Dimethyl Sulfoxide
Apexbio Technology LLC SB 225002 182498-32-4 10mM (in 1mL DMSO)
SB 225002 (CAS 182498-32-4) is a selective non-peptide antagonist targeting the chemokine receptor CXCR2 a G protein-coupled receptor involved in interleukin-8 (IL-8)-mediated neutrophil chemotaxis and polarization It inhibits IL-8 binding to CXCR2 with an IC50 of 22 nM and displays over 150-fold selectivity against CXCR1 SB 225002 suppresses neutrophil migration and polarization triggered by IL-8 and GRO in cell-based assays and animal models It also promotes apoptosis and mitotic catastrophe in ovarian cancer cells independently of p53 status highlighting its utility in inflammation and oncology research
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 GM 6001 142880-36-2 10mM (in 1mL DMSO)
GM 6001 (Ilomastat Galardin CAS 142880-36-2) is a broad-spectrum inhibitor of matrix metalloproteinases (MMPs) including MMP-1 -2 -3 -8 and -9 with reported Ki values of 0 4 nM 0 5 nM 27 nM 0 1 nM and 0 2 nM respectively MMPs participate in extracellular matrix remodeling and mediate signaling events induced by GPCR agonists through EGFR transactivation GM 6001 suppresses EGFR phosphorylation ERK activation and subsequent DNA synthesis induced by stimuli such as bombesin and lysophosphatidic acid (LPA) Additionally this compound has potential applications in cartilage research facilitating meniscal repair under inflammatory conditions by dampening IL-1-mediated MMP activity
Apexbio Technology LLC Belinostat (PXD101) 414864-00-9 10mM (in 1mL DMSO)
Belinostat (PXD101) is a hydroxamic acid-based inhibitor targeting histone deacetylase (HDAC) enzymes Its mechanism involves the suppression of HDAC enzymatic activity leading to increased acetylation of histone proteins H3 and H4 within cells In biochemical assays using Hela cell extracts belinostat exhibits inhibitory activity against HDAC with an IC50 value of approximately 27 nM In tumor cell culture models belinostat induces cytotoxicity and represses cellular proliferation with reported IC50 values ranging roughly from 0 5 M to 10 M varying by cell type and origin making it suitable for research on epigenetic modulation in oncology specifically in studies of bladder prostate and related cancer cell lines
Apexbio Technology LLC Brassinolide 72962-43-7 10mM (in 1mL DMSO)
Brassinolide (CAS 72962-43-7) is a naturally occurring steroidal plant growth regulator It influences various physiological processes in plants including stem elongation leaf differentiation flower formation and fruit development In vitro studies indicated that brassinolide induces apoptosis in human prostate cancer PC-3 cells characterized by increased caspase-3 activity and decreased Bcl-2 protein expression In animal models brassinolide reduced blood glucose levels in diabetic rats demonstrating non-dose-dependent hypoglycemic effects without observed toxicity Brassinolide is valuable in research related to cancer cell apoptosis and glucose metabolism regulation
Apexbio Technology LLC BOSUTINIB SKI-606 1ML DMSO
Bosutinib (SKI-606 CAS 380843-75-4) is a dual inhibitor targeting c-Src and Abl kinases with IC50 values of approximately 1 2 nM and 1 nM respectively It suppresses phosphorylation of Bcr-Abl Src and Stat5 in chronic myeloid leukemia (CML) cells thereby decreasing proliferation and inducing regression in K562 xenograft tumor models Bosutinib also reduces Src autophosphorylation and inhibits -catenin signaling by blocking its interaction with TCF4 transcription factor consequently downregulating cyclin D1 expression in colorectal cancer cells This mechanism results in decreased cell motility and enhanced -catenin binding to E-cadherin highlighting utility in cancer research
Apexbio Technology LLC BATIMASTAT BB-94 1ML DMSO
Batimastat (BB-94 CAS 130370-60-4) is a synthetic small-molecule inhibitor targeting matrix metalloproteinases (MMPs) Structurally a polypeptide-like analogue of collagen substrates batimastat contains a peptidic backbone and a hydroxamate moiety that binds the catalytic zinc atom of MMPs It inhibits several MMP subtypes markedly including MMP-1 MMP-2 MMP-3 MMP-7 and MMP-9 with reported IC50 values of 3 4 20 6 and 4 nM respectively In preclinical studies batimastat demonstrates inhibitory effects on tumor growth and angiogenesis across various tumor models including ovarian and colon carcinoma xenografts making it relevant for cancer research and therapeutic development
Apexbio Technology LLC BMX-IN-1 10MM IN 1ML DMSO
