Dimethyl Sulfoxide
Apexbio Technology LLC PF-477736 952021-60-2 10mM (in 1mL DMSO)
PF-477736 is an ATP-competitive small-molecule inhibitor of checkpoint kinase 1 (Chk1) It selectively inhibits Chk1 kinase activity demonstrating nanomolar inhibitory potency in kinase assays and exhibits lower affinity toward related kinases such as CDK1 and Chk2 In vitro studies utilizing human cancer cell lines show PF-477736 disrupts Chk1-dependent G2-phase cell-cycle arrest induced by DNA-damaging agents preferentially targeting tumor cells with compromised p53 function while minimizing cytotoxicity to normal cells PF-477736 is widely utilized experimentally to study DNA damage response mechanisms potential chemosensitizing effects and therapeutic implications for cancers harboring p53 mutations
Apexbio Technology LLC SM-164 957135-43-2 10mM (in 1mL DMSO)
SM-164 (CAS 957135-43-2) is a bivalent small molecule mimetic of the endogenous inhibitor Smac designed to antagonize cellular inhibitor of apoptosis proteins (cIAP-1 cIAP-2) and X-linked inhibitor of apoptosis protein (XIAP) By binding specifically to the BIR2 and BIR3 domains of cIAP-1 and XIAP as well as the BIR3 domain of cIAP-2 (Ki of 0 31 nM 0 56 nM and 1 1 nM respectively) SM-164 promotes degradation of cIAP-1 and inhibition of XIAP In tumor cells this leads to caspase activation and TNF -dependent apoptosis SM-164 is utilized in cancer research to investigate apoptosis regulation and anticancer therapy strategies
Apexbio Technology LLC Dacomitinib (PF299804, PF299) 1110813-31-4 10mM (in 1mL DMSO)
Dacomitinib (PF299804 CAS 1110813-31-4) is an irreversible pan-HER small-molecule inhibitor that targets the epidermal growth factor receptor (EGFR/ErbB-1) ERBB2 (HER2) and ERBB4 (HER4) It acts by covalently binding EGFR family tyrosine kinases inhibiting downstream signaling through phospho-HER family proteins AKT and ERK Dacomitinib shows activity in vitro inducing G0/G1 cell cycle arrest and apoptosis and suppresses proliferation in trastuzumab- or lapatinib-resistant HER2-amplified breast cancer cell lines In vivo studies demonstrate antitumor effects in EGFR-mutant (e g T790M) gefitinib-resistant lung cancer xenografts making it relevant for non-small cell lung cancer research
Apexbio Technology LLC TG100-115 677297-51-7 10mM (in 1mL DMSO)
TG100-115 (CAS 677297-51-7) is a selective inhibitor targeting phosphoinositide 3-kinase isoforms PI3K and PI3K with IC50 values of 83 nM and 235 nM respectively exhibiting negligible inhibition towards PI3K and PI3K Research in murine models demonstrates that treatment with TG100-115 significantly reduces eosinophil accumulation bronchoalveolar IL-13 cytokine levels mucus deposition and leukocyte infiltration associated with allergic asthma decreasing airway hyperresponsiveness by approximately 50% Moreover this compound attenuates neutrophil infiltration and TNF induction following exposure to cigarette smoke and LPS suggesting its utility as an investigational tool for asthma and inflammatory pulmonary diseases
Apexbio Technology LLC PD123319 130663-39-7 10mM (in 1mL DMSO)
PD123319 (CAS 130663-39-7) is a non-peptide antagonist targeting angiotensin II (Ang II) receptors particularly the AT2 receptor subtype It binds selectively exhibiting an IC50 of 34 nM in rat adrenal assays and 210 nM in rat brain binding assays Additionally PD123319 inhibits Ang II binding to bovine adrenal glomerulosa microsomal preparations with an IC50 of 6 9 nM Its antagonistic activity leads to reduced cyclic GMP synthesis and elevated prostaglandin E2 production without altering protein tyrosine phosphorylation or thymidine incorporation mediated by Ang II PD123319 serves as a useful pharmacological tool in investigating Ang II receptor signaling pathways
Apexbio Technology LLC Z-FA-FMK 105637-38-5;197855-65-5 10mM (in 1mL DMSO)
Z-FA-FMK is a peptidyl fluoromethyl ketone inhibitor targeting cysteine proteases specifically cathepsins such as cathepsin B and certain caspases It does not require a P1 aspartate residue for inhibition Mechanistically Z-FA-FMK suppresses the enzyme activity of effector caspases (including caspases-2 -3 -6 and -7) but shows minimal impact on initiator caspases (caspase-8 and caspase-10) and only partial attenuation of caspase-9 activity As a negative control inhibitor Z-FA-FMK is regularly applied in apoptosis research to differentiate specific caspase-dependent signaling pathways and to assess the role of cathepsins and caspases in biological contexts such as cell death mechanisms and related pathways
Apexbio Technology LLC Sirtinol 410536-97-9 10mM (in 1mL DMSO)
Sirtinol (CAS 410536-97-9) is a small-molecule inhibitor targeting class III histone deacetylases (HDAC) specifically the NAD-dependent deacetylases SIRT1 and SIRT2 In MCF-7 human breast cancer cells sirtinol exhibits inhibitory activity against cell proliferation with IC50 values of 48 6 M (24 h) and 43 5 M (48 h) Mechanistically sirtinol reduces SIRT1 expression inducing acetylation of p53 and downregulating cell-cycle proteins such as cyclin B1 cyclin D1 CDK2 and CDK6 leading to G1-phase arrest apoptosis and autophagy This molecule serves as a valuable research tool in epigenetic studies and cancer biology investigations
