Dimethyl Sulfoxide
Apexbio Technology LLC SP2509 1423715-09-6 10mM (in 1mL DMSO)
SP2509 (CAS 1423715-09-6) is a small molecule antagonist of lysine-specific demethylase 1 (LSD1/KDM1A) a histone-modifying enzyme responsible for demethylating mono- and dimethylated histone H3 lysine 4 (H3K4) SP2509 potently inhibits LSD1 activity (IC50 13 nM) without affecting monoamine oxidase isoforms MAO-A or MAO-B In acute myeloid leukemia (AML) cells SP2509 suppresses LSD1 function reduces colony formation induces apoptosis enhances promoter-specific H3K4 trimethylation and stimulates differentiation through upregulation of p53 p21 and C/EBP Its efficacy has been demonstrated in AML xenograft models supporting its utility as a tool compound for cancer research
Apexbio Technology LLC NSC23766 trihydrochloride 1177865-17-6 10mM (in 1mL DMSO)
NSC23766 trihydrochloride (CAS 1177865-17-6) is a selective inhibitor of the Rac1 GTPase It functions by binding specifically to guanine nucleotide exchange factors (GEFs) such as Trio and Tiam preventing their interaction with Rac1 and thus inhibiting Rac1 activation NSC23766 demonstrates an IC50 of approximately 50 M It has been used in various cellular models to study Rac1-dependent processes including endothelial barrier integrity and apoptosis regulation By modulating Rac1 activity NSC23766 serves as a tool compound for investigating the role of Rac signaling pathways in cellular apoptosis especially TNF- -induced JNK activation and barrier function dynamics
Apexbio Technology LLC Eptifibatide 188627-80-7 10mM (in 1mL DMSO)
Eptifibatide is a cyclic heptapeptide belonging to the glycoprotein IIb/IIIa inhibitor category functioning as an antagonist of platelet adhesion by reversibly binding to the platelet glycoprotein IIb/IIIa receptor This receptor located on platelet surfaces mediates platelet aggregation through binding fibrinogen and von Willebrand factor processes essential in thrombus formation By blocking the GP IIb/IIIa receptor binding site Eptifibatide inhibits fibrinogen-dependent platelet cross-linking reducing platelet aggregation In biomedical research Eptifibatide serves as a pharmacological tool to investigate platelet function thrombosis mechanisms and related cardiovascular diseases in preclinical and clinical models
Apexbio Technology LLC CPI-169 1450655-76-1 10mM (in 1mL DMSO)
CPI-169 is a selective small-molecule inhibitor targeting enhancer of zeste homolog 2 (EZH2) a catalytic component of polycomb repressive complex 2 (PRC2) By inhibiting EZH2 enzymatic activity CPI-169 suppresses methylation at histone H3 lysine 27 (H3K27me3) thereby altering chromatin structure and gene expression profiles Pharmacological experiments demonstrate inhibition of EZH2 with subnanomolar IC50 values and cellular studies indicate reductions of H3K27 trimethylation at nanomolar concentrations CPI-169 has been utilized experimentally to investigate EZH2-dependent epigenetic processes cell proliferation apoptosis pathways and therapeutic potential particularly in lymphoma and cancer biology studies employing in vitro and in vivo models
Apexbio Technology LLC LDC1267 1361030-48-9 10mM (in 1mL DMSO)
LDC1267 (CAS 1361030-48-9) is a selective inhibitor of the TAM receptor tyrosine kinases Mer Tyro3 and Axl demonstrating IC50 values of less than 5 nM 8 nM and 29 nM respectively By inhibiting TAM signaling LDC1267 abolishes Gas6-mediated suppression in NKG2D-activated natural killer (NK) cells thus enhancing NK-mediated cytotoxicity Preclinical studies show reduced metastasis of melanoma and 4T1 breast tumor cells upon LDC1267 administration in mouse models an effect reliant on NK cell function LDC1267 provides a research tool for investigating TAM-regulated immune modulation in cancer models