BMX-IN-1 (CAS 1431525-23-3) is a highly selective irreversible inhibitor targeting BMX (bone marrow kinase on chromosome X also known as ETK) a member of the Tec tyrosine kinase family BMX is prominently expressed in arterial endothelium and myeloid hematopoietic cells functioning in ischemia-induced arterial and lymphatic vessel formation processes and contributing to tumor growth In cellular models expressing Tel-BMX fusion proteins BMX-IN-1 treatment at low doses effectively reduces proliferation highlighting its potential utility in cancer research particularly prostate cancer studies
Apexbio Technology LLC PERAMIVIR 10MM IN 1ML DMSO
Peramivir (CAS 330600-85-6) is a neuraminidase inhibitor under investigation for antiviral activity against influenza virus Structurally peramivir functions as a transition-state analogue inhibitor selectively targeting viral neuraminidase to obstruct enzymatic cleavage required for virion release from infected host cells By this action peramivir effectively impedes viral propagation It has undergone clinical evaluation in research contexts notably receiving emergency use authorization for hospitalized patients during the 2009 H1N1 influenza pandemic
Apexbio Technology LLC MELATONIN 10MM IN 1ML DMSO
Melatonin (CAS 73-31-4) is a naturally occurring hormone functioning primarily as an agonist at the G protein-coupled melatonin receptors MT and MT Through receptor activation melatonin regulates circadian rhythmicity and contributes significantly to sleep-wake cycle maintenance Additionally melatonin demonstrates immunomodulatory capabilities and possesses robust antioxidant properties in vivo combating oxidative stress Due to these characteristics it is frequently investigated in research related to sleep disorders circadian biology immune function and oxidative stress signaling pathways
Apexbio Technology LLC A-740003 10MM IN 1ML DMSO
A-740003 (CAS 861393-28-4) is a selective and competitive antagonist targeting the P2X7 receptor a member of the ATP-gated ionotropic P2X receptor family involved in immune cell signaling cytokine secretion apoptosis and cellular proliferation The antagonist displays IC50 values of 18 nM and 40 nM against mouse and human P2X7 receptors respectively In human THP-1 macrophage-like cells A-740003 inhibits pore formation assessed by Yo-Pro uptake assay (IC50 92 nM) and reduces interleukin-1 secretion (IC50 156 nM) This compound is employed in research investigating P2X7-mediated inflammatory pathways and neuropathic pain mechanisms
Apexbio Technology LLC TARIQUIDAR 10MM IN 1ML DMSO
Tariquidar (CAS 206873-63-4) is a small-molecule inhibitor targeting the efflux transporter P-glycoprotein (Pgp) Pgp a 170-kDa transmembrane protein functions primarily as an ATP-dependent drug efflux pump removing structurally diverse molecules from cells Tariquidar acts through noncompetitive inhibition of Pgp-associated basal ATPase activity thereby reducing drug efflux In vitro assays across several cell models demonstrate tariquidar-mediated Pgp inhibition with IC50 values ranging from 15 to 223 nM Due to its selectivity for Pgp tariquidar serves as a significant research tool in studies of drug resistance and transporter-mediated drug disposition
Apexbio Technology LLC CRENOLANIB CP-868596 1ML DMSO
Crenolanib (CP-868596 CAS 670220-88-9) is a selective inhibitor targeting receptor tyrosine kinases PDGFR PDGFR and FLT3 exhibiting Kd values of 3 2 nM 2 1 nM and 0 74 nM respectively It notably suppresses the FLT3 autophosphorylation and proliferation mediated via PDGFR mutations that confer resistance to imatinib such as D842V (IC50 10 nM) but does not inhibit the V561D mutant Additionally crenolanib reduces kinase activity of the FIP1L1-PDGFRA fusion protein (IC50 1 nM) and proliferation in EOL-1 cells It serves as a research tool for kinase-driven malignancies particularly those resistant to other kinase inhibitors
Apexbio Technology LLC UMI-77 10MM IN 1ML DMSO
UMI-77 (CAS 518303-20-3) is a small-molecule inhibitor targeting the anti-apoptotic protein Myeloid cell leukemia-1 (Mcl-1) a member of the Bcl-2 protein family implicated in apoptotic regulation and cell survival signaling Biochemical assays demonstrate that UMI-77 binds selectively to the BH3-binding groove of Mcl-1 protein competing effectively against pro-apoptotic BH3 peptides (Ki 0 49 M) Additionally UMI-77 disrupts the interaction of Mcl-1 with pro-apoptotic factors such as Bax (IC50 1 43 M) promoting apoptosis in cancer cells Preclinical studies on pancreatic cancer cell lines and BxPC-3 xenograft mouse models show that UMI-77 suppresses tumor growth and induces apoptotic cell death highlighting its value as a research tool for studying apoptosis-related oncogenic pathways