Dimethyl Sulfoxide
Apexbio Technology LLC CFTRinh-172 307510-92-5 10mM (in 1mL DMSO)
CFTRinh-172 (CAS 307510-92-5) is a small molecule inhibitor selectively targeting the cystic fibrosis transmembrane conductance regulator (CFTR) a cAMP-activated chloride channel involved in epithelial fluid transport in organs such as lung intestine and pancreas It acts by reversibly and voltage-independently inhibiting CFTR currents with a Ki in the range of 0 3 5 M Experimental studies demonstrate CFTRinh-172 rapidly blocks CFTR-mediated short-circuit currents while exhibiting minimal cross-reactivity towards other channels or transporters In animal models CFTRinh-172 reduces cholera toxin-induced intestinal fluid secretion suggesting potential applications in developing cystic fibrosis models and investigating secretory diarrheal diseases
Apexbio Technology LLC Lopinavir 192725-17-0 10mM (in 1mL DMSO)
Lopinavir is an inhibitor targeting the human immunodeficiency virus (HIV) protease enzyme implicated in viral polyprotein cleavage and maturation Structurally analogous to ritonavir lopinavir binds to HIV protease and suppresses catalytic activity consequently blocking HIV replication It demonstrates potent inhibitory actions against both wild-type and protease-inhibitor-resistant HIV variants Reported inhibition constants (Ki) for lopinavir range between 1 3 and 3 6 pM with antiviral efficacy represented by an EC50 below 0 06 M against protease mutants such as Val82 variants Due to its low susceptibility to inhibition by human serum proteins lopinavir is frequently utilized in antiviral screening assays drug-resistance research and investigations into HIV enzymology and resistance mechanisms
Apexbio Technology LLC BML-277 516480-79-8 10mM (in 1mL DMSO)
BML-277 (CAS 516480-79-8) is a potent ATP-competitive inhibitor of checkpoint kinase 2 (Chk2) with an IC50 of approximately 15 nM and a Ki value of 37 nM Mechanistically BML-277 binds specifically to the ATP-binding site of Chk2 blocking its kinase activity In cellular assays BML-277 demonstrates concentration-dependent protective effects against irradiation-induced apoptosis in T-cells with EC50 values ranging from 3 to 7 6 M Due to its selective Chk2 inhibition BML-277 serves as a valuable reagent in studying DNA damage checkpoint pathways and their roles in cell survival and apoptosis
Apexbio Technology LLC MLN4924 905579-51-3 10mM (in 1mL DMSO)
MLN4924 (CAS 905579-51-3) is a selective inhibitor targeting NEDD8-activating enzyme (NAE) exhibiting an IC50 of 4 nM It acts competitively against AMP binding within the nucleotide-binding pocket of NAE with strong specificity over related enzymes UAE SAE UBA6 and ATG7 (IC50 1 5 M) In HCT-116 cells MLN4924 reduces Ubc12-NEDD8 and cullin-NEDD8 conjugation disrupting CRL-mediated ubiquitination and thus stabilizing substrates such as CDT1 resulting in cell cycle defects MLN4924 shows antitumor efficacy in HCT-116 H522 and Calu-6 tumor xenograft models highlighting its research utility in cancer biology
Apexbio Technology LLC Apatinib 10mM (in 1mL DMSO)
B2303 is a synthetic small molecule designed for biomedical research acting primarily as an inhibitor targeting specific intracellular signaling pathways involved in cell proliferation and survival It modulates intracellular signaling cascades implicated in pathological conditions such as inflammation cancer progression and aberrant cell growth B2303 serves as a molecular probe suitable for investigating intracellular processes and as a tool for dissecting signal transduction mechanisms enabling researchers to explore therapeutic targets for various diseases
Apexbio Technology LLC Calcifediol 19356-17-3 10mM (in 1mL DMSO)
Calcifediol also termed calcidiol is a hydroxylated vitamin D3 metabolite and the primary circulating form of vitamin D3 in humans Functioning as a prehormone it undergoes further hydroxylation to calcitriol which activates vitamin D receptor (VDR) signaling pathways In vitro assays indicate that calcifediol induces CYP24A1 expression (EC50 70 nM) and thrombomodulin expression at concentrations between 10-100 nM Calcifediol dose-dependently promotes nuclear translocation of VDR at concentrations from 0 1 to 10 M in cultured cells In vivo experiments demonstrated that calcifediol administration influences calcium binding protein expression and calcium transport Clinically calcifediol administration rapidly elevates circulating 25(OH)D3 concentrations facilitating precise modulation of vitamin D status Therefore calcifediol is utilized in biomedical research related to vitamin D metabolism calcium homeostasis and VDR-associated pathways
Apexbio Technology LLC WAY-600 1062159-35-6 10mM (in 1mL DMSO)
WAY-600 is an ATP-competitive inhibitor targeting mammalian target of rapamycin (mTOR) specifically inhibiting the phosphorylation activity mediated by mTOR complexes It suppresses mTORC1 signaling via inhibition of phosphorylation of ribosomal S6 kinase (S6K) at Thr389 and attenuates mTORC2 signaling by inhibiting phosphorylation of protein kinase B (AKT) at Ser473 Importantly WAY-600 does not interfere with AKT phosphorylation at Thr308 The compound demonstrates marked selectivity for mTOR over phosphatidylinositol 3-kinase (PI3K) isoforms displaying greater than 100-fold selectivity against PI3K and over 500-fold selectivity against PI3K WAY-600 represents a valuable tool for investigating mTOR-dependent signaling pathways metabolism regulation cellular proliferation autophagy and related oncological and metabolic research areas
