nucleus

DNQX disodium salt is a water-soluble form of selective antagonist of non-NMDA receptor

Kinsenoside ((+)-Kinsenoside) shows significant antihepatotoxic, and anti-inflammatory activities. Kinsenoside could be useful for repairing beta cells in pancreatic islet injury as well as improving its function, it could promote the glucose tolerance of acute glucose increase in both diabetic and normal healthy rats. Kinsenoside inhibits osteoclastogenesis from macrophages by attenuating RANKL-induced NF-κB and NFATc1 activities, which in turn, prevents bone loss from OVX mice.

DNQX (FG 9041) is a competitive, non-NMDA glutamate receptor antagonist (IC50s = 0.5 and 0.1 μM for AMPA and kainate receptors, respectively)

Echinocandin B nucleus (A-30912 A nucleus) is the reaction product catalyzed by Echinocandin B decarboxylase. It serves as an intermediate in the semisynthetic production of antifungal agents.

4-Hydroxytamoxifen (ICI 79280) is the active metabolite of Tamoxifen, an estrogen receptor modulator (SERM) with selective and oral potency. 4-Hydroxytamoxifen has antitumor activity and may be used in breast cancer research.

Beclometasone dipropionate (Vancenase) is the dipropionate ester of a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties. After cell surface receptor attachment and cell entry, beclomethasone enters the nucleus where it binds to and activates specific nuclear receptors, resulting in an altered gene expression and inhibition of proinflammatory cytokine production.

Desonide (Prednacinolone) is a synthetic glucocorticosteroid for topical use, with anti-inflammatory activity. Desonide binds to glucocorticoid receptors in the cytoplasm, and the ligand-receptor complex is translocated as a homodimer into the nucleus, where transcription activation via glucocorticoid response elements within glucocorticoid-responsive genes occur. This agent induces transcription of genes coding for anti-inflammatory proteins, including lipocortin-1, interleukin-10, interleukin-1 receptor antagonist and neutral endopeptidase. Increased synthesis of lipocortin-1 has an inhibitory effect on phospholipase A2, which in turn inhibits the release of arachidonic acid, thereby controlling the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes.

Pyrimidine (Metadiazine)s are heterocyclic, six-membered, nitrogen-containing carbon ring structures, with uracil, cytosine and thymine being the basal structures of ribose-containing nucleosides (uridine, cytidine, and thymidine respectively), or deoxyribose-containing deoxynucleosides, and their corresponding ribonucleotides or deoxyribonucleotides. Pyrimidines serve essential functions in human metabolism as ribonucleotide bases in RNA (uracil and cytosine), and as deoxyribonucleotide bases in DNA (cytosine and thymine), and are linked by phosphodiester bridges to purine nucleotides in double-stranded DNA, in both the nucleus and the mitochondria. Pyrimidine activated sugars are also involved in polysaccharide and phospholipid synthesis, glucuronidation in detoxification processes, glycosylation of proteins and lipids and in the recently identified novel endothelium-derived vasoactive dinucleotides.

ZZL-7 is a fast-onset antidepressant agent that disrupts the interaction between neuronal nitric oxide synthase (nNOS) and the serotonin transporter (SERT) in the dorsal raphe nucleus (DRN). It easily crosses the blood-brain barrier and has research value in major depressive disorder (MDD).

ECBN HCL (A-30912A nucleus hydrochloride) is the reaction product catalyzed by Echinocandin B (ECB) deacylase.

Triamcinolone (Aristocort) is a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties. Upon cell entry, triamcinolone binds to and activates the glucocorticoid receptor, which leads to translocation of the ligand-receptor complex to the nucleus and induces expression of glucocorticoid-responsive genes such as lipocortins. Lipocortins inhibit phospholipase A2, thereby blocking the release of arachidonic acid from membrane phospholipids and preventing the synthesis of prostaglandins and leukotrienes, both mediators of inflammation. In addition, pro-inflammatory cytokine production, including interleukin (IL)-1and IL-6, and the activation of cytotoxic T-lymphocytes is also inhibited. T-cells are prevented from making IL-2 and proliferating. This agent also decreases the number of circulating lymphocytes, induces cell differentiation, and stimulates apoptosis through increasing Ikappa-B expression and curtailing activation of nuclear factor (NF)kappa-B.

