Dimethyl Sulfoxide
Apexbio Technology LLC Enrofloxacin 93106-60-6 10mM (in 1mL DMSO)
Enrofloxacin a fluoroquinolone antibiotic exerts antibacterial activity by inhibiting bacterial DNA gyrase and topoisomerase IV enzymes essential for DNA replication and transcription This mechanism disrupts the DNA synthesis of pathogenic bacteria resulting in bacteriostatic outcomes In vitro experiments indicate that Enrofloxacin displays antimicrobial activity against Mycoplasma species such as Mycoplasma bovis with a minimum inhibitory concentration (MIC90) around 0 312 g/mL In biomedical research this compound is primarily utilized to establish microbial infection models and to study bacterial resistance mechanisms pharmaceutical efficacy and antibacterial pharmacodynamics
Apexbio Technology LLC Probenecid 57-66-9 10mM (in 1mL DMSO)
Probenecid is an inhibitor targeting organic anion transporters multidrug resistance-associated proteins (MRPs) and pannexin-1 channels showing an IC50 of 150 M for pannexin-1 inhibition MRPs a class of ATP-binding cassette (ABC) transporters mediate efflux of diverse molecules across cellular membranes contributing to drug resistance Probenecid counteracts MRP-mediated drug resistance in multidrug-resistant tumor cell lines enhancing cellular sensitivity to chemotherapeutic agents like daunorubicin and vincristine In animal research Probenecid protects neurons against ischemia/reperfusion-induced injury suppressing inflammation-associated enzyme activity and reducing glial cell activation
Apexbio Technology LLC Moclobemide (Ro 111163) 71320-77-9 10mM (in 1mL DMSO)
Moclobemide (Ro 111163 CAS 71320-77-9) is a reversible inhibitor of monoamine oxidase A (MAO-A) with a reported IC50 of approximately 10 M In vitro studies using rat brain homogenate indicate that it selectively targets MAO-A over MAO-B though with moderate potency Animal experiments demonstrate up to 80% inhibition of MAO-A activity in brain and liver tissues upon administration Prolonged high-dose exposure to Moclobemide alters adrenergic receptor profiles by downregulating -adrenergic receptors and enhancing affinity of 1-adrenergic agonist binding Due to its MAO-A specificity this compound serves as a prototype reversible inhibitor (RIMA) with relevance in antidepressant drug research
Apexbio Technology LLC GSK2334470 1227911-45-6 10mM (in 1mL DMSO)
GSK2334470 (CAS 1227911-45-6) is a highly selective inhibitor of 3-phosphoinositide-dependent protein kinase-1 (PDK1) demonstrating an IC50 of approximately 10 nM It specifically blocks PDK1-mediated phosphorylation of substrate proteins including Akt1 S6K1 and SGK isoforms inhibiting their T-loop phosphorylation sites GSK2334470 does not significantly inhibit other tested protein or lipid kinases This compound facilitates mechanistic research into signaling pathways regulated by PDK1 particularly those involving Akt and downstream effectors in cellular contexts
Apexbio Technology LLC Fidaxomicin 873857-62-6 10mM (in 1mL DMSO)
Fidaxomicin is a macrocyclic antibiotic derived from Actinomycetes functioning through inhibition of bacterial RNA polymerase by targeting the -subunit thereby interfering with bacterial RNA synthesis It exhibits specific antibacterial effects against Clostridium difficile suppressing toxin production and reducing disease recurrence in Clostridium difficile infections (CDI) Fidaxomicin has entered phase III clinical investigation for treatment of CDI Experimental results indicate an intravenous LD50 of approximately 200 mg/kg in rats reported inhibitory concentrations (IC50) against C difficile RNA polymerase range in the nanomolar scale It is utilized in research for studying bacterial transcription mechanisms and evaluating treatment strategies aimed at CDI
Apexbio Technology LLC Nicardipine HCl 54527-84-3 10mM (in 1mL DMSO)
Nicardipine HCl (CAS 54527-84-3) is a dihydropyridine-derived small molecule that functions primarily as a calcium-channel blocker through inhibition of voltage-dependent L-type calcium channels This mechanism prevents calcium ion influx causing vasodilation and decreased vascular resistance Widely applied in vascular biology and pharmacological research nicardipine hydrochloride serves as a useful tool to explore calcium-dependent processes cardiovascular pathophysiology and therapeutic strategies targeting calcium-mediated vascular conditions
Apexbio Technology LLC PF-477736 952021-60-2 10mM (in 1mL DMSO)
PF-477736 is an ATP-competitive small-molecule inhibitor of checkpoint kinase 1 (Chk1) It selectively inhibits Chk1 kinase activity demonstrating nanomolar inhibitory potency in kinase assays and exhibits lower affinity toward related kinases such as CDK1 and Chk2 In vitro studies utilizing human cancer cell lines show PF-477736 disrupts Chk1-dependent G2-phase cell-cycle arrest induced by DNA-damaging agents preferentially targeting tumor cells with compromised p53 function while minimizing cytotoxicity to normal cells PF-477736 is widely utilized experimentally to study DNA damage response mechanisms potential chemosensitizing effects and therapeutic implications for cancers harboring p53 mutations
Apexbio Technology LLC Azaguanine-8 134-58-7 10mM (in 1mL DMSO)
Azaguanine-8 (CAS 134-58-7) is a synthetic purine analog utilized in biomedical research due to its antineoplastic properties Structurally similar to guanine Azaguanine-8 exerts its biological activity by competitively interfering with guanine metabolism subsequently disrupting nucleic acid synthesis and cellular replication pathways Through this mechanism the compound demonstrates inhibitory effects on cell proliferation making it a valuable tool in investigating nucleic acid metabolism and cancer biology in preclinical studies
