Dimethyl Sulfoxide
Apexbio Technology LLC KPT-185 1333151-73-7 10mM (in 1mL DMSO)
KPT-185 (CAS 1333151-73-7) is an irreversible selective inhibitor of chromosome region maintenance 1 (CRM1) a nuclear export receptor essential for nuclear-cytoplasmic transport KPT-185 binds covalently at Cys528 of CRM1 thereby inhibiting CRM1-mediated nuclear export of tumor suppressor proteins Studies demonstrate that KPT-185 impairs proliferation and colony formation in acute myeloid leukemia (AML) cell lines exhibiting IC50 values ranging from 100 500 nM inducing G1 cell cycle arrest apoptosis and differentiation of AML blasts Additionally KPT-185 reduces growth and promotes apoptosis in pancreatic cancer models (Colo-357 HPAC BxPC-3) highlighting its potential in cancer research
Apexbio Technology LLC Zebularine 3690-10-6 10mM (in 1mL DMSO)
Zebularine (CAS number 3690-10-6) is a chemically stable cytidine analog containing a 2-(1H)-pyrimidinone ring structure It acts primarily through inhibition of DNA methylation by forming covalent complexes with DNA methyltransferases Zebularine treatment leads to demethylation and reactivation of hypermethylation-mediated silenced genes exemplified by the p16 gene Additionally induced myogenic differentiation has been observed upon zebularine administration in 10T1/2 cells Zebularine displays minimal cytotoxicity in certain cell models such as T24 cells and retains stability in aqueous solutions across a broad pH range (up to pH 12) These properties make zebularine relevant for studies in epigenetic regulation and cellular differentiation
Apexbio Technology LLC Purmorphamine 483367-10-8 10mM (in 1mL DMSO)
Purmorphamine (CAS 483367-10-8) is a synthetic small molecule agonist targeting the Smoothened (Smo) protein a critical component of the Hedgehog (Hh) signaling pathway By binding and activating Smo Purmorphamine induces downstream modulation of key pathway targets such as Gli1 and Patched In vitro studies demonstrated activation with an IC50 value of approximately 1 5 M during competitive assays with the antagonist cyclopamine and an EC50 of about 1 M for alkaline phosphatase (ALP) expression in C3H10T1/2 multipotent cells This agent has been applied in research contexts for inducing osteogenic differentiation with implications for studying bone regeneration and neural degeneration processes
Apexbio Technology LLC IWR-1-endo 1127442-82-3 10mM (in 1mL DMSO)
IWR-1-endo (CAS 1127442-82-3) is a synthetic small-molecule antagonist of the Wnt/ -catenin signaling pathway It inhibits the activity of WNT1 2 and 3 ligands preventing downstream -catenin accumulation by stabilizing Axin-based degradation complexes and disrupting signaling events mediated via LRP6 and DVL2 Experimentally IWR-1-endo suppresses processes dependent on Wnt/ -catenin activity such as tissue regeneration and epithelial stem cell self-renewal demonstrated notably in zebrafish tailfin regeneration models Additionally it reduces abnormal proliferation induced by APC loss in cancer cell lines highlighting its relevance in oncogenesis research
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 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 (-)-Huperzine A 102518-79-6 10mM (in 1mL DMSO)
(-)-Huperzine A (CAS 102518-79-6) known as HupA is an alkaloid compound serving as an inhibitor of acetylcholinesterase (AChE) with an IC50 value of 82 nmol/L By suppressing AChE activity HupA reduces the enzymatic breakdown of neurotransmitter acetylcholine potentially alleviating symptoms associated with Alzheimer s disease Furthermore HupA acts as a non-competitive antagonist at NMDA receptors attenuating NMDA-induced currents in rat hippocampal neurons Studies demonstrate sustained AChE inhibition lasting up to 360 minutes following systemic administration Consequently HupA has significant applications in neuropharmacological research targeting cognitive disorders and neuroprotection
Apexbio Technology LLC Clofazimine 2030-63-9 10mM (in 1mL DMSO)
