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CEP-18770 (CAS 847499-27-8) is a reversible boronic acid-based inhibitor of proteasome chymotrypsin-like activity It specifically targets the proteasome s P2 threonine protease subunit reducing NF- B signaling and the expression of downstream effectors With a reported IC50 of 3 8 nM CEP-18770 induces apoptosis in multiple myeloma cell lines and inhibits osteoclastogenesis and angiogenesis via suppression of RANKL signaling Research supports its potential use in oncology particularly for multiple myeloma showing selective cytotoxicity sparing normal epithelial and bone marrow-derived cells
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Belinostat (PXD101) is a hydroxamic acid-based inhibitor targeting histone deacetylase (HDAC) enzymes Its mechanism involves the suppression of HDAC enzymatic activity leading to increased acetylation of histone proteins H3 and H4 within cells In biochemical assays using Hela cell extracts belinostat exhibits inhibitory activity against HDAC with an IC50 value of approximately 27 nM In tumor cell culture models belinostat induces cytotoxicity and represses cellular proliferation with reported IC50 values ranging roughly from 0 5 M to 10 M varying by cell type and origin making it suitable for research on epigenetic modulation in oncology specifically in studies of bladder prostate and related cancer cell lines
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Bortezomib (PS-341 CAS number 179324-69-7) is a reversible proteasome inhibitor structurally composed as an N-terminally protected dipeptide (Pyz-Phe-boroLeu) containing pyrazinoic acid phenylalanine and leucine with boronic acid substitution It exerts biological activity primarily by inhibiting proteasomal degradation pathways thereby accumulating pro-apoptotic factors and initiating programmed cell death Bortezomib inhibits proliferation in cell-based assays such as human non-small cell lung cancer H460 cells (IC50 0 1 M) It has clinical approval for relapsed multiple myeloma and mantle cell lymphoma and is widely employed in research to study proteasome-regulated cellular processes and apoptosis signaling pathways
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AM095 (CAS 1345614-59-6) is an orally bioavailable antagonist targeting the lysophosphatidic acid receptor 1 (LPA1) It selectively inhibits recombinant human and mouse LPA1 receptors with IC50 values of 0 98 M and 0 73 M respectively In cell-based assays AM095 suppresses LPA1-mediated chemotaxis in mouse LPA1/CHO and human melanoma A2058 cells (IC50 values 0 78 M and 0 23 M respectively) In vivo studies demonstrate its ability to prevent LPA-triggered histamine release reduce collagen and protein accumulation and limit inflammatory cell infiltration in mouse pulmonary models AM095 serves as a valuable tool for investigating LPA1-associated pathologies
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AGN 194310 is a pan-retinoic acid receptor (RAR) antagonist with affinity for RAR RAR and RAR It binds these receptors with Kd values of 3 nM 2 nM and 5 nM respectively By competing with RAR agonists AGN 194310 blocks receptor-mediated cellular responses In cell-based assays AGN 194310 inhibits the proliferation and colony formation of prostate carcinoma cell lines (LNCaP PC3 DU-145) induces G1 cell cycle arrest and promotes apoptosis In addition it suppresses agonist-induced differentiation in HL60 cells AGN 194310 serves as a research tool to investigate RAR-driven signaling pathways and tumor cell growth mechanisms particularly in oncology studies examining retinoid receptor functions
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Avasimibe (CAS 166518-60-1) is an orally bioavailable inhibitor of acyl-coenzyme A cholesterol acyltransferase (ACAT) an enzyme involved in cholesterol esterification It exhibits potent inhibition with an IC50 of approximately 60 nM In cell-based studies avasimibe reduces intracellular cholesterol esters in a dose-dependent manner without elevating free cholesterol levels suggesting an advantageous safety profile Additionally avasimibe reduces synthesis and secretion of Apo B 100 a constituent of very low-density lipoprotein (VLDL) in HepG2 cells and increases bile acid synthesis in rat hepatocytes Beyond dyslipidemic modulation and anti-atherogenic activities it influences amyloid precursor protein (APP) trafficking reducing its maturation and subsequent amyloid-beta (A ) peptide generation providing avenues for Alzheimer s disease research
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Influenza hemagglutinin (HA) peptide (sequence YPYDVPDYA) is commonly utilized in biomedical studies as an epitope tag for protein detection and isolation Derived from the influenza virus hemagglutinin protein HA mediates viral entry into host cells through initial receptor binding (via HA1 subunit) and subsequent membrane fusion (via HA2 subunit) Under acidic intracellular conditions HA undergoes conformational changes enabling membrane destabilization and viral fusion Synthetic HA-derived peptides can mimic this fusogenic mechanism enhancing gene transfer efficiency in vitro through promoting cellular uptake of transfection complexes in various cultured cell lines including K562 HeLa and BNL CL 2 hepatocyte cells Typically employed within transferrin-polylysine-DNA based delivery systems these HA peptides facilitate membrane disruption increasing complex internalization reported IC50 values vary depending on specific cellular systems and experimental conditions
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