Dimethyl Sulfoxide
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 Pacritinib (SB1518) 937272-79-2 10mM (in 1mL DMSO)
Pacritinib (SB1518) is a small molecule inhibitor targeting Janus kinase 2 (JAK2) and Fms-like tyrosine kinase 3 (FLT3) with IC50 values of 23 nM for wild-type JAK2 19 nM for JAK2V617F and 22 nM for FLT3 It inhibits phosphorylation of downstream effectors such as STAT5 and STAT3 mediated by JAK2 in Ba/F3 cells as well as phosphorylation of FLT3 and STAT5 in MV4-11 cells Pacritinib demonstrates good microsomal stability selectivity limited inhibitory activity toward CYP3A4 favorable permeability in cell permeability assays and oral bioavailability In preclinical studies treatment with pacritinib in Ba/F3-JAK2V617F murine allograft and MV4-11 xenograft models reduces disease progression and enhances survival These properties make pacritinib suitable for research concerning hematologic malignancies involving dysregulated JAK2 or FLT3 signaling pathways
Apexbio Technology LLC Salubrinal 405060-95-9 10mM (in 1mL DMSO)
Salubrinal is a cell-permeable inhibitor of eukaryotic translation initiation factor 2 alpha (eIF2 ) dephosphorylation exhibiting an IC50 of approximately 15 M It prevents phosphatase complexes from removing phosphate groups from eIF2 thus maintaining its phosphorylated state and modulating protein synthesis during cellular stress responses Salubrinal is utilized experimentally in vitro to investigate apoptotic mechanisms related to endoplasmic reticulum (ER) stress For instance it provides cytoprotection against ER stress-induced apoptosis triggered by protein glycosylation inhibitors or ER-Golgi trafficking inhibitors In vivo murine models employ salubrinal to explore cellular processes underlying oxidative stress and nephrotoxicity induced by chemotherapeutic treatments through modulation of ER stress-associated apoptosis signaling pathways Currently no clinical trials involving salubrinal have been reported
Apexbio Technology LLC Calpain Inhibitor II, ALLM 136632-32-1 10mM (in 1mL DMSO)
Calpain inhibitor II (also termed ALLM or CPI-2) is a membrane-permeable inhibitor targeting calpain I calpain II as well as cathepsin L and B Calpain inhibition by this compound can activate apoptosis via caspase-mediated pathways Studies conducted in acute lymphoblastic leukemia (ALL) cell lines (such as ALL-1 RS4 11 JURKAT) and non-Hodgkin s lymphoma (NHL) cells (including RAMOS DAUDI) revealed apoptosis induction at concentrations of 50 100 M Additionally apoptosis triggered by calpain inhibitor II appears independent of tyrosine kinases BTK and LYN Unlike calpain inhibitor I calpain inhibitor II does not influence NF- B signaling nor sensitize tumor cells to TRAIL-induced apoptosis This inhibitor is widely employed in apoptosis-related research and studies exploring calpain-associated cellular pathways
Apexbio Technology LLC AVL-292 1202757-89-8 10mM (in 1mL DMSO)
AVL-292 (CAS 1202757-89-8) also known as CC-292 is an orally bioavailable irreversible small-molecule inhibitor targeting Bruton s tyrosine kinase (BTK) a member of the Tec kinase family crucial for B-cell receptor (BCR) signaling pathways AVL-292 covalently binds the cysteine residue (Cys481) within BTK suppressing its autophosphorylation and downstream signaling Reported IC50 and EC50 values in biochemical and cellular assays are 0 5 nM and 8 nM respectively AVL-292 has shown efficacy in preclinical models such as collagen-induced arthritis (CIA) mice and demonstrates therapeutic potential in clinical studies involving B-cell malignancies including CLL B-NHL and WM
Apexbio Technology LLC Zebularine 3690-10-6 10mM (in 1mL DMSO)
Zebularine (CAS number 3690-10-6) is a chemically stable cytidine analog containing a 2-(1H)-pyrimidinone ring structure It acts primarily through inhibition of DNA methylation by forming covalent complexes with DNA methyltransferases Zebularine treatment leads to demethylation and reactivation of hypermethylation-mediated silenced genes exemplified by the p16 gene Additionally induced myogenic differentiation has been observed upon zebularine administration in 10T1/2 cells Zebularine displays minimal cytotoxicity in certain cell models such as T24 cells and retains stability in aqueous solutions across a broad pH range (up to pH 12) These properties make zebularine relevant for studies in epigenetic regulation and cellular differentiation
