Dimethyl Sulfoxide
Apexbio Technology LLC Stattic 19983-44-9 10mM (in 1mL DMSO)
Stattic (CAS 19983-44-9) is a small-molecule inhibitor specifically targeting signal transducer and activator of transcription 3 (STAT3) It suppresses STAT3 activation by blocking its dimerization nuclear translocation and subsequent transcriptional activity In vitro studies demonstrate Stattic inhibits proliferation in multiple head and neck squamous cell carcinoma (HNSCC) cell lines including UM-SCC-17B OSC-19 Cal33 and UM-SCC-22B with reported IC50 values ranging from approximately 2 3 to 3 5 M Additionally Stattic downregulates STAT3-mediated hypoxia-inducible factor-1 (HIF-1) expression resulting in enhanced radiosensitivity in HNSCC cells and shows activity in mouse xenograft tumor models Therefore Stattic serves as a research tool for investigating STAT3-associated signaling pathways and cancer biology
Apexbio Technology LLC Rifapentine 61379-65-5 10mM (in 1mL DMSO)
Rifapentine is an antibiotic compound employed in the treatment of pulmonary tuberculosis an infectious disease primarily caused by Mycobacterium tuberculosis Rifapentine inhibits bacterial RNA polymerase thereby preventing RNA synthesis essential for bacterial replication and survival In vitro studies demonstrate that rifapentine possesses potent activity against intracellular M tuberculosis residing within human macrophages with reported MIC values ranging from 0 015 to 0 06 mg/ml Preclinical research indicates rifapentine accumulates extensively in host cells achieving higher intracellular concentrations than structurally related rifampin Clinically rifapentine administration schedules involve twice-weekly doses during the intensive phase of tuberculosis therapy followed by weekly dosing in the continuation phase Rifapentine is commonly investigated in pharmacological studies to assess efficacy and optimize dosing regimens in pulmonary tuberculosis treatment
Apexbio Technology LLC Topotecan 123948-87-8 10mM (in 1mL DMSO)
Topotecan (CAS 123948-87-8) a semisynthetic derivative of camptothecin functions by selectively inhibiting topoisomerase I This inhibition stabilizes enzyme-DNA cleavage complexes disrupting DNA replication and transcription processes essential for tumor cell proliferation In preclinical studies topotecan demonstrated antitumor activity in mouse models of leukemia (P388) Lewis lung carcinoma B16 melanoma and human colon adenocarcinoma xenograft HT-29 Its toxicity primarily affecting rapidly proliferating tissues such as bone marrow and gastrointestinal epithelium was concentration-dependent and reversible Topotecan is employed extensively as a research tool in oncology studies focusing on DNA-topoisomerase interactions and targeting solid tumor growth
Apexbio Technology LLC Losmapimod 585543-15-3 10mM (in 1mL DMSO)
Losmapimod (CAS 585543-15-3) also known as GW856553 is a selective orally bioavailable inhibitor of p38 mitogen-activated protein kinase (MAPK) It exhibits potent inhibitory activity against p38 and p38 isoforms with reported pKi values of 8 1 and 7 6 respectively By inhibiting p38 MAPK a kinase essential in inflammatory signaling pathways and cytokine production Losmapimod has demonstrated beneficial effects in preclinical and clinical models It improves nitric oxide-mediated vasodilation and reduces markers of systemic inflammation such as C-reactive protein and fibrinogen This molecule is utilized in research studies addressing inflammation-driven cardiovascular disorders hypercholesterolemia and chronic obstructive pulmonary disease (COPD)
Apexbio Technology LLC GW4064 278779-30-9 10mM (in 1mL DMSO)
GW4064 (CAS 278779-30-9) is a non-steroidal agonist targeting the farnesoid X receptor (FXR) a nuclear receptor involved in lipid and cholesterol regulation Reported EC50 values of GW4064 for FXR activation are approximately 15 nM in isolated receptor assays and 90 nM in human FXR-transfected cell studies In animal models including KK-Ay and ob/ob mice GW4064 administration was associated with reduced serum triglyceride (TG) concentrations and diminished very-low-density lipoprotein (VLDL) production However due to limitations such as poor solubility chemical instability under UV exposure and a potentially toxic stilbene pharmacophore GW4064 primarily serves as a research tool for investigating FXR signaling pathways
Apexbio Technology LLC YO-01027 (Dibenzazepine, DBZ) 209984-56-5 10mM (in 1mL DMSO)
YO-01027 (Dibenzazepine DBZ CAS 209984-56-5) is a potent inhibitor targeting -secretase a multimeric aspartyl protease involved in the proteolytic cleavage of type I integral membrane proteins notably amyloid precursor protein-like (APPL) proteins and Notch receptors YO-01027 interacts with the N-terminal regions of presenilin dose-dependently inhibiting cleavage of APPL and Notch proteins Research indicates that YO-01027 modulates cell differentiation by suppressing Notch signaling pathways influencing cellular transitions and mucin (MUC16) synthesis illustrating its utility in cell biology and therapeutic studies of Notch-related signaling processes
Apexbio Technology LLC Rucaparib (AG-014699,PF-01367338) 459868-92-9 10mM (in 1mL DMSO)
Rucaparib (AG-014699 PF-01367338 CAS 459868-92-9) is a small molecule inhibitor targeting poly(ADP-ribose) polymerase (PARP) a nuclear enzyme activated by DNA damage and central to the base excision repair pathway By blocking PARP activity rucaparib impairs DNA repair especially in cells with pre-existing DNA repair deficiencies such as those induced by genotoxic stress In prostate cancer research rucaparib induces radiosensitization notably in PTEN-deficient cells expressing ETS fusion proteins through inhibition of non-homologous end joining (NHEJ) It is thus relevant in studies investigating DNA damage response pathways cancer biology and therapeutic radiosensitization strategies
Apexbio Technology LLC Tariquidar(Synonyms: XR9576, Tariquidar fumarate, XR-9576, UNII-1W8830WSA2, P-glycoprotein inhibitor XR9576), 10mM (in 1mL DMSO), CAS: 206873-63-4.
