicity (ADCC), mediated by FcγRIIIa engagement. Meanwhile, it acts as a costimulatory molecule for cells with lower ICOS levels, such as CD8+ T Effector cells, via FcγR-dependent clustering. KY-1044 leverages varying ICOS expression levels across T-cell subsets to enhance the intratumoral immune milieu and reinvigorate antitumor immune responses [1].

Tricyclene, a monoterpene identified in various conifers such as Abies, Pinus, Picea, and Tsuga, exhibits notable presence across these species.

Tetanus Toxin (830–844), a biologically active peptide and a tetanus toxin-derived peptide TT830–844 CD4+ T-cell epitope, exhibits promiscuity by binding to a wide spectrum of HLA–DRB molecules. Consequently, it is anticipated to elicit CD4+ T-cell responses across a broad segment of the human population.

LP-184 (Compound 6), referred to as an acylfulvene analog, demonstrates the ability to inhibit tumor growth with noteworthy anti-cancer efficacy observed across multiple cell lines, including ovarian, colon, prostate, and pancreatic.

Transdermal Peptide is a 11-amino acid peptide, binds to Na+/K+-ATPase beta-subunit (ATP1B1), and enhances the transdermal delivery of many macromolecules. Transdermal Peptide (TD1) binds to ATP1B1, and mainly interacts with the C-terminus of ATP1B1 in yeast and mammalian cells. The interaction affects the expression and localization of ATP1B1 and epidermal structure, but can be antagonized by the exogenous competitor ATP1B1 or be inhibited by ouabain. Inhibition of Transdermal Peptide binding to ATP1B1 causes decreased delivery of macromolecular drugs across the skin[1]. [1]. Wang C, et al. Role of the Na(+)/K(+)-ATPase beta-subunit in peptide-mediated transdermal drug delivery. Mol Pharm. 2015 Apr 6;12(4):1259-67.

CU06-1004 (Sac-1004) is an orally active compound that acts as an endothelial dysfunction blocker. It mitigates endothelial dysfunction by inhibiting hyperpermeability and inflammation. The compound demonstrates efficacy in reducing vascular leakage and inflammation across multiple animal models, including those for diabetic retinopathy, stroke, cancer, and inflammatory bowel disease. Additionally, CU06-1004 improves conditions in a CDAA-induced mouse model of NASH and enhances cardiac function [1] [2] [3].

SRI-37240 is a potent inhibitor of premature termination codons (PTCs) with read-across activity that induces a prolonged pause at the termination codon and inhibits PTCs associated with cystic fibrosis.SRI-37240 can be used to study PTC-related diseases.

6-Methoxypurine arabinoside (Ara-m), a potent inhibitor of the varicella-zoster virus (VZV), exhibits 50% inhibitory concentrations (IC50) between 0.5 and 3 microM across eight VZV strains [1].

HN-1, a 12-mer peptide with specificity for head and neck squamous cell carcinoma (HNSCC), penetrates tumor tissue and facilitates the translocation of agents across cell membranes [1].

Inubritannolide A exhibits moderate to robust neuroprotective effects across various neuronal cell types against inducers such as H2O2, 6-hydroxydopamine (6-OHDA), and lipopolysaccharide (LPS).

KMG-104 is a fluorescent magnesium (Mg2+) probe known for its exceptional selectivity. It has been extensively utilized to investigate the mobilization of Mg2+ in the cytoplasm across different cell types.

Allo-aca TFA, a potent and specific leptin receptor antagonist peptide, inhibits leptin signaling and function across various in vitro and in vivo models [1] [2].

ODN 2007, a class B CpG ODN (oligodeoxynucleotide) and Toll-like receptor (TLR) ligand, serves as an immunomodulator and vaccine adjuvant, promoting enhanced immune responses across mammals, fish, and humans. Its sequence is 5'-TCGTCGTTGTCGTTTTGTCGTT-3' [1] [2] [3].

UDP-xylose, a natural product isolated from Cryptococcus laurentii (NRRL Y-1401), serves as a sugar donor in the synthesis of glycoproteins, polysaccharides, various metabolites, and oligosaccharides across plants, vertebrates, and fungi [1] [2].

Substance P (2-11), a fragment peptide of Substance P (SP), exhibits contractile effects on the guinea pig ileum and inhibits the permeation of tritiated SP (3 H SP) across brain microvessel endothelial cell (BBMEC) monolayers [1] [2].

rTAT is a potent cell-penetrating peptide (CPP) that effectively translocates across cellular membranes [1] [2].

β-Amyloid (1-40), England mutation, is a biologically active peptide with a histidine (His) to arginine (Arg) substitution at position 6, known to enhance oligomerization kinetics that serve as fibril seeds and increase neurotoxicity in cultured neurons. This alteration is one of several mutations in the beta-amyloid precursor gene implicated in autosomal dominant Alzheimer's Disease across multiple kindreds.

Cantuzumab ravtansine (IMGN242; huC242-DM4), an antibody-drug conjugate (ADC), consists of the humanized monoclonal antibody huC242 covalently bonded through a disulfide linkage to the cytotoxic agent DM4 (DM4). This compound demonstrates extensive antitumor effectiveness across various CanAg-positive human tumor xenografts [1] [2].

PIM-IN-2 (Pim-2) is a potent inhibitor of Pim kinases, demonstrating an inhibition concentration half-maximal (IC50) value of 25 nM . It exhibits antiapoptotic properties conducive to cell survival and has been found to have increased expression levels across various human tumors [1].