Dimethyl Sulfoxide
Apexbio Technology LLC GSK3787 188591-46-0 10mM (in 1mL DMSO)
GSK3787 is an irreversible antagonist targeting peroxisome proliferator-activated receptor beta/delta (PPAR- / ) Structurally it acts through covalent modification by binding specific cysteine residues within the ligand-binding domain of PPAR- / thereby disrupting receptor activation and subsequent co-regulator interactions Due to receptor selectivity GSK3787 preferentially inhibits PPAR- / relative to PPAR- Experimental evidence in rodent models demonstrates that oral administration of GSK3787 counteracts agonist-induced gene expression such as Angptl4 and Adrp by reducing recruitment of activated PPAR- / to target gene promoters indicating potential utility in studying PPAR- / -mediated regulatory pathways related to lipid metabolism and gene transcription in vitro and in vivo
Apexbio Technology LLC GDC-0994 1453848-26-4 10mM (in 1mL DMSO)
GDC-0994 (CAS 1453848-26-4) is a selective small-molecule inhibitor targeting extracellular signal-regulated kinases 1 and 2 (ERK1/2) components of the MAP kinase signaling cascade downstream of RAS/RAF/MEK ERK1/2 mediates cell proliferation and differentiation frequently activated due to oncogenic mutations in RAS and BRAF GDC-0994 shows inhibition of ERK1 and ERK2 with IC50 values of 1 1 and 0 3 nM respectively In preclinical models bearing KRAS or BRAF mutant tumor xenografts oral administration of GDC-0994 suppresses ERK phosphorylation and downstream signaling demonstrating significant anti-tumor activity GDC-0994 is a potent tool for studying ERK signaling in cancer research
Apexbio Technology LLC Piceatannol 10083-24-6 10mM (in 1mL DMSO)
Piceatannol (CAS 10083-24-6) is a naturally occurring small molecule exhibiting anti-inflammatory immunomodulatory and antiproliferative activities It functions primarily by inhibiting protein tyrosine kinases including p56lck and syk kinases and suppressing tumor necrosis factor (TNF)-induced nuclear factor-kappa B (NF- B) activation and downstream gene expression Biologically piceatannol arises as a metabolite of resveratrol through oxidation by cytochrome P450 1B1 This compound is employed in biomedical research to explore kinase signaling pathways inflammatory response regulation and potential therapeutic interventions
Apexbio Technology LLC E 64d 88321-09-9 10mM (in 1mL DMSO)
E-64d is a membrane-permeable cysteine protease inhibitor derived from E-64c acting via covalent modification of the proteolytic active site thiol group It demonstrates inhibitory activity primarily against calpain a calcium-dependent cysteine protease involved in diverse cellular processes E-64d readily penetrates intact cells allowing researchers to inhibit intracellular protease activity without disruption In intact platelet models short incubation with E-64d results in persistent suppression of calpain activity even after removal of extracellular inhibitor by washing Experimentally it is commonly utilized to investigate calpain s role in physiological and pathological events particularly in platelets and cellular apoptosis pathways The typical reported IC50 value of E-64d against calpain is approximately 0 5 1 M
Medchemexpress LLC Cimetidine sulfoxide | 54237-72-8 | 97.0% | 268.35 | 25 MG
Cimetidine sulfoxide is a sulfoxide metabolite of Cimetidine. Cimetidine acts as a histamine H2-receptor antagonist and has potential for treating peptic ulcer disease and upper gastrointestinal hemorrhage. Active transport of Cimetidine across the rat small intestine is observable at lower substrate concentrations. Cimetidine sulfoxide is detected after some incubations, and its enantiomeric composition has been determined in rat urine following Cimetidine administration.
- Histamine H2-receptor antagonist
- Potential for peptic ulcer disease treatment
- Potential for upper gastrointestinal hemorrhage treatment
- Sulfoxide metabolite
- Soluble in various solvents for in vitro and in vivo studies
- Store powder at -20°C for 3 years
- Store in solvent at -80°C for 6 months or -20°C for 1 month
Apexbio Technology LLC Maraviroc(Synonyms: Selzentry, Celsentri, UK-427857, MVC), 10mM (in 1mL DMSO), CAS: 376348-65-1.
