Dimethyl Sulfoxide
Apexbio Technology LLC (-)-MK 801 121917-57-5 10mM (in 1mL DMSO)
(-)-MK 801 (CAS 121917-57-5) is a small molecule serving as a non-competitive antagonist at the N-methyl-D-aspartate (NMDA) receptor It crosses the blood-brain barrier binding reversibly and with high affinity to cortical membranes in a saturable regionally specific manner notably within the hippocampus (-)-MK 801 selectively inhibits depolarization responses to NMDA receptor activation leading to suppression of seizure-like neuronal activity induced by neurotoxins such as tetrodotoxin Due to these properties it has widespread use as a research tool in neuroscience particularly in investigating excitotoxicity epilepsy and neurological disorders associated with NMDA receptor dysfunction
Apexbio Technology LLC Proparacaine HCl 5875-06-9 10mM (in 1mL DMSO)
Proparacaine HCl (CAS 5875-06-9) is a small-molecule antagonist of voltage-gated sodium channels By inhibiting sodium ion entry through these channels Proparacaine HCl effectively suppresses action potential generation and neuronal signaling Assays demonstrate an ED50 value of approximately 3 4 mM Due to its sodium channel inhibition Proparacaine HCl is utilized in scientific research to study neuronal excitability ion channel function and related electrophysiological processes
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 YM201636 371942-69-7 10mM (in 1mL DMSO)
YM201636 is a cell-permeable selective inhibitor of the mammalian class III phosphatidylinositol phosphate kinase PIKfyve It functions by targeting and inhibiting PIKfyve enzymatic activity at an IC50 of approximately 33 nM thus reducing the biosynthesis of phosphatidylinositol (3 5)-bisphosphate (PtdIns(3 5)P2) Treatment of various mammalian cell lines (including NIH3T3 MDCK MCF10A COS7 and MEFs) with YM201636 induces the formation of enlarged intracellular vacuoles pointing toward changes in endosomal transport and membrane trafficking Furthermore YM201636 has shown utility in studying insulin-mediated signaling by inhibiting insulin-dependent class I PI3K activation lowering Akt phosphorylation and preventing surface translocation of GLUT4 in adipocytes Researchers frequently utilize this compound to analyze intracellular vesicular transport pathways and phosphoinositide-dependent signaling events
Apexbio Technology LLC CP-673451 343787-29-1 10mM (in 1mL DMSO)
CP-673451 (CAS 343787-29-1) is an ATP-competitive inhibitor with specificity for platelet-derived growth factor receptors (PDGFR- / ) It exhibits inhibitory potency with IC50 values of 10 nM for PDGFR- and 1 nM for PDGFR- while demonstrating significantly less inhibition toward kinases such as VEGFR-1 VEGFR-2 Lck TIE-2 and EGFR In cellular assays CP-673451 effectively inhibits PDGFR- phosphorylation in PAE- cells (IC50 6 4 nM) and reduces c-kit activity in H526 cells at micromolar range Its anticancer efficacy has been established by suppressing tumor growth and vascularization in xenograft models indicating its potential utility in cancer research and angiogenesis studies
Apexbio Technology LLC Prilocaine 721-50-6 10mM (in 1mL DMSO)
Prilocaine (CAS 721-50-6) is a local anesthetic molecule categorized within the amino amide class Its primary pharmacological mechanism involves reversible blockade of voltage-gated sodium channels in neuronal membranes thereby inhibiting action potential propagation and sensory nerve impulse conduction Due to its sodium channel-blocking profile prilocaine is commonly investigated in biomedical research examining reversible neural inhibition pain modulation pathways and sensory signal transmission mechanisms
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 LY2584702 1082949-67-4 10mM (in 1mL DMSO)
LY2584702 (CAS 1082949-67-4) is an orally bioavailable ATP-competitive inhibitor selectively targeting p70 S6 kinase (p70S6K) a serine/threonine kinase downstream of the PI3K/Akt/mTOR signaling cascade By inhibiting p70S6K activity LY2584702 effectively suppresses phosphorylation of ribosomal protein S6 (S6) thereby modulating protein translation LY2584702 exhibits potent inhibition of p70S6K (IC50 4 nM) and effectively reduces phosphorylated S6 levels in HCT116 colorectal cancer cells (IC50 between 0 1-0 24 M) Notably LY2584702 demonstrated anticancer activity in preclinical xenograft models supporting its role in targeted cancer research and therapeutic development
Apexbio Technology LLC BV6 1001600-56-1 10mM (in 1mL DMSO)