Apexbio Technology LLC MHY1485 326914-06-1 10mM (in 1mL DMSO)
MHY1485 (CAS 326914-06-1) is a potent activator of mammalian target of rapamycin (mTOR) a serine/threonine kinase critical for cellular growth metabolism and survival pathways By activating mTOR signaling MHY1485 inhibits autophagy initiation and disrupts the fusion step between autophagosomes and lysosomes resulting in accumulation of autophagic marker LC3-II and enlarged autophagic structures In cultured rat Ac2F hepatic cells MHY1485 suppresses basal and starvation-induced autophagic flux Additionally MHY1485 treatment promotes ovarian follicular development and increases explant growth in mouse ovarian culture models providing a useful tool in biomedical research of mTOR signaling and reproductive biology
Apexbio Technology LLC Rocilinostat (ACY-1215) 1316214-52-4 10mM (in 1mL DMSO)
Rocilinostat (ACY-1215 CAS 1316214-52-4) is a selective inhibitor of histone deacetylase 6 (HDAC6) HDAC6 enzymatically regulates various cellular processes including protein trafficking cell-cycle progression and cytoskeletal organization and its dysregulated activity is implicated in tumor progression and cancer metastasis Rocilinostat potently inhibits HDAC6 (IC50 5 nM) while showing minimal activity against other HDAC isoforms and sirtuins (IC50 1 M) Preclinical studies using multiple myeloma (MM) cell lines and xenograft mouse models demonstrated rocilinostat can enhance acetylation of -tubulin disrupt protein stability pathways and sensitize cancer cells to proteasome inhibitors such as bortezomib and carfilzomib resulting in increased apoptosis and reduction in tumor growth
Apexbio Technology LLC Z-IETD-FMK 210344-98-2 10mM (in 1mL DMSO)
Z-IETD-FMK (CAS 210344-98-2) is a cell-permeable peptide-derived inhibitor targeting caspase-8 It reduces T-cell proliferation induced by stimuli such as phytohemagglutinin (PHA) or anti-CD3/anti-CD28 antibodies primarily through downregulation of CD25 expression without affecting IL-2 or IFN- secretion Additionally Z-IETD-FMK inhibits NF- B activation at higher concentrations (100 M) Studies also demonstrate its protective effects against TRAIL-induced apoptosis by inhibiting processing of procaspases-2 -3 -9 and PARP cleavage in cancer cell lines such as HCT116 and SW480
Apexbio Technology LLC GDC-0032 1282512-48-4 10mM (in 1mL DMSO)
GDC-0032 (CAS 1282512-48-4) is a benzofused small-molecule inhibitor targeting PI3K with high potency and selectivity It demonstrates strong inhibitory activity against PI3K PI3K and PI3K with IC50 values of 0 29 nM 0 91 nM and 0 97 nM respectively and notably exhibits greater selectivity towards PI3K In vitro GDC-0032 effectively inhibits cell proliferation and cellular function showing EC50 values of 25 nM (MCF7 cells) and 571 nM (PC3 cells) with corresponding IC50 values of 4 nM and 31 nM In vivo experiments indicate antitumor activity in MCF7-neo/Her2 xenograft models GDC-0032 serves as a valuable tool compound for PI3K-related oncology research
Apexbio Technology LLC Prucalopride 179474-81-8 10mM (in 1mL DMSO)
Prucalopride (CAS 179474-81-8) is a selective serotonin 5-HT4 receptor agonist with high affinity for both 5-HT4A and 5-HT4B receptor subtypes demonstrating Ki values of 2 5 nM and 8 nM respectively It displays substantial selectivity exceeding 290-fold against other serotonin receptor classes By activating 5-HT4 receptors prucalopride promotes gastrointestinal motility making it a valuable tool compound for investigating serotonergic mechanisms underlying gastrointestinal disorders and motility regulation Currently prucalopride is evaluated in Phase 3 clinical trials
Apexbio Technology LLC GSK 650394 890842-28-1 10mM (in 1mL DMSO)
GSK 650394 is a small-molecule inhibitor selectively targeting serum- and glucocorticoid-regulated kinase 1 (SGK1) showing inhibition through competitive binding mechanism with an IC50 of approximately 13 nM in fluorescence polarization assays SGK1 functions as an androgen-regulated kinase inhibition of this signaling reduces androgen-driven growth in prostate cancer cell lines Experimental studies demonstrate that GSK 650394 blocks SGK1 and SGK2 kinase activity with IC50 values of 62 nM and 103 nM respectively assessed by scintillation proximity assays Additionally GSK 650394 reduces androgen-induced phosphorylation of SGK substrate Nedd4-2 and suppresses androgen-stimulated proliferation of prostate cancer LNCaP cells (IC50 1 M) suggesting its use in prostate cancer research as a potential therapeutic strategy
Apexbio Technology LLC Epinephrine HCl 55-31-2 10mM (in 1mL DMSO)
Epinephrine hydrochloride is an adrenergic receptor agonist functioning as both a hormone and neurotransmitter Structurally epinephrine hydrochloride is the hydrochloride salt form of epinephrine facilitating receptor binding and signal transduction mediated by adrenergic receptor subtypes ( and ) Upon receptor activation it initiates downstream signaling pathways through G-protein-coupled mechanisms influencing intracellular second messengers such as cAMP calcium influx and protein kinase activity In biomedical research epinephrine hydrochloride serves as a pharmacological tool for investigating adrenergic receptor-mediated physiological responses including cardiac function modulation bronchodilation metabolic processes and vasoconstriction Its controlled application aids in studying sympathetic nervous system mechanisms cellular signaling cascades cardiovascular pharmacology and stress response frameworks