Dimethyl Sulfoxide
Apexbio Technology LLC Chidamide(Synonyms: Epidaza, HBI-8000, CS055, Tucidinostat, Entinostat analog, Chidamide (CS055)), 10mM (in 1mL DMSO), CAS: 743420-02-2.
Chidamide (CAS 743420-02-2) is a benzamide-based histone deacetylase (HDAC) inhibitor that targets enzymes responsible for the reversible acetylation of lysine residues on histone tails By modulating HDAC activity Chidamide promotes chromatin remodeling influencing transcription factor access and subsequent gene transcription In vitro studies on human leukemia cell lines and primary myeloid leukemia cells indicate that Chidamide induces cell cycle arrest at the G1 phase differentiation and apoptosis via ROS-dependent mechanisms Therefore Chidamide shows considerable potential in research focused on hematologic malignancies and cancer therapy
Apexbio Technology LLC Cediranib (AZD217) 288383-20-0 10mM (in 1mL DMSO)
Cediranib (AZD2171 CAS 288383-20-0) is an orally bioavailable small molecule inhibitor targeting the kinase insert domain receptor (KDR VEGFR-2) with potent inhibition observed in recombinant assays (IC50 1 nM) Additionally cediranib suppresses related vascular endothelial growth factor receptors VEGFR-1 (Flt-1 IC50 5 nM) and VEGFR-3 (Flt-4 IC50 3 nM) It also blocks select platelet-derived growth factor receptors notably c-Kit PDGFR PDGFR and CSF-1R at nanomolar to sub-micromolar concentrations indicating multiple-kinase targeting capability Cediranib serves as a valuable research compound for studying tumor angiogenesis and kinase-driven oncogenic pathways
Apexbio Technology LLC BKM120 944396-07-0 10mM (in 1mL DMSO)
BKM120 (CAS 944396-07-0) is a potent orally bioavailable inhibitor of class I phosphatidylinositol 3-kinases (PI3Ks) specifically targeting the isoforms p110 p110 p110 and p110 with IC50 values of 52 nM 166 nM 262 nM and 116 nM respectively By blocking PI3K activity this molecule suppresses downstream phosphorylation of AKT an important mediator within the PI3K-AKT-mTOR signaling cascade implicated in tumor growth and survival Preclinical studies demonstrate that BKM120 restricts tumor cell proliferation promotes cell cycle arrest at G1 phase and induces apoptosis particularly noted in PTEN-deficient cancer models Thus BKM120 serves as a useful tool for studying PI3K pathway-dependent cancers
Apexbio Technology LLC Crenolanib (CP-868596)(Synonyms: CP-868596, Crenolanib besylate, AR-868596, PDGFR inhibitor CP-868596, PDGFR-beta inhibitor CP-868596), 10mM (in 1mL DMSO), CAS: 670220-88-9.
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 Tenofovir Disoproxil Fumarate 202138-50-9 10mM (in 1mL DMSO)
Tenofovir disoproxil fumarate is an antiviral nucleotide analog functioning as a nucleoside reverse transcriptase inhibitor (NRTI) Upon cellular uptake it undergoes enzymatic hydrolysis to form the active metabolite tenofovir subsequently phosphorylated to the diphosphate derivative This phosphorylated metabolite competitively inhibits HIV-1 reverse transcriptase and induces DNA chain termination In vitro studies using MT-2 cells and peripheral blood mononuclear cells (PBMC) have demonstrated suppression of HIV replication with reported EC50 values approximately 0 007 mol/L and 0 005 mol/L respectively This compound is routinely utilized in research investigating HIV replication mechanisms antiretroviral therapies and drug resistance profiles
Apexbio Technology LLC GYY 4137 morpholine salt(Synonyms: GYY4137, Morpholin-4-ium 4-methoxyphenyl(morpholino)phosphinodithioate, GYY-4137), 10mM (in 1mL DMSO), CAS: 106740-09-4.
GYY 4137 morpholine salt (CAS 106740-09-4) is a slow-releasing hydrogen sulfide (H S) donor that exerts biological activity by modulating signaling pathways involved in vasodilation and blood pressure regulation In experimental studies this compound demonstrates the capacity to suppress cellular proliferation induce apoptosis and arrest cell cycle progression Due to these properties GYY 4137 morpholine salt is widely utilized in research investigating hypertension inflammation and cancer biology
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 Phenacetin 62-44-2 10mM (in 1mL DMSO)
Phenacetin (CAS 62-44-2) is a synthetic non-opioid analgesic historically utilized for alleviating pain and reducing fever lacking intrinsic anti-inflammatory effects Its analgesic mechanism primarily involves inhibition of cyclooxygenase (COX) enzyme activity in the central nervous system leading to decreased prostaglandin synthesis Previously studied for its pharmacological action on pain modulation pathways phenacetin serves currently as an experimental reference compound in evaluating nephrotoxic effects in biomedical research following its market withdrawal due to nephropathy concerns
Apexbio Technology LLC NVP DPP 728 dihydrochloride 247016-69-9 10mM (in 1mL DMSO)
NVP DPP 728 dihydrochloride (CAS 247016-69-9) is a potent orally active inhibitor of dipeptidyl peptidase IV (DPP-IV) Mechanistically it reversibly inhibits human DPP-IV enzyme through formation of a nitrile-dependent complex characterized by transitional-state kinetic properties exhibiting a Ki of 11 nM In aged rat models oral administration of NVP DPP 728 reduces plasma DPP-IV activity enhances early-phase insulin secretion and improves glucose tolerance following glucose challenge This compound is under preclinical investigation for type 2 diabetes research targeting the DPP-IV/glucagon-like peptide-1 pathway
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 Dynasore 304448-55-3 10mM (in 1mL DMSO)
Dynasore is a non-competitive inhibitor targeting dynamin family GTPases including dynamin1 dynamin2 and Drp1 with an IC50 of approximately 15 M Dynamin GTPases mediate membrane fission processes required for endocytosis and intracellular vesicle trafficking through catalyzing GTP hydrolysis Dynasore inhibits dynamin-mediated endocytic pathways by blocking GTPase activity thus preventing vesicle scission during endocytosis In biological research dynasore is frequently used to investigate dynamin-dependent endocytosis in cellular and neuronal models facilitating studies on synaptic vesicle recycling membrane trafficking and signaling dynamics
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 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 AM966 1228690-19-4 10mM (in 1mL DMSO)
AM966 (CAS 1228690-19-4) is an orally bioavailable small-molecule antagonist that selectively targets Lysophosphatidic acid type 1 receptor (LPA1) AM966 exhibits potent inhibitory activity against LPA1 receptors from humans and mice with IC50 values of approximately 17 nM and 19 nM respectively demonstrating selectivity over other LPA receptor subtypes (LPA2 5) In vitro AM966 blocks LPA-mediated chemotactic responses in IMR-90 human lung fibroblasts A2058 human melanoma cells and CHO cell lines In vivo AM966 effectively attenuates lung fibrosis inflammation and associated weight loss in bleomycin-induced murine pulmonary fibrosis models highlighting its utility in research on fibrotic diseases
Apexbio Technology LLC Lafutidine 118288-08-7 10mM (in 1mL DMSO)
Lafutidine (CAS 118288-08-7) is a histamine H2 receptor antagonist that functions by inhibiting histamine-induced gastric acid secretion Through selective blockade of H2 receptors on gastric parietal cells it reduces basal and stimulated levels of gastric acid production Lafutidine is utilized in biomedical research exploring gastric physiology receptor signaling pathways and gastrointestinal pharmacology particularly in contexts related to acid-related disorders