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 Ro3280 1062243-51-9 10mM (in 1mL DMSO)
Ro3280 (CAS 1062243-51-9) is a selective small-molecule inhibitor targeting Polo-like kinase 1 (PLK1) exerting inhibitory activity with an IC50 of 3 nM PLK1 is a cell cycle kinase involved prominently in regulating progression from G2 to M phase frequently overexpressed in various malignancies Ro3280 inhibits PLK1 activity and induces apoptosis and cell cycle disruption in acute leukemia cell lines (e g U937 HL-60 NB4 K562 MV4-11) and diverse solid tumor models (e g lung carcinoma H82 colon carcinoma HT-29 breast carcinoma MDA-MB-468) In mouse xenografts of HT-29 tumors Ro3280 demonstrates significant tumor regression highlighting its potential in cancer therapeutics research
Apexbio Technology LLC PF-04449913 1095173-27-5 10mM (in 1mL DMSO)
PF-04449913 (CAS 1095173-27-5) is an orally bioavailable small molecule inhibitor targeting smoothened (SMO) a critical component of the Hedgehog (Hh) signaling pathway Activation of SMO by Hh ligands typically initiates signaling cascades involving Gli transcription factors influencing cellular proliferation and oncogenesis PF-04449913 inhibits SMO activity with an IC50 of 5 nM thereby suppressing downstream Gli-mediated signaling Preclinical pharmacokinetic studies demonstrated favorable properties including a half-life of approximately 30 hours 55% oral bioavailability low plasma clearance (1 03 mL/min/kg) and moderate distribution (2 7 L/kg) PF-04449913 is actively explored in cancer research contexts
Apexbio Technology LLC Aloperine 56293-29-9 10mM (in 1mL DMSO)
Aloperine is a naturally derived alkaloid known for its biological properties including anti-inflammatory antiviral antibacterial and antitumor activities Mechanistic studies suggest that aloperine exerts anti-inflammatory effects through inhibition of inflammatory mediators and inflammatory signaling pathways such as nuclear factor-kappa B (NF- B) and mitogen-activated protein kinase (MAPK) pathways In vitro assays demonstrate antiviral potential related to inhibition of specific viral replication stages Additionally its antitumor properties have been identified in multiple cancer cell lines where aloperine can induce apoptosis inhibit proliferation and migration and modulate cell cycle progression Aloperine typically exhibits IC50 values ranging from low micromolar to sub-micromolar concentrations depending on cell lines and experimental settings It serves as a research tool compound in immunological oncological and infectious disease studies
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 Gemfibrozil 25812-30-0 10mM (in 1mL DMSO)
Gemfibrozil is a small-molecule pharmacological agent that functions primarily through activation of the nuclear receptor peroxisome proliferator-activated receptor-alpha (PPAR ) By modulating PPAR signaling pathways gemfibrozil regulates lipid metabolism influencing the transcription of genes associated with fatty acid oxidation and lipoprotein synthesis resulting in reduced triglyceride levels and altered lipoprotein profiles In biomedical research contexts gemfibrozil is utilized to explore molecular mechanisms underlying lipid metabolic processes atherosclerosis progression and related metabolic disorders Furthermore gemfibrozil serves as a useful experimental tool to dissect PPAR -dependent pathways and to investigate therapeutic potentials targeting lipid abnormalities and cardiovascular disease
Apexbio Technology LLC Panobinostat (LBH589) 404950-80-7 10mM (in 1mL DMSO)
Panobinostat (LBH589) is a histone deacetylase (HDAC) inhibitor targeting class I II and IV HDAC enzymes regulating gene expression through histone hyperacetylation In vitro studies indicate panobinostat induces apoptosis and growth arrest in Ph-negative acute lymphoblastic leukemia (ALL) cell lines T-cell (MOLT-4) and pre-B cell (Reh) via caspase activation PARP cleavage and downregulation of c-Myc accompanied by H3K9 and H4K8 hyperacetylation and elevation of cell-cycle regulators (p21 p27) Panobinostat has shown anti-proliferative effects in various cancer models including cutaneous T-cell lymphoma and multiple myeloma (IC50 5-30 nM) and serves as a research tool in studies assessing epigenetic regulation and tumor biology
Apexbio Technology LLC Rivaroxaban 366789-02-8 10mM (in 1mL DMSO)
Rivaroxaban (CAS 366789-02-8) is a small molecule inhibitor targeting coagulation Factor Xa a serine protease essential in the thrombin generation pathway involved in clot formation It binds reversibly to the S1 pocket of Factor Xa engaging specifically through interactions between its chlorothiophene moiety and the Tyr288 residue Binding kinetics are rapid (kon 1 7 10 7 mol L 1 s 1 koff 5 10 3 s 1) and affinity is high (Ki 0 4 nmol/L) Rivaroxaban is studied extensively in thrombosis research including venous thromboembolism stroke prevention in atrial fibrillation and cardiovascular event management post-acute coronary syndrome