BV6 (CAS 1001600-56-1) is a selective inhibitor targeting the inhibitor of apoptosis protein (IAP) family The IAP family includes proteins such as XIAP c-IAP1 and c-IAP2 that regulate programmed cell death pathways BV6 induces apoptosis and sensitizes cancer cells to chemotherapeutic agents and radiation by decreasing expression levels of IAPs including XIAP and c-IAP1 In vitro treatment with BV6 exhibited an IC50 of 7 2 M in H460 non-small cell lung carcinoma cells and enhanced their response to radiation BV6 is employed in research exploring cancer cell apoptosis modulation and therapeutic resistance
Apexbio Technology LLC Sephin1 13098-73-2 10mM (in 1mL DMSO)
Sephin1 (CAS 13098-73-2) is a selective inhibitor of PPP1R15A a regulatory subunit of protein phosphatase 1 involved in the regulation of stress-induced eIF2 dephosphorylation Under endoplasmic reticulum (ER) stress phosphorylated eIF2 attenuates protein synthesis preventing accumulation of misfolded proteins By inhibiting PPP1R15A Sephin1 sustains eIF2 phosphorylation extending translational attenuation during ER stress In cell assays Sephin1 selectively disrupts PPP1R15A-PP1c complexes without affecting PPP1R15B-mediated complexes In mouse models harboring misfolded protein mutations (e g MPZ or SOD1) Sephin1 administration mitigates molecular cellular and functional deficits thus relevant for proteostasis-related disease studies
Apexbio Technology LLC 4μ8C 14003-96-4 10mM (in 1mL DMSO)
4 8C (CAS 14003-96-4) is a small molecule inhibitor targeting the RNase activity of inositol-requiring enzyme 1 alpha (IRE1 ) an important transmembrane serine/threonine kinase involved in the unfolded protein response (UPR) By selectively blocking IRE1-mediated RNase function 4 8C inhibits downstream UPR gene activation in cell lines exposed to hypoxia or endoplasmic reticulum (ER) stressors including HCT116 colon carcinoma and KP4 pancreatic cancer cells without affecting proliferation or clonogenic survival under these conditions Due to its selective action 4 8C serves as a valuable tool in research investigating ER stress pathways and their roles in cellular adaptation and disease pathology
Apexbio Technology LLC Kaempferol(Synonyms: Kempferol, Kaempherol, Kaempferide, Robigenin, Rhamnolutein, Populnetin), 10mM (in 1mL DMSO), CAS: 520-18-3.
Kaempferol (CAS 520-18-3) is a naturally derived flavonoid isolated from sources including Gingko biloba and red wine It functions biologically by activating the mitochondrial calcium uniporter (EC50 7 M) Additionally kaempferol promotes apoptosis through the caspase-9 pathway by suppressing polo-like kinase 1 (PLK1) expression thereby inhibiting cancer cell proliferation in diverse cell lines It also demonstrates antioxidant properties and reduces osteoclast-mediated bone resorption in vitro These characteristics make kaempferol valuable for researching mitochondrial physiology cancer biology and bone metabolism
Apexbio Technology LLC Fluvastatin Sodium 93957-55-2 10mM (in 1mL DMSO)
Fluvastatin Sodium (CAS 93957-55-2) is an inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase the rate-limiting enzyme in cholesterol biosynthesis By blocking HMG-CoA reductase activity fluvastatin reduces serum total cholesterol LDL-cholesterol and apolipoprotein B while increasing HDL-cholesterol and apolipoprotein A-I levels In research settings fluvastatin exhibits anti-atherosclerotic anti-thrombotic and antioxidant properties Studies have shown fluvastatin decreases platelet aggregation dose-dependently in vitro reducing platelet aggregation by approximately 10-15% at clinical doses (40 mg/day) Additionally fluvastatin inhibits inflammatory angiogenesis and NO production suggesting potential applications in inflammatory and cardiovascular research
Apexbio Technology LLC Evacetrapib (LY2484595) 1186486-62-3 10mM (in 1mL DMSO)
Evacetrapib (LY2484595 CAS 1186486-62-3) is a potent and selective inhibitor targeting cholesteryl ester transfer protein (CETP) a regulator of lipid metabolism Evacetrapib exhibits inhibitory activity with IC50 values of 5 5 nM in assays containing recombinant human CETP and 26 nM within human plasma CETP assays In vivo oral administration at 30 mg/kg in human CETP/ApoAI double-transgenic mice significantly reduces CETP activity and elevates HDL-cholesterol concentration (ED50 5 mg/kg) Evacetrapib does not elevate blood pressure nor induce aldosterone or cortisol synthesis in model systems highlighting its potential in cardiovascular research related to coronary artery disease