Dimethyl Sulfoxide
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 GSK1838705A 1116235-97-2 10mM (in 1mL DMSO)
GSK1838705A (CAS 1116235-97-2) is a small molecule inhibitor targeting the kinase activity of insulin-like growth factor-1 receptor (IGF-1R) insulin receptor and anaplastic lymphoma kinase (ALK) It exhibits potent inhibition with IC50 values of 2 0 nM for IGF-1R 1 6 nM for insulin receptor and 0 5 nM for ALK In preclinical research GSK1838705A suppresses proliferation of hematologic malignancy-derived tumor cells including multiple myeloma and Ewing sarcoma lines and inhibits tumor xenograft growth in vivo Additionally despite targeting the insulin receptor it minimally affects glucose homeostasis at effective doses Due to its multi-target kinase inhibitory profile GSK1838705A serves as a promising tool for cancer biology research
Apexbio Technology LLC Nanaomycin A 52934-83-5 10mM (in 1mL DMSO)
Nanaomycin A is a selective inhibitor targeting DNA methyltransferase 3B (DNMT3B) with an IC50 of approximately 500 nM It acts by specifically inhibiting DNMT3B-mediated DNA methylation without notably affecting DNMT1 activity In cell-based studies employing cancer cell lines such as HCT116 A549 and HL60 treatment with Nanaomycin A reduced global DNA methylation levels and reactivated transcription of tumor suppressor genes previously silenced via promoter hypermethylation Its use in epigenetics-related research includes quantitative assessment of DNMT3B function investigation of DNA methylation regulation mechanisms and evaluation of gene reactivation consequent to DNMT3B inhibition
Apexbio Technology LLC Vemurafenib (PLX4032, RG7204) 918504-65-1 10mM (in 1mL DMSO)
Vemurafenib (PLX4032 RG7204 CAS 918504-65-1) is a small-molecule inhibitor targeting BRAF kinase primarily inhibiting the activity of the oncogenic BRAF V600E mutant by competitively binding its ATP-binding site It also inhibits related kinases such as CRAF ARAF and wild-type BRAF In cells lacking BRAF mutations vemurafenib may paradoxically stimulate downstream MEK signalling due to transactivation mechanisms within RAF dimers Vemurafenib serves as an important research tool for investigating RAF-mediated signaling pathways in oncology particularly in melanoma studies
Apexbio Technology LLC Febuxostat 144060-53-7 10mM (in 1mL DMSO)
Febuxostat (CAS 144060-53-7) is a non-purine selective inhibitor of xanthine oxidase (XO) an enzyme involved in purine metabolism responsible for producing uric acid and reactive oxygen species (ROS) It exerts its inhibitory action by noncompetitive binding at the molybdenum-pterin active center of XO effectively inhibiting both its oxidized and reduced forms Compared to allopurinol febuxostat demonstrates notably higher potency with a reported IC50 of 1 8 nM versus 2 9 M Febuxostat is utilized in clinical and preclinical research exploring hyperuricemia gout and associated metabolic disorders
Apexbio Technology LLC AM095 1345614-59-6 10mM (in 1mL DMSO)
AM095 (CAS 1345614-59-6) is an orally bioavailable antagonist targeting the lysophosphatidic acid receptor 1 (LPA1) It selectively inhibits recombinant human and mouse LPA1 receptors with IC50 values of 0 98 M and 0 73 M respectively In cell-based assays AM095 suppresses LPA1-mediated chemotaxis in mouse LPA1/CHO and human melanoma A2058 cells (IC50 values 0 78 M and 0 23 M respectively) In vivo studies demonstrate its ability to prevent LPA-triggered histamine release reduce collagen and protein accumulation and limit inflammatory cell infiltration in mouse pulmonary models AM095 serves as a valuable tool for investigating LPA1-associated pathologies
Apexbio Technology LLC Propylthiouracil 51-52-5 10mM (in 1mL DMSO)
Propylthiouracil is a thioureylene derivative characterized by inhibitory effects on thyroid hormone synthesis through targeting thyroid peroxidase (TPO) and type 1 iodothyronine deiodinase (DIO1) Its mechanistic actions involve suppression of TPO activity disrupting iodine oxidation and subsequent thyroid hormone formation as well as inhibition of peripheral thyroid hormone conversion via decreased DIO1 enzymatic activity In biomedical research Propylthiouracil is commonly utilized to investigate molecular pathways underlying hyperthyroid conditions such as Graves disease as well as to experimentally explore metabolic regulation of thyroid hormones
Apexbio Technology LLC CO-1686 (AVL-301) 1374640-70-6 10mM (in 1mL DMSO)
