Dimethyl Sulfoxide
Apexbio Technology LLC TWS119 601514-19-6 10mM (in 1mL DMSO)
TWS119 (CAS 601514-19-6) is a selective inhibitor of glycogen synthase kinase-3 (GSK-3 ) exhibiting an IC50 of approximately 30 nM Originally identified from a library of pyrrolopyrimidine-based compounds TWS119 binds GSK-3 with a Kd value around 126 nM By inhibiting GSK-3 activity TWS119 modulates downstream transcriptional events promoting neuronal differentiation in murine embryonic carcinoma (P19) and mouse embryonic stem cells through mechanisms distinct from classical Wnt signaling Due to this property TWS119 serves as a useful tool for research in neural differentiation and regenerative medicine
Apexbio Technology LLC Edaravone 89-25-8 10mM (in 1mL DMSO)
Edaravone (CAS 89-25-8) is a small-molecule antioxidant and free radical scavenger that mitigates cell injury primarily by intercepting reactive oxygen species and suppressing oxidative stress responses Its cytoprotective mechanism has been linked to the inhibition of lipid peroxidation pathways potentially involving suppression of lipoxygenase activity Edaravone has been investigated for neuroprotective effects notably demonstrating protection against neurotoxicity induced by MPTP a well-established model to study Parkinson s disease pathology This compound serves as a significant research tool for examining oxidative injury in ischemic and neurodegenerative conditions
Apexbio Technology LLC Roflumilast 162401-32-3 10mM (in 1mL DMSO)
Roflumilast is an orally available selective inhibitor of phosphodiesterase-4 (PDE-4) with an IC50 value of approximately 0 11 nM PDE-4 enzymes catalyze the hydrolysis of cyclic adenosine monophosphate (cAMP) and are predominantly expressed in various inflammatory and immune cells By selectively inhibiting PDE-4 activity Roflumilast elevates intracellular cAMP levels thus regulating cellular inflammatory signaling pathways This mechanism supports its use in the reduction of inflammatory responses associated with chronic obstructive pulmonary disease (COPD) Additionally Roflumilast has been investigated experimentally regarding its potential influence on glucose metabolism in early-stage type 2 diabetes mellitus
Apexbio Technology LLC AT9283 896466-04-9 10mM (in 1mL DMSO)
AT9283 (CAS 896466-04-9) is a synthetic small-molecule inhibitor developed through fragment-based drug design It inhibits Aurora kinases A and B key components of the serine/threonine kinase family involved in regulating cell division processes as well as targets including Janus kinases (JAKs) BCR-ABL kinase (including the T315I mutant) and Flt-3 With a potent IC50 around 3 nM against Aurora kinases AT9283 exhibits antiproliferative and pro-apoptotic activity in leukemia myeloproliferative diseases solid tumors and B-cell lymphoma models It is utilized primarily in cancer biology research to investigate its therapeutic potential targeting aberrant kinase activity
Apexbio Technology LLC Dacomitinib (PF299804, PF299) 1110813-31-4 10mM (in 1mL DMSO)
Dacomitinib (PF299804 CAS 1110813-31-4) is an irreversible pan-HER small-molecule inhibitor that targets the epidermal growth factor receptor (EGFR/ErbB-1) ERBB2 (HER2) and ERBB4 (HER4) It acts by covalently binding EGFR family tyrosine kinases inhibiting downstream signaling through phospho-HER family proteins AKT and ERK Dacomitinib shows activity in vitro inducing G0/G1 cell cycle arrest and apoptosis and suppresses proliferation in trastuzumab- or lapatinib-resistant HER2-amplified breast cancer cell lines In vivo studies demonstrate antitumor effects in EGFR-mutant (e g T790M) gefitinib-resistant lung cancer xenografts making it relevant for non-small cell lung cancer research
Apexbio Technology LLC Pioglitazone HCl 112529-15-4 10mM (in 1mL DMSO)
Pioglitazone HCl is a potent and highly selective agonist of the peroxisome proliferator-activated receptor gamma (PPAR ) a nuclear receptor involved in glucose and lipid metabolism regulation Acting via PPAR activation pioglitazone increases insulin sensitivity in hepatic adipose and peripheral tissues enhancing insulin-mediated glucose uptake and utilization Pioglitazone requires the presence of insulin to exert its biological activity through receptor activation limiting its application in scenarios characterized by substantial insulin deficiency Clinically pioglitazone HCl has been widely applied in the management and investigation of hyperglycemia associated with type 2 diabetes mellitus (T2DM) Additionally pioglitazone demonstrates effects on lipid regulation notably reducing triglyceride levels and increasing high-density lipoprotein (HDL) cholesterol making it useful in metabolic research
