Dimethyl Sulfoxide
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 Dapivirine (TMC120) 244767-67-7 10mM (in 1mL DMSO)
Dapivirine (TMC120) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) targeting HIV-1 viral replication By binding directly to HIV-1 reverse transcriptase dapivirine inhibits viral RNA-dependent DNA polymerase activity thus blocking viral DNA synthesis Dapivirine demonstrates activity against HIV-1 reverse transcriptase with reported IC50 values in the low nanomolar range (approximately 1-10 nM) Due to its molecular specificity and promising in vitro antiviral profile dapivirine is widely utilized in biomedical research exploring topical prevention strategies particularly in the development of vaginal microbicides aimed at reducing HIV transmission
Apexbio Technology LLC Etodolac 41340-25-4 10mM (in 1mL DMSO)
Etodolac (CAS 41340-25-4) is a selective cyclooxygenase-2 (COX-2) inhibitor belonging to the class of non-steroidal anti-inflammatory drugs (NSAIDs) It exhibits inhibitory activity against COX-2 with an IC50 of 53 5 nM Etodolac is commonly utilized for research involving inflammatory conditions such as osteoarthritis and rheumatoid arthritis In isolated rabbit articular chondrocytes stimulated with TNF Etodolac prevented apoptotic cell shrinkage and suppressed caspase-3/7 activation Conversely in human malignant rhabdoid tumor cells (FRTK-1) Etodolac induced apoptosis in a dose-dependent manner increasing activities of caspase-3 -8 and -9
Apexbio Technology LLC A66 1166227-08-2 10mM (in 1mL DMSO)
A66 (CAS 1166227-08-2) is a selective inhibitor of the p110 catalytic subunit of class I phosphatidylinositol-4 5-bisphosphate 3-kinase (PI3K) with an IC50 of 32 nM This compound specifically decreases phosphorylation of Akt/PKB and downstream S6K at Thr389 in various cell models including PIK3CA-mutant H1047R cell lines C2C12 myoblasts and 3T3-L1 adipocytes In animal studies A66 reduces tumor growth in xenograft models and improves insulin sensitivity under chronic metabolic stress highlighting its utility in research on PI3K signaling in cancer and metabolic disease
Apexbio Technology LLC Cyclo (-RGDfK) 161552-03-0 10mM (in 1mL DMSO)
Cyclo(-RGDfK) is a cyclic pentapeptide that functions as an inhibitor targeting the integrin v 3 Integrins are transmembrane receptors mediating cell adhesion by recognizing specific peptide sequences notably the Arg-Gly-Asp (RGD) motif Integrin v 3 is involved in cell adhesion processes such as angiogenesis tissue remodeling and tumor development and is abundantly expressed on activated endothelial cells and various tumor cells Cyclo(-RGDfK) specifically binds integrin v 3 disrupting integrin-mediated cell attachment Consequently it is frequently utilized in bioengineering applications to modify biomaterial surfaces for enhanced cellular adherence and integration Additionally cyclo(-RGDfK) serves as a targeting ligand in imaging probes aimed at localizing integrin-positive tissues in cancer research
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 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 Forskolin 66575-29-9 10mM (in 1mL DMSO)
Forskolin (CAS 66575-29-9) is a diterpenoid isolated from the plant Coleus forskohlii known to directly activate adenylate cyclase type I thereby elevating cellular cyclic AMP (cAMP) concentrations It exhibits an IC50 of approximately 41 nM against adenylate cyclase By increasing intracellular cAMP forskolin modulates signaling pathways involved in inflammation and oxidative stress reducing macrophage activation and subsequent production of thromboxane B2 and superoxide Forskolin has been explored in various experimental models and clinical contexts including cardiovascular disorders diabetes mellitus and asthma research
Apexbio Technology LLC Sephin1 13098-73-2 10mM (in 1mL DMSO)
Sephin1 (CAS 13098-73-2) is a selective inhibitor of PPP1R15A a regulatory subunit of protein phosphatase 1 involved in the regulation of stress-induced eIF2 dephosphorylation Under endoplasmic reticulum (ER) stress phosphorylated eIF2 attenuates protein synthesis preventing accumulation of misfolded proteins By inhibiting PPP1R15A Sephin1 sustains eIF2 phosphorylation extending translational attenuation during ER stress In cell assays Sephin1 selectively disrupts PPP1R15A-PP1c complexes without affecting PPP1R15B-mediated complexes In mouse models harboring misfolded protein mutations (e g MPZ or SOD1) Sephin1 administration mitigates molecular cellular and functional deficits thus relevant for proteostasis-related disease studies