Apexbio Technology LLC Linifanib (ABT-869) 796967-16-3 10mM (in 1mL DMSO)
Linifanib (ABT-869 CAS 796967-16-3) is an ATP-competitive inhibitor of receptor tyrosine kinases targeting platelet-derived growth factor (PDGF) and vascular endothelial growth factor receptors (VEGFRs) as well as FMS-like tyrosine kinase 3 (FLT3) including its activating internal tandem duplication (ITD) mutations Linifanib selectively reduces cell growth in FLT3 ITD-expressing cell lines such as Ba/F3 FLT3 ITD cells inhibits phosphorylation of FLT3 and Akt and induces apoptosis preferentially in ITD mutant cells In vivo experiments with ITD-expressing leukemia xenografts show reduced leukemia progression and prolonged survival in mice treated orally with linifanib This compound is widely used in preclinical research for acute myeloid leukemia studies
Apexbio Technology LLC Epoxomicin 134381-21-8 10mM (in 1mL DMSO)
Epoxomicin (CAS 134381-21-8) is a naturally occurring proteasome inhibitor initially isolated from actinomycete cultures It acts primarily by forming covalent bonds through its -epoxyketone moiety with catalytic residues of the proteasome resulting in potent inhibition of the chymotrypsin-like (CTRL) activity of the 20S proteasome subunit Epoxomicin also inhibits proteasomal trypsin-like and peptidyl-glutamyl peptide hydrolysis activities albeit at significantly lower rates It exhibits anti-inflammatory and antitumor activities and is employed experimentally to study ubiquitin-proteasome-mediated cellular pathways bone formation regulation and Parkinson s disease model generation
Apexbio Technology LLC Maraviroc(Synonyms: Selzentry, Celsentri, UK-427857, MVC), 10mM (in 1mL DMSO), CAS: 376348-65-1.
Maraviroc (CAS 376348-65-1) is a potent selective antagonist of the chemokine receptor CCR5 CCR5 functions as a coreceptor expressed on immune cells and facilitates entry of certain HIV-1 virus strains (R5-tropic) By binding CCR5 maraviroc effectively blocks HIV-1 envelope protein gp120 anchoring and consequently prevents viral fusion and subsequent cell entry In cellular assays with CCR5-tropic HIV-1 maraviroc demonstrates substantial antiviral activity (IC50 approximately 2 0 nM) and efficiently inhibits gp120-CCR5 interaction Maraviroc serves as a valuable research tool to explore CCR5-mediated viral entry and HIV tropism dynamics
Apexbio Technology LLC Kaempferol(Synonyms: Kempferol, Kaempherol, Kaempferide, Robigenin, Rhamnolutein, Populnetin), 10mM (in 1mL DMSO), CAS: 520-18-3.
Kaempferol (CAS 520-18-3) is a naturally derived flavonoid isolated from sources including Gingko biloba and red wine It functions biologically by activating the mitochondrial calcium uniporter (EC50 7 M) Additionally kaempferol promotes apoptosis through the caspase-9 pathway by suppressing polo-like kinase 1 (PLK1) expression thereby inhibiting cancer cell proliferation in diverse cell lines It also demonstrates antioxidant properties and reduces osteoclast-mediated bone resorption in vitro These characteristics make kaempferol valuable for researching mitochondrial physiology cancer biology and bone metabolism
Apexbio Technology LLC RO4929097(Synonyms: RO-4929097, RO 4929097, Gamma-Secretase Inhibitor RO4929097, RO4929097 γ-secretase inhibitor), 10mM (in 1mL DMSO), CAS: 847925-91-1.
RO4929097 (CAS 847925-91-1) is a potent selective small-molecule inhibitor of -secretase an essential protease in the Notch signaling pathway It inhibits -secretase with high specificity (IC50 4 nM EC50 5 nM) showing minimal inhibitory activity against closely related proteases and over 100-fold selectivity versus a broad spectrum of other proteases By preventing Notch receptor cleavage and subsequent signaling activation RO4929097 suppresses proliferation and tumorigenesis across various tumor models including melanoma breast colorectal pancreatic and lung cancers Clinical studies have assessed RO4929097 alone or combined with other anticancer agents for advanced solid tumors