modulation

Y-27632 dihydrochloride (Y-27632 2HCl) is an orally potent, ATP-competitive inhibitor of ROCK-I and ROCK-II. Y-27632 dihydrochloride also inhibits isolation-induced apoptosis in mouse prostate stem or progenitor cells.

Punicalagin is a major ellagitannin found in pomegranates that is reported to produce antioxidant, anti-inflammatory, and anticancer effects. It has been shown to prevent high-fat diet-induced obesity-associated accumulation of cardiac triglyceride and ch

Atinvicitinib, a selective Janus kinase (JAK) inhibitor, demonstrates high specificity for Janus kinase 1 (JAK1), consequently inhibiting downstream cytokine signaling pathways that rely on JAK1 enzymatic activity. Atinvicitinib modulates a wide range of cytokines that are implicated in itch responses, allergic reactions, and inflammatory conditions, making it a significant research tool for studying cytokine-mediated immune processes as well as therapeutic modulation of allergic and inflammatory diseases.

Prostaglandin E2 (PGE2) is a natural hormone-like substance involved in various physiological functions, including the contraction and relaxation of smooth muscles, dilation and constriction of blood vessels, regulation of blood pressure, and modulation of inflammation. It can be used to induce neuropathic pain models.

Agomelatine (L(+)-Tartaric acid) is a specific agonist of MT1 and MT2 receptors (Kis: 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2), and Agomelatine (S-20098). L(+)-Tartaric acid also functions as a selective 5-HT2C receptor antagonist (pKis: 6.4 and 6.2 at native porcine and cloned human 5-HT2C receptors), actively supporting research into melatonergic signaling pathways, receptor-mediated regulation, and novel psychiatric therapeutics by enabling precise modulation of circadian and serotonergic systems in cellular models to improve neuropharmacological understanding and experimental reproducibility across neuroscientific and clinical translational studies.

XU1(Benzo[c][1,8]naphthyridin-6(5h)-One) is an Aurora protein kinase inhibitor used for the treatment of diseases suitable for inhibition, regulation or modulation of kinase signaling.

CGP 20376 is a benzothiazole compound, an anthelmintic, with dual dose-dependent modulation of in vitro effects on the respiratory burst of eosinophils and antifibrillatory properties.

Viloxazine (Viloxazin) (Viloxazin) is a dual-action compound that functions as a norepinephrine reuptake inhibitor and exhibits potent agonistic activity towards 5-HT 2C receptors while acting as an antagonist for 5-HT 2B receptors, with respective potency values of EC 50 = 32 μM and IC 50 = 27 μM. Its primary mechanism of action involves the modulation of serotonergic and noradrenergic pathways. Viloxazine is commonly employed in depression research [1] [2].

Ceramides Mixture, an endogenous ceramide, consists of hydroxy and non-hydroxy fatty acid-containing ceramides. It is involved in the regulation of cell cycle arrest, growth inhibition, and modulation of telomerase activity.

2,2,5,7,8-Pentamethyl-6-Chromanol (PMC) is the antioxidant component of vitamin E (α-tocopherol) and exhibits significant androgen receptor (AR) signaling modulation and anti-cancer activity against prostate cancer cell lines.

Suberoyl bis-hydroxamic acid (SBHA) is a Histone deacetylase (HDAC) inhibitor. HDAC is required for transcriptional modulation, cell cycle regulation and development. It is an enzyme that deacetylates lysine residues on the N-terminal of the core histones.

NOD1/2 antagonist-1 is a dual inhibitor of nucleotide-binding oligomerization domain-like receptors NOD1 and NOD2, exhibiting IC50 values of 1.13 uM for NOD1 and 0.77 uM for NOD2, with an acceptable half-life of 67.6 minutes. NOD1/2 antagonist-1 enhances the antitumor efficacy of paclitaxel and serves as a potent experimental tool for investigating innate immune receptor-mediated signaling and cancer therapy modulation.

BC-1293 is an inhibitor of the E3 ligase subunit FBXO24 that acts by disrupting the interaction between FBXO24 and aspartyl-tRNA synthetase (DARS2). BC-1293 treatment results in increased levels of DARS2, showing its capacity to stabilize this essential enzyme. Furthermore, BC-1293 elevates levels of cytokines including IL-1β, IL-9, MIP-2, and TNF-α in murine models, thereby demonstrating immunostimulatory activity with potential relevance to immune modulation research.

