Dimethyl Sulfoxide
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 UNC0638 1255580-76-7 10mM (in 1mL DMSO)
UNC0638 is a selective inhibitor of histone methyltransferases G9a and GLP enzymes responsible for mono- and dimethylation of histone H3 lysine-9 (H3K9) It inhibits G9a and GLP activity with IC50 values of 15 nM and 19 nM respectively UNC0638 reduces cellular H3K9 dimethylation levels demonstrated in MDA-MB-231 cells with an IC50 of 81 9 nM at 48 hours It has been utilized in models to study epigenetic regulation including neuroendocrine tumor xenografts and hair cell damage induced by aminoglycosides addressing roles of H3K9 methylation in disease pathogenesis and therapeutic responses
Apexbio Technology LLC Reserpine 50-55-5 10mM (in 1mL DMSO)
Reserpine a naturally derived alkaloid isolated from plants of the genus Rauvolfia functions primarily through the inhibition of vesicular monoamine transporter 2 (VMAT2) By blocking VMAT2-mediated uptake reserpine causes depletion of monoamine neurotransmitters such as dopamine norepinephrine and serotonin from synaptic storage vesicles In biochemical assays reserpine inhibits VMAT2 activity with an IC50 value typically ranging from 30-50 nM depending on assay specifics In biomedical and pharmacological research this compound is commonly utilized to model neurotransmitter depletion mechanisms in vitro and in animal models facilitating studies on monoamine-related neurological disorders neurotransmission pathways as well as serotonergic dopaminergic and adrenergic signaling
Apexbio Technology LLC AZD2461 1174043-16-3 10mM (in 1mL DMSO)
AZD2461 (CAS 1174043-16-3) is a novel small-molecule inhibitor of poly(ADP-ribose) polymerase (PARP) exhibiting potency with an IC50 of 5 nM PARP enzymes are pivotal regulators of DNA repair and apoptosis-associated processes In breast cancer cell lines such as SKBR-3 and MCF-7 AZD2461 reduces cell viability in a concentration- and time-dependent manner arresting cells predominantly in the G2 phase In BRCA1-deficient mouse KB1P tumors AZD2461 disrupts PARP activity regardless of P-glycoprotein-mediated resistance to other inhibitors like olaparib highlighting its utility in overcoming drug resistance and elucidating DNA repair pathways in cancer research
Apexbio Technology LLC Afatinib (BIBW2992) 439081-18-2 10mM (in 1mL DMSO)
Afatinib (BIBW2992 CAS 439081-18-2) is an irreversible inhibitor targeting receptor tyrosine kinases in the ErbB protein family specifically EGFR (ErbB1) and HER2 (ErbB2) By covalently binding to their kinase domains it suppresses downstream ErbB signaling showing demonstrated inhibition with IC50 values of 0 5 nM for EGFR and 14 nM for HER2 Afatinib blocks EGF-induced phosphorylation and cellular proliferation in multiple EGFR- or HER2-expressing lines including A431 NIH-3T3-HER2 NCI-N87 and BT-474 Research applications include tumor xenograft studies and transgenic lung cancer models evaluating EGFR-dependent oncogenic processes and therapeutic responses
Apexbio Technology LLC Carvedilol 72956-09-3 10mM (in 1mL DMSO)
Carvedilol is an antagonist targeting 1- and -adrenergic receptors employed in research on cardiovascular diseases especially congestive heart failure and hypertension Mechanistically carvedilol blocks adrenergic receptor-mediated signaling influencing sympathetic nervous system activity Additionally carvedilol exhibits antioxidative properties in vitro studies demonstrate suppression of Fe2 -induced lipid peroxidation (IC50 8 1 M) protection of -tocopherol depletion due to Fe2 exposure (IC50 17 6 M) and reduction of hydroxyl radical-derived DMPO-OH signals (IC50 25 M) It also inhibits proliferation (IC50 0 3-2 0 M) and migration (IC50 3 M) in vascular smooth muscle cells induced by platelet-derived growth factor supporting investigation of vascular remodeling processes
