Dimethyl Sulfoxide
Apexbio Technology LLC WZ4003 1214265-58-3 10mM (in 1mL DMSO)
WZ4003 (CAS 1214265-58-3) is a selective inhibitor targeting NUAK1 and NUAK2 kinases members of the AMP-activated protein kinase (AMPK) family activated by tumor suppressor kinase LKB1 WZ4003 inhibits NUAK1 and NUAK2 with IC50 values of 20 nM and 100 nM respectively In cellular assays treatment with WZ4003 reduces NUAK1-mediated phosphorylation of MYPT1 at Ser445 It suppresses cell proliferation migration of mouse embryonic fibroblasts and invasion of U2OS cells Thus WZ4003 serves as a valuable tool for investigating NUAK kinase functions in cell proliferation mobility and signaling mechanisms relevant to oncology research
Apexbio Technology LLC Tadalafil 171596-29-5 10mM (in 1mL DMSO)
Tadalafil (CAS 171596-29-5) also known as IC351 is a selective inhibitor of phosphodiesterase type 5 (PDE5) a primary phosphodiesterase isoenzyme responsible for hydrolyzing cyclic guanosine monophosphate (cGMP) in pulmonary vasculature By competitively and reversibly inhibiting PDE5 tadalafil elevates intracellular cGMP levels thereby inducing vasodilation and attenuating pathological pulmonary arterial constriction Due to high selectivity tadalafil shows minimal inhibition of other PDE isoforms such as PDE1 PDE4 PDE6 PDE7 PDE8 PDE9 and PDE10 It is commonly studied in pulmonary arterial hypertension research and utilized clinically for erectile dysfunction
Apexbio Technology LLC Pralatrexate 146464-95-1 10mM (in 1mL DMSO)
Pralatrexate (CAS 146464-95-1) is a small molecule inhibitor targeting dihydrofolate reductase (DHFR) with a Ki value of 45 nM DHFR mediates the reduction of dihydrofolate to tetrahydrofolate a critical cofactor in purine thymidylate and amino acid biosynthesis Pralatrexate exhibits high affinity for folylpolyglutamate synthetase (FPGS) and reduced folate carrier-1 (RFC-1) facilitating intracellular accumulation It demonstrates notable antiproliferative activity against various human cancer cell lines in vitro and reduces tumor growth in NSCLC xenograft models indicating its suitability for oncology research
Apexbio Technology LLC Reparixin 266359-83-5 10mM (in 1mL DMSO)
Reparixin (CAS 266359-83-5) is a noncompetitive allosteric inhibitor of chemokine receptors CXCR1 and CXCR2 which are seven-transmembrane G-protein coupled receptors involved notably in acute inflammatory responses Reparixin specifically disrupts CXCR1/2-mediated neutrophil recruitment and migration without affecting other receptor pathways In murine ischemia-reperfusion injury models Reparixin administration significantly inhibits neutrophil influx and associated inflammation-related tissue damage Thus Reparixin serves as a valuable research tool for investigating CXCR-dependent inflammatory mechanisms and evaluating therapeutic potentials in conditions such as acute lung injury and spinal cord damage
Apexbio Technology LLC Flucytosine 2022-85-7 10mM (in 1mL DMSO)
Flucytosine also known as 5-Fluorocytosine (5-FC) is a fluorinated pyrimidine analogue with antifungal properties It exerts its biological activity by penetrating fungal cells and undergoing intracellular conversion into 5-fluorouracil (5-FU) via cytosine deaminase Subsequently 5-FU metabolites inhibit nucleic acid synthesis interfering with fungal RNA and DNA synthesis pathways thus blocking cellular proliferation In laboratory experiments Flucytosine is commonly utilized for antifungal susceptibility assays fungal growth inhibition studies as well as research into antifungal resistance mechanisms The typical reported in vitro antifungal activity displays IC50 values ranging from approximately 0 12 to 8 g/mL depending on fungal species and experimental conditions
Apexbio Technology LLC A66 1166227-08-2 10mM (in 1mL DMSO)
A66 (CAS 1166227-08-2) is a selective inhibitor of the p110 catalytic subunit of class I phosphatidylinositol-4 5-bisphosphate 3-kinase (PI3K) with an IC50 of 32 nM This compound specifically decreases phosphorylation of Akt/PKB and downstream S6K at Thr389 in various cell models including PIK3CA-mutant H1047R cell lines C2C12 myoblasts and 3T3-L1 adipocytes In animal studies A66 reduces tumor growth in xenograft models and improves insulin sensitivity under chronic metabolic stress highlighting its utility in research on PI3K signaling in cancer and metabolic disease
Apexbio Technology LLC Nilotinib(AMN-107) 641571-10-0 10mM (in 1mL DMSO)
