Dimethyl Sulfoxide
Apexbio Technology LLC Fidaxomicin 873857-62-6 10mM (in 1mL DMSO)
Fidaxomicin is a macrocyclic antibiotic derived from Actinomycetes functioning through inhibition of bacterial RNA polymerase by targeting the -subunit thereby interfering with bacterial RNA synthesis It exhibits specific antibacterial effects against Clostridium difficile suppressing toxin production and reducing disease recurrence in Clostridium difficile infections (CDI) Fidaxomicin has entered phase III clinical investigation for treatment of CDI Experimental results indicate an intravenous LD50 of approximately 200 mg/kg in rats reported inhibitory concentrations (IC50) against C difficile RNA polymerase range in the nanomolar scale It is utilized in research for studying bacterial transcription mechanisms and evaluating treatment strategies aimed at CDI
Apexbio Technology LLC Brefeldin A(Synonyms: BFA, Ascotoxin, Cyanein, Decumbin, Brefeldin, γ), 10mM (in 1mL DMSO), CAS: 20350-15-6.
Brefeldin A (CAS 20350-15-6) commonly abbreviated as BFA is a small-molecule inhibitor targeting ATPase activity with a reported IC50 of approximately 0 2 M Its primary mechanism of action involves disruption of intracellular vesicle transport by blocking protein trafficking from the endoplasmic reticulum (ER) to the Golgi apparatus and inhibiting GTP/GDP exchange Through these activities BFA reduces ATP-mediated vesicular exocytosis thereby diminishing stimulus-dependent hyperalgesia Additionally it induces endoplasmic reticulum stress and promotes p53 expression in tumor cell models like MCF-7 and HeLa ultimately enhancing apoptosis in colorectal cancer cells (HCT116) BFA is widely employed as a pharmacological tool in cellular biology research to study protein secretion vesicular transport dynamics and ER stress pathways
Apexbio Technology LLC AST-1306 897383-62-9 10mM (in 1mL DMSO)
AST-1306 (CAS 897383-62-9) is an inhibitor of epidermal growth factor receptor (EGFR) and HER2 receptor tyrosine kinases In biochemical assays AST-1306 inhibits EGFR and HER2 kinase activity with IC50 values of 0 5 nM and 3 nM respectively It also demonstrates inhibitory activity against EGFR mutations such as T790M/L858R reducing receptor phosphorylation and downstream signaling in both cell-free and cellular systems In various animal tumor models including ErbB2-overexpressing and SK-OV-3 xenografts AST-1306 suppresses tumor growth and signaling pathways supporting its use in EGFR- and HER2-related oncology research
Apexbio Technology LLC ABT-199 1257044-40-8 10mM (in 1mL DMSO)
ABT-199 (CAS 1257044-40-8) is a selective small-molecule inhibitor targeting BCL-2 developed through structure-guided drug design By specifically interfering with the mitochondrial apoptotic pathway regulated by BCL-2 ABT-199 induces apoptosis predominately in cells dependent on BCL-2 signaling rather than BCL-XL In preclinical assessments ABT-199 exhibited antitumor activity against hematologic malignancies including BCL-2-dependent non-Hodgkin lymphoma (NHL) and acute myeloid leukemia (AML) cell lines and xenograft models while demonstrating minimal platelet toxicity
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 A-803467 944261-79-4 10mM (in 1mL DMSO)
A-803467 (CAS 944261-79-4) is a potent selective blocker of the voltage-gated sodium channel subtype NaV1 8 It inhibits human and rat recombinant NaV1 8 channels with IC50 values of approximately 79 nM and 45 nM respectively Its selectivity for NaV1 8 over other sodium channel subtypes (e g NaV1 2 NaV1 3 NaV1 5 and NaV1 7) is 300 1000 fold By specifically reducing activity in tetrodotoxin-resistant sodium currents of dorsal root ganglion neurons A-803467 suppresses induced and spontaneous action potential firing exhibiting analgesic properties in animal models of neuropathic and inflammatory pain
Apexbio Technology LLC Sitaxentan sodium(Synonyms: TBC11251, Sitaxsentan sodium, Thelin, Sitaxentan sodium hydrate, Sitaxentan sodium salt), 10mM (in 1mL DMSO), CAS: 210421-74-2.