Apexbio Technology LLC Vardenafil 224785-90-4 10mM (in 1mL DMSO)
Vardenafil (CAS 224785-90-4) is a potent and selective inhibitor of phosphodiesterase type 5 (PDE5) It inhibits PDE5 enzyme activity with an IC50 of approximately 0 7 nM in vitro Compared with other PDE isoforms (PDE1-4 and PDE6) vardenafil demonstrates superior selectivity toward PDE5 though moderate inhibition of PDE6 (IC50 11 nM) is observed Vardenafil enhances cGMP accumulation in human corpus cavernosum and significantly potentiates nitric oxide (SNP)- acetylcholine- and electrical field stimulation-induced relaxation in human trabecular smooth muscle Its vasodilatory effects render it suitable for research in erectile function and related vascular physiology
Apexbio Technology LLC A939572 1032229-33-6 10mM (in 1mL DMSO)
A939572 (CAS 1032229-33-6) is an orally bioavailable small-molecule inhibitor targeting stearoyl-CoA desaturase 1 (SCD1) an enzyme that catalyzes the formation of monounsaturated fatty acids involved in lipid metabolism and body weight regulation A939572 selectively inhibits human and mouse SCD1 with IC50 values of 37 nM and 4 nM respectively exhibiting no inhibitory effect on associated cofactors cytochrome b5 or cytochrome b5 reductase By specifically interacting with SCD1 A939572 serves as a pharmacological tool in metabolic research particularly in studies focused on obesity and diabetes
Apexbio Technology LLC CGP 57380 522629-08-9 10mM (in 1mL DMSO)
CGP 57380 (CAS 522629-08-9) is a specific and selective inhibitor targeting the serine/threonine kinase MNK1 an enzyme implicated in translation regulation via phosphorylation of the eukaryotic initiation factor 4E (eIF4E) It inhibits MNK1 activity in vitro with an IC50 of approximately 2 2 M CGP 57380 suppresses stimulus-induced phosphorylation of eIF4E in various cellular contexts including 293 cells vascular smooth muscle cells and macrophages reducing translation of mRNAs encoding proinflammatory mediators such as TNF- IL-6 and monocyte chemoattractant protein-1 (MCP-1) Hence CGP 57380 is valuable for investigating MNK1-mediated translational control in inflammation and cell signaling
Apexbio Technology LLC PD98059 167869-21-8 10mM (in 1mL DMSO)
PD98059 (CAS 167869-21-8) is a selective reversible inhibitor of MAP kinase kinase (MEK/MAPK/ERK kinase) It specifically targets MEK1 affecting both basal and partially activated forms with a reported IC50 of approximately 10 M Treatment with PD98059 inhibits ERK1/2 phosphorylation in a dose-dependent manner resulting in downregulation of cyclin E/Cdk2 and cyclin D1/Cdk4 complexes In cell-based studies such as human leukemia U937 cell models treatment leads to cell growth arrest at the G1 phase and induction of apoptosis PD98059 is widely employed in research investigating signaling pathways involving ERK activation cell cycle regulation and apoptosis
Apexbio Technology LLC U-73122 112648-68-7 10mM (in 1mL DMSO)
U-73122 (CAS 112648-68-7) is a phospholipase C (PLC) inhibitor utilized in biomedical research By selectively targeting PLC an enzyme responsible for hydrolyzing phosphatidylinositol 4 5-bisphosphate into intracellular messengers diacylglycerol and inositol-triphosphate U-73122 attenuates downstream signaling events such as protein kinase C activation and intracellular calcium release In vitro U-73122 inhibits recombinant human PLC- 2 with an IC50 of approximately 6 M while minimally affecting PLC- 1 3 and 4 isoforms In animal models U-73122 demonstrates anti-inflammatory properties reducing carrageenan-induced rat paw edema and TPA-induced mouse ear edema
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 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