Maraviroc (CAS 376348-65-1) is a potent selective antagonist of the chemokine receptor CCR5 CCR5 functions as a coreceptor expressed on immune cells and facilitates entry of certain HIV-1 virus strains (R5-tropic) By binding CCR5 maraviroc effectively blocks HIV-1 envelope protein gp120 anchoring and consequently prevents viral fusion and subsequent cell entry In cellular assays with CCR5-tropic HIV-1 maraviroc demonstrates substantial antiviral activity (IC50 approximately 2 0 nM) and efficiently inhibits gp120-CCR5 interaction Maraviroc serves as a valuable research tool to explore CCR5-mediated viral entry and HIV tropism dynamics
Medchemexpress LLC Encorafenib (Synonyms: LGX818) 10 mM * 1 mL in DMSO
Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E (EC50=4 nM).
Apexbio Technology LLC (-)-JQ1 1268524-71-5 10mM (in 1mL DMSO)
(-)-JQ1 (CAS 1268524-71-5) is a stereoisomer of ( )-JQ1 designed as a negative control in bromodomain inhibition studies Unlike ( )-JQ1 a competitive BET bromodomain inhibitor known to displace BRD4 fusion oncoproteins from chromatin the (-)-enantiomer shows negligible interaction with tested bromodomains It exhibits minimal inhibitory activity against BRD4(1) with an IC50 of 10 000 nM Due to the lack of significant bromodomain binding (-)-JQ1 serves widely as an appropriate negative control compound in experiments investigating BET protein functions and related signaling
Apexbio Technology LLC EPZ5676 1380288-87-8 10mM (in 1mL DMSO)
EPZ5676 (CAS 1380288-87-8) is a selective inhibitor targeting DOT1L a histone methyltransferase responsible for H3K79 methylation Structural studies indicate EPZ5676 occupies the enzyme s S-adenosylmethionine (SAM) binding pocket inducing conformational changes and partial opening beyond the SAM hydrophobic pocket EPZ5676 displays potent inhibitory activity against DOT1L (IC50 0 8 nM) with markedly lower affinity for other methyltransferases In MLL-rearranged leukemia models EPZ5676 reduces H3K79 methylation inhibits MLL fusion target gene expression and induces cytotoxicity in leukemia cell lines harboring MLL translocations
Apexbio Technology LLC Thioridazine HCl 130-61-0 10mM (in 1mL DMSO)
Thioridazine HCl is a pharmacological inhibitor targeting dopamine receptor subtypes D2 and D4 as well as a calcium channel blocker It modulates dopaminergic neurotransmission by interfering with receptor-mediated signaling and reduces intracellular calcium influx via calcium channel inhibition (IC50 approximately 1 0 M) Thioridazine is frequently utilized in research contexts involving dopaminergic signaling pathways calcium-related cellular processes and investigations of pharmacological sensitivity shifts following prolonged receptor modulation Specifically it is employed experimentally to examine receptor-mediated cardiovascular responses such as hypotension and to assess alterations in dopamine receptor responsiveness induced by chronic exposure regimens
Apexbio Technology LLC Dofetilide 115256-11-6 10mM (in 1mL DMSO)
Dofetilide (CAS 115256-11-6) chemically designated as UK 68789 is a class III antiarrhythmic small molecule that selectively inhibits the rapid delayed rectifier potassium channel (IKr) This inhibition leads to prolonged ventricular action potential duration and extended effective refractory periods in cardiac cells Noted for favorable oral bioavailability Dofetilide is extensively utilized in cardiac electrophysiological research including studies aimed at elucidating arrhythmogenic mechanisms linked to IKr channel function assessing novel antiarrhythmic candidates and exploring physiological and pathological aspects of cardiac rhythm regulation
Apexbio Technology LLC Mitomycin C 10mM (in 1mL DMSO)
Mitomycin C (CAS 50-07-7) is an antibiotic compound derived from Streptomyces caespitosus or Streptomyces lavendulae exhibiting anti-cancer properties by interfering with DNA synthesis Its mode of action involves direct formation of covalent adducts with DNA impeding DNA replication In PC3 cells mitomycin C presents an EC50 of approximately 0 14 M Moreover it can potentiate apoptosis induced by TRAIL (TNF-related apoptosis-inducing ligand) through mechanisms independent of p53 modulating apoptosis-related protein expression and caspase activation Due to its cytotoxic mechanism mitomycin C continues to serve as a useful compound in cancer research particularly in apoptosis signaling studies