AZ82 is a selective inhibitor of kinesin-like protein KIFC1 (HSET/KIFC1), with a Ki of 43 nM and an IC50 of 300 nM for KIFC1.

CWP232228, a potent and selective Wnt / β-catenin signaling inhibitor, antagonizes the binding of β-catenin to T-cell factor (TCF) in the nucleus. CWP232228 inhibits the formation and metastasis of tumors by inhibiting the growth of breast cancer and live

FG 7142 (LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 can increase tyrosine hydroxylation and cause upregulation of β-adrenoceptors in mouse cerebral cortex. FG 7142 , a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM).

ML218 is an orally active, selective, potent, and blood-brain barrier-crossing inhibitor of T-type Ca2+ channels (Cav3.1, Cav3.2, Cav3.3) (IC50 for Cav3.2 and Cav3.3 is 310 nM and 270 nM, respectively).ML218 inhibits the burst activity of neurons in the subthalamic nucleus (STN).

NIC3 is a selective nucleus accumbens-associated protein-1 (NAC1) inhibitor with anti-cancer activity.

PIN1 inhibitor API-1 is a specific Pin1 inhibitor (IC50: 72.3 nM) that retains the active conformation of pXPO5, restoring its ability to transport pre-miRNAs from the nucleus to the cytoplasm, thereby up-regulating anticancer miRNA biogenesis to suppress hepatocellular carcinoma development both in vitro and in vivo. PIN1 inhibitor API-1 directly and specifically binds to the Pin1 peptidyl-prolyl isomerase domain, effectively inhibiting Pin1 cis-trans isomerizing activity.

Fludrocortisone acetate (9α-Fludrocortisone acetate), a glucocorticoid-receptor agonist, binds to cytoplasmic receptors, translocates to the nucleus, and initiates transcription of glucocorticoid-responsive genes like lipocortins to inhibit phospholipase A2 (PLA2). As the acetate salt of a synthetic fluorinated corticosteroid, it exhibits anti-inflammatory and antiallergic activities. PLA2 inhibition prevents arachidonic acid release, a precursor of eicosanoids such as prostaglandins and leukotrienes, which are key mediators in the pro-inflammatory response. As a mineralocorticoid-receptor agonist, it stimulates Na+ reabsorption, water retention, and K+ and H+ secretion in the distal tubules and collecting ducts of the kidney.

(E)-KPT330 is a CRM1-selective inhibitor of nuclear export. It inhibits protein trafficking from the nucleus and induces cell cycle arrest and apoptosis in mesothelioma cells.

GTCpFE, a compound synthesized from Dimethyl fumarate (DMF) and Aspirin (ASA), inhibits IKKα/β in the NF-κB pathway, exhibiting anti-inflammatory activity by preventing p65 from entering the nucleus. It selectively inhibits cancer stem cell (CSC) activity by reducing the growth of mammospheres and the expression of the CD44+CD24- immune phenotype. Furthermore, GTCpFE targets breast cancer stem cells, crucial in aggressive cancer phenotypes that depend on NFκB and PGE2.

Compound 3 (DOR agonist 2) acts as a Delta Opioid Receptor agonist. It inhibits the expression of TNF-α, obstructs NF-κB transportation to the nucleus, and activates the G protein-mediated ERK1/2 pathway. This compound is useful for research into neurodegenerative diseases.

Nrf2/HO-1 Activator 3 (Compound C3a) is an activator of the Nrf2 signaling pathway that facilitates the translocation of Nrf2 into the nucleus and enhances the expression of heme oxygenase-1 (HO-1). In H9c2 cardiomyocytes subjected to H2O2 or high glucose stimulation, Nrf2/HO-1 Activator 3 inhibits the excessive expression of ROS and MDA, suppressing cell viability and colony formation, thereby exhibiting antioxidant activity.

G-quadruplexligand 3 (Compound 16) is a G-quadruplex ligand with the ability to chelate iron and exhibits anticancer properties. It stabilizes G-quadruplex structures within human leukemia Jurkat cells. Additionally, G-quadruplexligand 3 is localized in the cell nucleus and serves as a fluorescent nuclear tracer for the labile iron pool.

DL5055 (compound 6k) is a highly effective selective activator of hCAR, with an EC50 of 0.35 μM. It induces the expression of CYP2B6 in primary human hepatocytes and facilitates the translocation of hCAR to the nucleus.