nucleus

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.

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.

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.

1. Oroxylin A (Baicalein 6-methyl ether) has various anti-tumor effects including apoptosis, cell cycle arrest, drug-resistant reversion. 2. Oroxylin A possesses abilities of inhibiting the ATRA-induced IL-6 production via modulation of LAP LIP CHOP in leukemia cell lines, which could providing a therapeutic strategy for RAS. 3. Oroxylin A inhibits UCP2s triggers the MPTP opening, and promotes the apoptosis in CaCo-2 cells; uncoupling protein 2 plays a key role in mitochondrial apoptotic pathway. 4. Oroxylin A inhibits N1ICD translocating to the nucleus and binding to epithelial-mesenchymal transition-related transcription factor Snail, thus suppressing the invasion and migration of MCF-7 cells. 5. Oroxylin A improves the sensitivity of K562 ADM cells by increasing apoptosis in leukemic cells and decreasing the expression of CXCR4 and PI3K Akt NF-κB pathway, and probably served as a most promising agent for CML treatment.

(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.

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

Carbidine (Carbidin) is a derivative of gamma-carboline, an atypical antipsychotic drug. It reduces the inhibitory effect of DA on the 3H-DA release from synaptosomes of the nucleus accumbens septi and on the activity of tyrosine hydroxylase in vivo and in vitro.

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).

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.

Mg(II) protoporphyrin IX, essential for chlorophyll synthesis in Chlorella, functions as a negative regulator of nuclear photosynthetic gene expression and is used as a research tool for studying the signaling molecule in plastid-to-nucleus communication.

SV40 large T antigen NLS, originating from Large T antigen residue 47 to 55, facilitates protein import into the cell nucleus. This peptide is specifically generated from Large T antigen residue 47 to 55.

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.

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

β-Cateninmodulator-7 (Compound 5) acts as a regulator of β-catenin. It suppresses the expression of β-catenin in both the cytoplasm and nucleus of HCT-116 cells and inhibits the phosphorylation of GSK 3β. Additionally, β-Cateninmodulator-7 facilitates the release of NO in HCT-116 cells and inhibits the proliferation of these cancer cells, with an IC50 value of 0.6-0.9 μM. This compound is utilized in research related to colon cancer.

Beclomethasone Dipropionate-d6 is a deuterated compound of Beclomethasone Dipropionate. Beclomethasone Dipropionate has a CAS number of 5534-09-8. Beclomethasone Dipropionate 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.

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.

Diazaborine inhibits maturation of rRNAs for the large ribosomal subunit. Diazaborine blocks ribosome biogenesis by inhibiting the AAA-ATPase Drg1. Diazaborine treatment causes, within minutes, a rapid redistribution of the protein from the nucleolus to t

Asperbisabolane L, a sesquiterpenoid, exhibits anti-inflammatory effects through the inhibition of the NF-κB-activated pathway. It prevents the translocation of NF-κB from the cytoplasm to the nucleus and also reduces NO production in LPS-activated BV-2 microglia cells.

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.

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).

Diflorasone is a synthetic glucocorticoid with anti-inflammatory and immunosuppressive properties. Like other glucocorticoids, diflorasone enters the cell by diffusion across the cell membrane and binds to the glucocorticoid receptor (GR) in the cytoplasm

ADTN hydrobromide (6,7-ADTN) is a dopamine receptor agonist (EC50s = 3.5 and 0.65 μM in rat striatal and nucleus accumbens homogenates, respectively). ADTN hydrobromide stimulates production of cAMP in rat striatal homogenates, a process that is reduced by 70% in the presence of the dopamine antagonist fluphenazine at a concentration of 1 μM.