Apexbio Technology LLC Carbadox 6804-07-5 10mM (in 1mL DMSO)
Carbadox is an antibiotic compound employed in bacterial infection research primarily targeting pathogenic organisms associated with gastrointestinal infections in swine including swine dysentery Its antibacterial mechanism involves inhibition of bacterial DNA synthesis and disruption of nucleic acid metabolism thereby interfering with pathogen replication Carbadox is frequently utilized in microbiology studies investigating therapeutic interventions against enteric bacterial pathogens under controlled laboratory conditions In vitro studies report Carbadox demonstrating bacteriostatic activity with IC50 values typically ranging between 0 5 2 g/mL for common susceptible bacterial strains serving as a reference substance in microbial sensitivity assays
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 Pirarubicin 72496-41-4 10mM (in 1mL DMSO)
Pirarubicin is a DNA intercalating anthracycline antibiotic structurally related to doxorubicin that targets the DNA topoisomerase II enzyme By stabilizing the cleavable DNA-enzyme complex pirarubicin induces DNA strand breaks and inhibits DNA replication and cellular proliferation Its primary mode of action involves disruptive interactions with topoisomerase II-mediated DNA cleavage and repair mechanisms Pirarubicin is utilized as an antineoplastic agent in oncology research particularly in evaluating its activity against diverse cancer cell lines In vitro studies reported IC50 values typically ranging from approximately 0 1 to several micromolar concentrations varying according to cell type and experimental conditions Therefore pirarubicin serves as a tool compound in pharmacological studies investigating DNA-topoisomerase inhibitors and therapeutic resistance mechanisms
Apexbio Technology LLC Fluvastatin Sodium 93957-55-2 10mM (in 1mL DMSO)
Fluvastatin Sodium (CAS 93957-55-2) is an inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase the rate-limiting enzyme in cholesterol biosynthesis By blocking HMG-CoA reductase activity fluvastatin reduces serum total cholesterol LDL-cholesterol and apolipoprotein B while increasing HDL-cholesterol and apolipoprotein A-I levels In research settings fluvastatin exhibits anti-atherosclerotic anti-thrombotic and antioxidant properties Studies have shown fluvastatin decreases platelet aggregation dose-dependently in vitro reducing platelet aggregation by approximately 10-15% at clinical doses (40 mg/day) Additionally fluvastatin inhibits inflammatory angiogenesis and NO production suggesting potential applications in inflammatory and cardiovascular research
Apexbio Technology LLC Evacetrapib (LY2484595) 1186486-62-3 10mM (in 1mL DMSO)
Evacetrapib (LY2484595 CAS 1186486-62-3) is a potent and selective inhibitor targeting cholesteryl ester transfer protein (CETP) a regulator of lipid metabolism Evacetrapib exhibits inhibitory activity with IC50 values of 5 5 nM in assays containing recombinant human CETP and 26 nM within human plasma CETP assays In vivo oral administration at 30 mg/kg in human CETP/ApoAI double-transgenic mice significantly reduces CETP activity and elevates HDL-cholesterol concentration (ED50 5 mg/kg) Evacetrapib does not elevate blood pressure nor induce aldosterone or cortisol synthesis in model systems highlighting its potential in cardiovascular research related to coronary artery disease
Apexbio Technology LLC THZ2 1604810-84-5 10mM (in 1mL DMSO)
THZ2 (CAS 1604810-84-5) is a selective inhibitor of cyclin-dependent kinase 7 (CDK7) demonstrating an IC50 of 13 9 nM CDK7 a serine/threonine kinase bound and activated by cyclins regulates cell cycle progression and transcriptional control through phosphorylation of RNA polymerase II (RNAPII) In triple-negative breast cancer (TNBC) cell models THZ2 reduces cellular proliferation induces apoptotic cell death without affecting cell-cycle distribution and inhibits colony formation at low-nanomolar concentrations (IC50 10 nM) In xenograft mouse models THZ2 suppresses tumor growth without noticeable toxicity Thus THZ2 is useful in research investigating CDK7-mediated oncogenic mechanisms in cancer