Sitaxentan sodium (CAS 210421-74-2) is a small molecule compound functioning as an orally bioavailable and highly selective antagonist for endothelin receptor subtype A (ETA) By specifically inhibiting ETA receptor signaling sitaxentan sodium interferes with endothelin-1 mediated vasoconstriction and cellular proliferation pathways In biomedical research contexts it serves as a valuable tool for investigating endothelin-related physiological and pathological processes with particular relevance to studies on vascular disorders and pulmonary arterial hypertension
Apexbio Technology LLC Nepicastat (SYN-117) HCl 170151-24-3 10mM (in 1mL DMSO)
Nepicastat (SYN-117) HCl is a potent and selective inhibitor targeting dopamine -hydroxylase (DBH) an enzyme responsible for converting dopamine to norepinephrine in catecholamine biosynthesis pathways By inhibiting DBH activity Nepicastat decreases norepinephrine synthesis and concurrently elevates dopamine levels Preclinical studies conducted in animal models such as spontaneously hypertensive rats and canine models demonstrate a dose-dependent reduction of norepinephrine levels accompanied by elevation of dopamine concentration across central nervous system and cardiac tissues Nepicastat serves as a valuable research tool in investigating catecholamine homeostasis cardiovascular function sympathetic regulation and dopamine-mediated neurotransmission
Apexbio Technology LLC Floxuridine 50-91-9 10mM (in 1mL DMSO)
Floxuridine is an antineoplastic antimetabolite compound functioning through inhibition of thymidylate synthase leading to interference with thymidine nucleotide biosynthesis This interruption induces DNA replication stress characterized by formation of double-strand DNA breaks Floxuridine exposure activates cellular DNA damage response pathways specifically ATR and ATM kinase signaling cascades and leads to the phosphorylation of checkpoint kinase 1 (Chk1) This compound has been widely utilized in oncology research to analyze DNA damage mechanisms cellular proliferation inhibition and apoptosis induction in human tumor cell lines Floxuridine demonstrates antiproliferative activity in cell-based assays with reported IC50 values typically ranging between 50 nM and 500 nM depending on cell line and experimental conditions
Apexbio Technology LLC Roscovitine (Seliciclib,CYC202) 186692-46-6 10mM (in 1mL DMSO)
Roscovitine (Seliciclib CYC202 CAS number 186692-46-6) is a selective inhibitor of cyclin-dependent kinases (CDKs) It targets cdc2 (CDK1/cyclin B) CDK2 (CDK2/cyclin A and CDK2/cyclin E) and CDK5 (CDK5/p35) with reported IC50 values of 0 65 M 0 7 M 0 7 M and 0 16 M respectively Additionally roscovitine inhibits extracellular signal-regulated kinases Erk1 and Erk2 displaying IC50 values of 34 M and 14 M respectively In cellular studies roscovitine has been shown to delay or halt transitions during early mitosis specifically preventing cell progression from prophase to metaphase as observed in Xenopus oocyte maturation induced by progesterone Due to its distinct inhibitory profile roscovitine is commonly utilized in research examining cell cycle regulation and kinase signaling pathways relevant to oncology
Selleck Chemical LLC Trametinib DMSO solvate S4484-25mg
Trametinib DMSO solvate is a highly specific and potent MEK1/2 inhibitor with IC50 of 0 92 nM/1 8 nM in cell-free assay Trametinib activates autophagy and induces apoptosis
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
Cayman Chemical DMSO asy Reagent 1mL
A DPP-9 inhibitor (IC50 0.0034 UM) selective for DDP-9 over DPP-8 DPP-4 DPP-2 FAP and prolyl endopeptidase (IC50s 0.6 >10 >5 10 and >10 UM respectively) induces LDH release from THP-1 and HL-60 leukemia cells at 10 UM