Apexbio Technology LLC Mupirocin 12650-69-0 10mM (in 1mL DMSO)
Mupirocin is an antibiotic targeting bacterial protein synthesis by inhibition of isoleucyl-tRNA synthetase Structurally analogous to isoleucine it binds the enzyme s active site blocking formation of isoleucyl-tRNA thus arresting bacterial protein production with reported MIC values around 0 05 g/ml for Staphylococcus aureus Primarily active against Gram-positive strains notably methicillin-resistant Staphylococcus aureus (MRSA) it is widely applied in biomedical research focused on antimicrobial resistance soft tissue infections biofilm studies and nasal colonization control strategies
Apexbio Technology LLC AG-1478 153436-53-4 10mM (in 1mL DMSO)
AG-1478 is a selective inhibitor of epidermal growth factor receptor (EGFR) a receptor tyrosine kinase involved in cellular proliferation and survival It inhibits EGFR-mediated Erk1/2 phosphorylation induced by EGF stimulation with an IC50 of approximately 10 M in Ishikawa ovarian cell lines In experimental cancer research AG-1478 has been applied to study EGFR signaling mechanisms by reducing receptor phosphorylation and downstream pathway activation Studies using diverse cancer cell lines including ovarian (CAOV-3 SKOV-3) colorectal (SW480) hepatocellular (HA22T/VGH) and lung (A549) carcinomas employ AG-1478 to investigate EGFR s role in tumor growth and chemoresistance Additionally AG-1478 is utilized in preclinical xenograft models to assess tumor growth modulation via EGFR inhibition
Apexbio Technology LLC DMXAA (Vadimezan) 117570-53-3 10mM (in 1mL DMSO)
DMXAA (Vadimezan AS-1404) is a tumor vascular disrupting and apoptosis-inducing agent functioning primarily through inhibition of DT-diaphorase (DTD) It acts by suppressing DTD enzymatic activity showing an IC50 of approximately 62 5 M Additionally DMXAA inhibits various kinases notably VEGFR2 disrupting endothelial cells and blood vessel formation to induce tumor cell apoptosis and vascular necrosis Experimentally DMXAA demonstrates activity in murine tumor models including induction of apoptosis in endothelial cells and tumor vasculature promoting necrosis and tumor regression Therefore DMXAA is commonly used in oncology research focused on anti-angiogenesis and tumor vascular disruption mechanisms
Apexbio Technology LLC Wortmannin 19545-26-7 10mM (in 1mL DMSO)
Wortmannin is a selective inhibitor targeting phosphatidylinositol-3-kinase (PI3K) with reported IC50 of approximately 1 9 nM It inhibits PI3K through an ATP-noncompetitive binding mechanism interacting directly with the catalytic region Additionally wortmannin functions as a noncompetitive inhibitor of myosin light chain kinase (MLCK) with an IC50 around 1 9 M thus decreasing myosin light chain phosphorylation and associated smooth muscle contraction In biomedical research wortmannin is commonly employed to dissect the PI3K signaling pathway evaluate smooth muscle contractility and explore therapeutic potentials related to vascular dilation and inflammation modulation
Apexbio Technology LLC Axitinib (AG 013736) 319460-85-0 10mM (in 1mL DMSO)
Axitinib (CAS 319460-85-0) also known as AG 013736 is an orally bioavailable selective inhibitor targeting vascular endothelial growth factor receptor (VEGFR) tyrosine kinases 1 2 and 3 It inhibits VEGFR phosphorylation with IC50 values of approximately 0 1 nM (VEGFR-1) 0 2 nM (VEGFR-2) and 0 1 0 3 nM (VEGFR-3) and demonstrates significantly higher selectivity relative to FGFR-1 Axitinib reduces phosphorylation of VEGF-mediated intracellular signaling proteins Akt eNOS and ERK1/2 and exhibits in vivo suppression of VEGFR-2 activation (EC50 0 49 nM) Its antiangiogenic action results in tumor growth delay in human xenograft models (e g HCT-116 SN12C) highlighting its utility in cancer 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 GW501516 317318-70-0 10mM (in 1mL DMSO)
GW501516 is a subtype-selective synthetic agonist targeting peroxisome proliferator-activated receptor delta (PPAR ) exhibiting a Ki value of approximately 1 1 nM PPAR widely expressed in various tissues mediates cholesterol metabolism and interacts with retinoid X receptor (RXR) In cellular reporter assays utilizing a GAL4-driven system GW501516 activates PPAR -dependent transcription with an EC50 value close to 1 2 nM and demonstrates roughly 1000-fold greater selectivity toward PPAR compared to other PPAR isoforms Experimental studies in primate models of metabolic disease have shown GW501516 promotes HDL-cholesterol elevation reduces fasting triglycerides modifies LDL/VLDL particle profiles to larger forms enhances cholesterol efflux via increasing ABCA1 expression and partially reduces hyperinsulinemia without adverse effects on glucose handling GW501516 serves as a research tool for exploring the mechanisms and functions of PPAR activation in metabolic regulation
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