Apexbio Technology LLC CYT387 1056634-68-4 10mM (in 1mL DMSO)
CYT387 (CAS 1056634-68-4) is an aminopyrimidine derivative identified through high-throughput screening and optimized with structure-guided medicinal chemistry It functions as an inhibitor targeting Janus kinase family enzymes JAK1 JAK2 JAK3 and TYK2 with reported IC50 values of 11 nM 18 nM 155 nM and 17 nM respectively At concentrations between 500 1500 nM CYT387 selectively suppresses JAK2 signaling inhibits proliferation of JAK2-dependent hematopoietic cell lines and induces apoptosis with minimal effects on non-hematopoietic cells CYT387 is employed in experimental studies of JAK2-mediated signaling pathways and myeloproliferative neoplasms
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 Zafirlukast 107753-78-6 10mM (in 1mL DMSO)
Zafirlukast (CAS 107753-78-6) is an antagonist targeting cysteinyl leukotriene receptors (CysLTR) which mediate inflammatory signaling pathways By competitively inhibiting leukotriene receptor binding it disrupts the leukotriene-driven inflammatory response Zafirlukast demonstrates antagonist potency against leukotriene receptors with an IC50 value of approximately 0 6 M and exhibits moderate inhibitory activity on CYP2C9 enzyme (IC50 of about 7 0 M) In biomedical research Zafirlukast serves as a pharmacological tool for studying leukotriene-mediated inflammation and receptor signaling processes
Apexbio Technology LLC GW0742 317318-84-6 10mM (in 1mL DMSO)
GW0742 is a synthetic selective agonist of peroxisome proliferator-activated receptor / (PPAR / ) a ligand-dependent transcription factor involved in regulating lipid metabolism inflammation and energy homeostasis Activation of PPAR / modulates downstream gene transcription influencing physiological processes including inflammatory responses and neuronal protection Experimental studies demonstrate GW0742 s role in attenuating inflammation-mediated tissue injury such as ischemia/reperfusion-induced intestinal damage as well as mitigating radiation-induced neuroinflammation and cognitive impairment in animal models Thus GW0742 serves as a research tool to study PPAR / specific pathways in inflammatory diseases metabolic processes and neuroprotective mechanisms
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 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 Trichostatin A (TSA) 58880-19-6 10mM (in 1mL DMSO)
Trichostatin A (TSA CAS 58880-19-6) is a histone deacetylase (HDAC) inhibitor and antifungal antibiotic isolated from microbial sources TSA acts by reversibly inhibiting HDAC enzymes in a noncompetitive manner leading to increased acetylation of histones particularly histone H4 In mammalian cell cultures TSA treatment results in G1 and G2 phase arrest induction of differentiation and reversion of transformed cellular phenotypes In human breast cancer cell lines TSA inhibits proliferation (IC50 124 4 120 4 nM) and induces hyperacetylation of histone proteins highlighting its utility as a tool compound for investigating epigenetic regulation and oncology-related mechanisms
Apexbio Technology LLC Rivaroxaban 366789-02-8 10mM (in 1mL DMSO)
Rivaroxaban (CAS 366789-02-8) is a small molecule inhibitor targeting coagulation Factor Xa a serine protease essential in the thrombin generation pathway involved in clot formation It binds reversibly to the S1 pocket of Factor Xa engaging specifically through interactions between its chlorothiophene moiety and the Tyr288 residue Binding kinetics are rapid (kon 1 7 10 7 mol L 1 s 1 koff 5 10 3 s 1) and affinity is high (Ki 0 4 nmol/L) Rivaroxaban is studied extensively in thrombosis research including venous thromboembolism stroke prevention in atrial fibrillation and cardiovascular event management post-acute coronary syndrome
Apexbio Technology LLC Acetaminophen 103-90-2 10mM (in 1mL DMSO)
Acetaminophen (paracetamol) is a cyclooxygenase-2 (COX-2) inhibitor widely employed in biomedical studies for investigating analgesic and antipyretic mechanisms Its inhibition of COX-2 enzyme activity occurs with an IC50 of approximately 25 8 M Experimental use includes inducing cellular hepatotoxicity models where acetaminophen exposure triggers glutathione depletion impaired glutathione peroxidase activity and ferroptosis-mediated cell death This makes acetaminophen useful in examining oxidative stress hepatic cell injury and associated cellular response mechanisms in vitro and in animal studies Additionally acetaminophen-mediated toxicity is applicable in screening protective agents or evaluating ferroptosis inhibitors in pharmacological research