Nitroaspirin (NCX 4016) is a nitric oxide donor and a nitro-derivative of Aspirin that inhibits cyclooxygenase. It induces cell cycle arrest and apoptosis in Cisplatin-resistant human ovarian cancer cells by down-regulating EGFR/PI3K/STAT3 signaling and modulating Bcl-2 family proteins. Additionally, Nitroaspirin possesses antithrombotic and antiplatelet properties and acts as a direct and irreversible inhibitor of COX-1.

COR659 is a GABAB positive allosteric modulator (PAM) . COR659 suppresses alcohol and chocolate self-administration in rats[1]. COR659 apparently exerts its effects via a composite mechanism, including positive allosteric modulation of the GABAB receptor and an action at the cannabinoid CB1 receptor[3]. COR659 (0, 2.5, 5 and 10 mg/kg) treatment is completely ineffective on lever-responding (FR10) for regular food pellets in food-deprived Wistar rats[1].COR659 is able to suppress lever-responding for a sucrose solution in sP rats and a chocolate solution in Wistar rats[2]. Animal Model: Male sP and Wistar rats[1]. [1]. Paola Maccioni, et al. Suppressing effect of COR659 on alcohol, sucrose, and chocolate self-administration in rats: involvement of the GABA B and cannabinoid CB 1 receptors. Psychopharmacology (Berl). 2017 Sep;234(17):2525-2543. [2]. Francesca Ferlenghi, et al. The GABA B receptor positive allosteric modulator COR659: In vitro metabolism, in vivo pharmacokinetics in rats, synthesis and pharmacological characterization of metabolically protected derivatives. Eur J Pharm Sci. 2020 Dec 1;155:105544. [3]. Paola Maccioni, et al. Anti-addictive properties of COR659 - Additional pharmacological evidence and comparison with a series of novel analogues. Alcohol. 2019 Mar;75:55-66.

(+)-Dropropizine can inhibit histamine receptor, anti-allergic, and reduce a cough by modulation of neuropeptides involved in the cough reflex and by interfering with stimulus activation of peripheral endings of sensory nerves.

Gamma-secretase modulator 2 is a potent, selective compound for the treatment of Alzheimer's disease, specifically designed to modulate γ-secretase activity. This modulation selectively attenuates the production of Aβ(1-42), addressing diseases associated with Aβ deposition in the brain, particularly Alzheimer's disease.

RR-11a is a synthetic enzyme legumain inhibitor. This compound specifically targets and inhibits the activity of legumain, an enzyme implicated in various biological processes. RR-11a's synthetic nature allows for precise modulation of legumain activity, making it a valuable tool in biochemical research and potential therapeutic applications.

(R)-BAY1238097 represents the R-isomer of BAY1238097, which exhibits relatively lower activity compared to its counterpart. BAY1238097 is a highly potent and selective inhibitor targeting the binding of BET proteins to histones, demonstrating significant anti-proliferative effects in various acute myeloid leukemia (AML) and multiple myeloma (MM) models. The high activity is achieved through the down-regulation of c-Myc levels and the subsequent modulation of its downstream transcriptome.

AP5 is a potent and selective agonist for the GPR40 receptor with positive allosteric modulation of endogenous ligands (AgoPAM). AP5 demonstrates a rat hIP1 EC50 of 0.49 nM against the GPR40 receptor.

AP1867 (FK506-binding protein) is a synthetic FKBP12 F36V-directed ligand attached to 320 substituted tetrahydrooxazepines (THOXs). AP1867 (FK506-binding protein) was synthesized via combined liquid- and solid-phase methods employing sequential Mitsunobu displacements followed by ruthenium-mediated olefin metathesis to close seven-membered rings; the resin-bound THOX ligands were coupled to AP1867 in parallel, yielding candidate heterodimerizers that demonstrated membrane permeability and bioactivity in human fibrosarcoma cells, facilitating the study of targeted protein interactions and intracellular modulation.

ar-Turmerone ((+)-ar-Turmerone) is a major bioactive compound of the herb Curcuma longa with anti-tumorigenesis and anti-inflammatory activities[1][2][3]. It positively modulates murine DCs, induces NSC proliferation, and constitutes a promising therapeutic agent for various neurologic disorders[4][5]. It also activates apoptotic proteins in human lymphoma U937 cells[3].

Mal-NH-ethyl-SS-propionic acid, a cleavable linker employed for the synthesis of antibody-drug conjugates (ADCs)[1], plays a crucial role in the modulation of drug release from the conjugate.

PF-4778574 is a positive AMPA receptor allosteric modulation (EC50: 45 to 919 nM in different cells).