Clofazimine is a rhimophenazine compound with demonstrated antimicrobial and anti-inflammatory properties commonly utilized in biomedical research related to tuberculosis treatment and drug-resistance studies It functions primarily through the intercalation into bacterial DNA interfering with microbial DNA replication and transcription processes Furthermore it may induce bacterial phospholipid membrane disruption and modulate inflammatory responses Experimental studies report IC50 values in the micromolar range against Mycobacterium tuberculosis strains Clofazimine is frequently employed as a reference compound in antimicrobial assays mechanistic studies on DNA-targeting agents and evaluations of cellular inflammatory pathways within infectious disease model systems
Apexbio Technology LLC Ondansetron hydrochloride dihydrate 103639-04-9 10mM (in 1mL DMSO)
Ondansetron hydrochloride dihydrate (CAS 103639-04-9) is a small molecule antagonist targeting the serotonin (5-HT3) receptor a ligand-gated ion channel prominent in the central and peripheral nervous systems Through blockade of 5-HT3 receptor signaling ondansetron inhibits serotonin-induced emetic responses Due to this mechanism it is widely utilized in biomedical research investigating serotonin-related signaling pathways and nausea mechanisms particularly in contexts involving chemotherapy-induced emesis
Apexbio Technology LLC Tianeptine sodium(Synonyms: Stablon, Coaxil, Tatinol, Tianeurax, Salymbra, Tianeptine Sodium Salt), 10mM (in 1mL DMSO), CAS: 30123-17-2.
Tianeptine sodium (CAS 30123-17-2) is a small molecule known to selectively facilitate serotonin (5-HT) uptake in both in vitro and in vivo experimental models It exhibits minimal affinity toward various neurotransmitter receptors including serotonin and dopamine receptors (IC 10 M) and does not affect the uptake mechanisms of noradrenaline or dopamine Due to its distinct serotonergic modulation tianeptine sodium is extensively used in neuroscience research particularly in studies investigating the molecular basis and therapeutic potential of antidepressants
Apexbio Technology LLC Orlistat(Synonyms: Xenical, Alli, tetrahydrolipstatin, THL, Roche Xenical, lipase inhibitor, (-)-tetrahydrolipstatin), 10mM (in 1mL DMSO), CAS: 96829-58-2.
Orlistat (CAS 96829-58-2) also referred to as tetrahydrolipstatin is a synthetic derivative of lipstatin originally isolated from Streptomyces toxytricini This small molecule specifically inhibits gastrointestinal lipases particularly pancreatic lipase impeding enzymatic hydrolysis of dietary triglycerides and consequently decreasing intestinal absorption of fat Due to its targeted lipase inhibition Orlistat is widely studied in obesity-related metabolic research and lipid metabolism investigations providing a valuable experimental tool for evaluating effects of reduced dietary fat uptake and downstream physiological responses
Apexbio Technology LLC Pepstatin A 26305-03-3 10mM (in 1mL DMSO)
Pepstatin A is a pentapeptide functioning as an inhibitor targeting aspartic proteases including pepsin renin HIV protease and cathepsin D It inhibits human renin and HIV protease with IC50 values of approximately 15 M and 2 M respectively and shows inhibitory activity toward pepsin and cathepsin D at IC50 values below 5 M and 40 M Mechanistically Pepstatin A acts through binding to the catalytic site of aspartic proteases restricting proteolytic activity In biomedical research it is utilized to study viral protein processing osteoclast differentiation mediated by cathepsins and as a standard tool in enzyme inhibition assays examining aspartic protease function
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
Apexbio Technology LLC PTC-209 315704-66-6 10mM (in 1mL DMSO)
PTC-209 (CAS 315704-66-6) is a small-molecule inhibitor targeting BMI-1 identified through Gene Expression Modulation by Small molecules (GEMS) technology It acts by suppressing BMI-1 expression at the transcriptional level displaying an IC50 of approximately 0 5 M In HCT116 cells PTC-209 reduces both UTR-mediated and endogenous BMI-1 expression It selectively restricts cell proliferation in certain tumor and stem cell types including U937 HT1080 and human hematopoietic stem cells without affecting viability in cell lines such as HEK293 and HT1080 Thus PTC-209 is primarily utilized in studies exploring cancer stem cell growth and oncogenesis involving BMI-1 and the PRC1 complex