CO-1686 (AVL-301 CAS 1374640-70-6) is an orally delivered irreversible small molecule inhibitor targeting mutated epidermal growth factor receptor (EGFR) It functions by forming a covalent bond at cysteine 797 in the ATP-binding domain of EGFR selectively inhibiting mutant variants such as L858R/T790M with reported IC50 values below 0 51 nM CO-1686 preferentially targets mutant EGFR over wild-type demonstrating approximately 22-fold selectivity Preclinical studies using non-small cell lung cancer (NSCLC) cell lines and xenograft models carrying EGFR mutations showed potent anti-proliferative and tumor regression effects Thus CO-1686 represents a valuable research tool in studying mutant EGFR-mediated oncogenesis
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 SGC-CBP30 1613695-14-9 10mM (in 1mL DMSO)
SGC-CBP30 (CAS 1613695-14-9) is a selective small-molecule inhibitor targeting the bromodomains of CREB-binding protein (CREBBP) and E1A-binding protein p300 (EP300) exhibiting IC50 values of 21 nM and 38 nM respectively Both EP300 and CREBBP function as transcriptional coactivators involved in diverse regulatory processes including cell proliferation differentiation and transcription factor activation Through its inhibitory action SGC-CBP30 is utilized widely in biomedical research to investigate the molecular roles of CREBBP/EP300 as well as in studies examining related signaling pathways in tumor biology and cellular regulation
Apexbio Technology LLC GDC-0032 1282512-48-4 10mM (in 1mL DMSO)
GDC-0032 (CAS 1282512-48-4) is a benzofused small-molecule inhibitor targeting PI3K with high potency and selectivity It demonstrates strong inhibitory activity against PI3K PI3K and PI3K with IC50 values of 0 29 nM 0 91 nM and 0 97 nM respectively and notably exhibits greater selectivity towards PI3K In vitro GDC-0032 effectively inhibits cell proliferation and cellular function showing EC50 values of 25 nM (MCF7 cells) and 571 nM (PC3 cells) with corresponding IC50 values of 4 nM and 31 nM In vivo experiments indicate antitumor activity in MCF7-neo/Her2 xenograft models GDC-0032 serves as a valuable tool compound for PI3K-related oncology research
Apexbio Technology LLC Bexarotene 153559-49-0 10mM (in 1mL DMSO)
Bexarotene is a synthetic selective agonist for retinoid X receptors (RXRs) a subclass of nuclear hormone receptors involved in the regulation of gene transcription Upon binding to RXRs Bexarotene modulates the expression of target genes associated with cell differentiation proliferation and apoptosis Due to this mechanism Bexarotene is commonly employed in research investigating tumor growth inhibition cellular differentiation pathways and apoptosis induction Researchers also frequently utilize this retinoid derivative to elucidate RXR-mediated signaling pathways in oncology and to explore potential therapeutic applications for various malignancies
Apexbio Technology LLC Ezetimibe 163222-33-1 10mM (in 1mL DMSO)
Ezetimibe (CAS 163222-33-1) is a cholesterol absorption inhibitor that targets the intestinal cholesterol transporter Niemann-Pick C1 Like 1 (NPC1L1) It reduces intestinal uptake of cholesterol and dietary carotenoids including - and -carotene lycopene lutein and -cryptoxanthin through downregulating transport proteins such as SR-BI ABCA1 NPC1L1 and transcription factors including SREBP-1/-2 and LXR- In ApoE-deficient mouse models ezetimibe significantly decreases plasma cholesterol levels and attenuates atherosclerotic lesion formation Clinically it lowers LDL cholesterol total cholesterol and triglycerides while elevating HDL cholesterol
Apexbio Technology LLC ZM 447439 331771-20-1 10mM (in 1mL DMSO)
ZM 447439 (CAS 331771-20-1) is a selective inhibitor of Aurora kinases a subgroup within the serine/threonine kinase family involved in chromosome segregation during cell division It inhibits recombinant Aurora A and Aurora B kinases with IC50 values of approximately 110 nM and 130 nM respectively consequently reducing phosphorylation of histone H3 at serine 10 ZM 447439 demonstrates limited inhibitory activity towards other kinases with IC50 values above 10 M for CDK1/2/4 IKK1/2 PLK1 CHK1 cFLT2 KDR2 FAK and Zap-70 In biological research ZM 447439 is commonly employed to study mitotic regulation chromosomal alignment and apoptosis signaling pathways
Apexbio Technology LLC Prucalopride 179474-81-8 10mM (in 1mL DMSO)
Prucalopride (CAS 179474-81-8) is a selective serotonin 5-HT4 receptor agonist with high affinity for both 5-HT4A and 5-HT4B receptor subtypes demonstrating Ki values of 2 5 nM and 8 nM respectively It displays substantial selectivity exceeding 290-fold against other serotonin receptor classes By activating 5-HT4 receptors prucalopride promotes gastrointestinal motility making it a valuable tool compound for investigating serotonergic mechanisms underlying gastrointestinal disorders and motility regulation Currently prucalopride is evaluated in Phase 3 clinical trials