Nilotinib (AMN-107 CAS 641571-10-0) is an orally bioavailable selective inhibitor targeting the BCR-ABL tyrosine kinase Derived structurally from imatinib nilotinib inhibits both wild-type (WT p210) and mutant forms (E281K E292K F317L M351T F486S) of BCR-ABL reducing their autophosphorylation activity with IC50 values ranging from 20 to 42 nM It also exhibits substantial inhibitory activity against activated KIT mutants (e g V560del K642E) and various KIT double mutations and effectively suppresses PDGFR and PDGFR kinases Nilotinib is utilized extensively in research related to chronic myeloid leukemia and gastrointestinal stromal tumors involving kinase-driven pathologies
Apexbio Technology LLC DMOG 89464-63-1 10mM (in 1mL DMSO)
DMOG (Dimethyloxalylglycine CAS 89464-63-1) is a small molecule inhibitor of prolyl-4-hydroxylase domain (PHD) enzymes thereby modulating the stability of hypoxia-inducible factor (HIF) PHD inhibition by DMOG prevents HIF-1 prolyl hydroxylation and subsequent degradation stabilizing HIF-1 protein even under normoxic conditions (0 1 1 mmol/L in vitro) Additionally DMOG treatment suppresses NF- B signaling during LPS-induced inflammatory responses in animal models improving survival rates and enhancing IL-10 expression predominantly in peritoneal B-1 cells Thus DMOG serves as a valuable research tool to explore hypoxia signaling pathways and inflammatory responses
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 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
Apexbio Technology LLC Forskolin 66575-29-9 10mM (in 1mL DMSO)
Forskolin (CAS 66575-29-9) is a diterpenoid isolated from the plant Coleus forskohlii known to directly activate adenylate cyclase type I thereby elevating cellular cyclic AMP (cAMP) concentrations It exhibits an IC50 of approximately 41 nM against adenylate cyclase By increasing intracellular cAMP forskolin modulates signaling pathways involved in inflammation and oxidative stress reducing macrophage activation and subsequent production of thromboxane B2 and superoxide Forskolin has been explored in various experimental models and clinical contexts including cardiovascular disorders diabetes mellitus and asthma research
Apexbio Technology LLC Z-YVAD-FMK 210344-97-1 10mM (in 1mL DMSO)
Z-YVAD-FMK (CAS 210344-97-1) is a cell-permeable irreversible inhibitor of caspase-1 By inhibiting caspase-1 activity it interferes with caspase-mediated signaling cascades involved in cell apoptosis and cytokine maturation In Caco-2 cells Z-YVAD-FMK reduces butyrate-induced growth inhibition and fully abrogates butyrate s effects at 100 mol/L Additionally in MyD88-deficient murine bone marrow dendritic cells Z-YVAD-FMK effectively blocks alum-induced caspase-1 activation and subsequent IL-1 release It serves as a valuable research tool for investigating caspase-dependent apoptotic pathways and inflammatory responses
Apexbio Technology LLC Dofetilide 115256-11-6 10mM (in 1mL DMSO)
Dofetilide (CAS 115256-11-6) chemically designated as UK 68789 is a class III antiarrhythmic small molecule that selectively inhibits the rapid delayed rectifier potassium channel (IKr) This inhibition leads to prolonged ventricular action potential duration and extended effective refractory periods in cardiac cells Noted for favorable oral bioavailability Dofetilide is extensively utilized in cardiac electrophysiological research including studies aimed at elucidating arrhythmogenic mechanisms linked to IKr channel function assessing novel antiarrhythmic candidates and exploring physiological and pathological aspects of cardiac rhythm regulation
Apexbio Technology LLC AST-1306 897383-62-9 10mM (in 1mL DMSO)
AST-1306 (CAS 897383-62-9) is an inhibitor of epidermal growth factor receptor (EGFR) and HER2 receptor tyrosine kinases In biochemical assays AST-1306 inhibits EGFR and HER2 kinase activity with IC50 values of 0 5 nM and 3 nM respectively It also demonstrates inhibitory activity against EGFR mutations such as T790M/L858R reducing receptor phosphorylation and downstream signaling in both cell-free and cellular systems In various animal tumor models including ErbB2-overexpressing and SK-OV-3 xenografts AST-1306 suppresses tumor growth and signaling pathways supporting its use in EGFR- and HER2-related oncology research
Apexbio Technology LLC HOAt 39968-33-7 10mM (in 1mL DMSO)
HOAt (1-Hydroxy-7-azabenzotriazole) is a peptide coupling reagent frequently employed in peptide synthesis for the activation of carboxylic groups Structurally HOAt serves as an activating additive that forms reactive intermediates facilitating amide bond formation while mitigating side reactions such as racemization As reported in experimental peptide coupling studies combining HOAt with diisopropylcarbodiimide (DIC) promotes coupling reactions with improved retention of stereochemical integrity relative to traditional coupling systems utilizing other benzotriazole derivatives HOAt is thus commonly used both in segment coupling and stepwise solid-phase peptide assembly methodologies aimed at synthesizing peptides requiring minimal epimerization