Apexbio Technology LLC AICAR 10mM (in 1mL DMSO)
A8184 is a small molecule developed primarily as a biomedical research tool It functions through modulation of specific cellular signaling pathways implicated in disease states enabling researchers to probe biological targets and cellular mechanisms By influencing these pathways A8184 provides a methodological approach for dissecting cellular responses and clarifying mechanisms involved in pathological conditions This compound is suited for controlled in vitro studies aimed at elucidating disease pathways and evaluating potential therapeutic avenues in biomedical research contexts
Apexbio Technology LLC EPZ015666 1616391-65-1 10mM (in 1mL DMSO)
EPZ015666 (CAS 1616391-65-1) is a potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) an enzyme implicated in several cellular pathways including tumorigenesis EPZ015666 inhibits PRMT5 with an IC50 of 22 nM and displays a Ki value of approximately 5 nM It exhibits over 20 000-fold selectivity for PRMT5 relative to other protein methyltransferases tested In mantle cell lymphoma (MCL) cell lines treatment with EPZ015666 reduced methylation levels of the PRMT5 substrate SmD3 and exerted concentration-dependent anti-proliferative effects Additionally EPZ015666 demonstrated dose-dependent tumor growth inhibition in mouse xenograft models of MCL highlighting its potential utility as a molecular tool in cancer biology research
Apexbio Technology LLC Linifanib (ABT-869) 796967-16-3 10mM (in 1mL DMSO)
Linifanib (ABT-869 CAS 796967-16-3) is an ATP-competitive inhibitor of receptor tyrosine kinases targeting platelet-derived growth factor (PDGF) and vascular endothelial growth factor receptors (VEGFRs) as well as FMS-like tyrosine kinase 3 (FLT3) including its activating internal tandem duplication (ITD) mutations Linifanib selectively reduces cell growth in FLT3 ITD-expressing cell lines such as Ba/F3 FLT3 ITD cells inhibits phosphorylation of FLT3 and Akt and induces apoptosis preferentially in ITD mutant cells In vivo experiments with ITD-expressing leukemia xenografts show reduced leukemia progression and prolonged survival in mice treated orally with linifanib This compound is widely used in preclinical research for acute myeloid leukemia studies
Apexbio Technology LLC Macitentan 441798-33-0 10mM (in 1mL DMSO)
Macitentan (CAS 441798-33-0) is a small molecule endothelin receptor antagonist acting as a dual inhibitor of ETA and ETB receptors Experimental data using recombinant ETA-expressing CHO cells show that macitentan exhibits potent inhibition of ET-1 ligand binding with an IC50 of approximately 0 5 nM whereas its inhibitory effect on ETB receptors in similar CHO cell systems is weaker (IC50 391 nM) In vivo rodent studies indicate macitentan rapidly converts into ACT-132577 a circulating metabolite with extended half-life and retained dual receptor antagonism This pharmacological profile makes macitentan relevant for biomedical research on endothelin-associated vascular pathologies
Apexbio Technology LLC Empagliflozin (BI 10773) 864070-44-0 10mM (in 1mL DMSO)
Empagliflozin (BI 10773 CAS 864070-44-0) is a potent selective inhibitor targeting sodium-glucose cotransporter 2 (SGLT-2) a transmembrane protein primarily expressed in the kidneys and responsible for glucose reabsorption Empagliflozin inhibits SGLT-2 with an IC50 of 3 1 nM demonstrating high selectivity relative to related transporters (SGLT-1 4 5 and 6) In vitro studies using HK2 human proximal tubular cells showed that empagliflozin suppresses high glucose-induced pro-inflammatory signaling pathways including TLR4 NF- B AP-1 and IL-6 secretion Empagliflozin has been widely studied in diabetic animal models such as Zucker diabetic obese rats effectively reducing blood glucose and increasing urinary glucose excretion supporting its application in diabetes research