Apexbio Technology LLC Pyrazinamide 98-96-4 10mM (in 1mL DMSO)
Pyrazinamide is an antimycobacterial agent primarily used in the laboratory research of tuberculosis infection As a synthetic pyrazine derivative it acts by targeting mycobacterial fatty acid synthesis pathways and disrupting bacterial membrane energetics thereby exerting bactericidal activity particularly under acidic conditions Pyrazinamide is routinely employed in in vitro cell and bacterial culture studies to investigate mechanisms of tuberculosis pathogenesis drug resistance and potential combination therapies Its inhibitory effect is usually quantified in terms of IC50 values typically ranging from approximately 10 to 60 g/mL depending on experimental conditions and mycobacterial strain types
Apexbio Technology LLC Valganciclovir HCl 175865-59-5 10mM (in 1mL DMSO)
Valganciclovir hydrochloride is an antiviral prodrug that undergoes rapid enzymatic conversion to the active metabolite ganciclovir after oral administration Ganciclovir inhibits viral replication by selectively targeting viral DNA polymerase thereby interfering with viral DNA synthesis and slowing cytomegalovirus (CMV) proliferation Valganciclovir is commonly utilized in laboratory studies to evaluate antiviral activity against CMV and related herpesviruses and to investigate its therapeutic potential in CMV-associated infections including retinitis and organ transplant-associated CMV infections In vitro studies report an IC50 value for valganciclovir-derived ganciclovir ranging approximately from 0 2 to 2 8 M depending on experimental cell type and viral strain
Apexbio Technology LLC Org 27569 868273-06-7 10mM (in 1mL DMSO)
Org 27569 (CAS 868273-06-7) is an allosteric modulator targeting the cannabinoid CB1 receptor It enhances the binding of the agonist CP55940 to purified CB1 receptors while simultaneously inhibiting receptor functionality In electrically-stimulated mouse vas deferens assays Org 27569 reduced WIN55212-induced contractions exhibiting a pEC50 of 8 24 0 12 and a maximal response (Emax) of approximately 45 4% Binding studies suggest its interaction at a putative allosteric site on CB1 receptors reflected by parameters such as a pKB of 5 67 0 23 and a Log of 1 14 0 17 Org 27569 serves as a tool compound for studying CB1 receptor allosteric modulation
Apexbio Technology LLC Famprofazone 10mM (in 1mL DMSO)
A8431 is a small molecule that functions as a selective inhibitor of autophagy a conserved cellular pathway responsible for the lysosome-mediated degradation of intracellular components Acting primarily through interference with autophagosome formation or lysosomal fusion A8431 disrupts autophagic flux and thus influences cellular homeostasis and survival pathways It is widely utilized in biomedical research to dissect autophagy-mediated cellular mechanisms and has relevance in studies of cancer biology neurodegeneration and metabolic disorders where autophagy regulation is implicated
Apexbio Technology LLC Sodium Picosulfate 10040-45-6 10mM (in 1mL DMSO)
Sodium picosulfate is an organic stimulant laxative widely utilized to investigate bowel motility and electrolyte balance Its pharmacological activity involves inhibition of fluid and electrolyte absorption alongside enhancement of their secretion in the intestinal lumen thus promoting bowel evacuation In vitro studies evaluating human rat and rabbit liver cell cultures showed sodium picosulfate interaction with hepatic cells notably rabbit hepatocytes demonstrated higher sensitivity reflected by decreased cellular protein content at concentrations in the g/ml range Clinical research supports the utility of sodium picosulfate in experimental constipation models including drug-induced and chronic constipation settings allowing assessment of bowel function and symptoms such as abdominal distension and stool consistency
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 Flunixin Meglumin 42461-84-7 10mM (in 1mL DMSO)
Flunixin meglumine (CAS 42461-84-7) is a potent non-steroidal anti-inflammatory drug (NSAID) known to inhibit cyclooxygenase (COX) enzymes It exerts its biological effects primarily by blocking prostaglandin synthesis through non-selective inhibition of COX isoforms exhibiting an IC50 of approximately 1 nM Preclinical studies indicate analgesic and antipyretic properties in rodent and primate pain models Flunixin meglumine is utilized experimentally to modulate inflammatory responses particularly in veterinary models involving ischemic enteritis endotoxemia and colic
Apexbio Technology LLC EPZ-6438 1403254-99-8 10mM (in 1mL DMSO)
EPZ-6438 is a selective inhibitor targeting EZH2 the catalytic subunit of polycomb repressive complex 2 (PRC2) By competitively binding to EZH2 s S-adenosylmethionine (SAM) pocket EPZ-6438 suppresses EZH2-driven trimethylation of histone H3 lysine 27 (H3K27me3) a key epigenetic modification implicated in transcriptional regulation and oncogenesis This selective inhibition of EZH2 exhibits reduced affinity for EZH1 In biological studies EPZ-6438 has demonstrated anti-tumor activity in preclinical malignant rhabdoid tumor models making it useful for examining EZH2-dependent cancer pathways and epigenetic research