Dimethyl Sulfoxide
Apexbio Technology LLC Rivaroxaban 366789-02-8 10mM (in 1mL DMSO)
Rivaroxaban (CAS 366789-02-8) is a small molecule inhibitor targeting coagulation Factor Xa a serine protease essential in the thrombin generation pathway involved in clot formation It binds reversibly to the S1 pocket of Factor Xa engaging specifically through interactions between its chlorothiophene moiety and the Tyr288 residue Binding kinetics are rapid (kon 1 7 10 7 mol L 1 s 1 koff 5 10 3 s 1) and affinity is high (Ki 0 4 nmol/L) Rivaroxaban is studied extensively in thrombosis research including venous thromboembolism stroke prevention in atrial fibrillation and cardiovascular event management post-acute coronary syndrome
Apexbio Technology LLC Bedaquiline 843663-66-1 10mM (in 1mL DMSO)
Bedaquiline a diarylquinoline antibiotic targets Mycobacterium tuberculosis via dual inhibition of subunits c and within the bacterial F1FO-ATP synthase complex disrupting ATP production It is applied primarily in research addressing multi-drug resistant (MDR) tuberculosis Recent studies have expanded its use into oncology where bedaquiline inhibits mitochondrial respiratory function and reduces glycolytic activity in cancer stem-cell-like populations In vitro experiments employing breast cancer MCF7 cells revealed bedaquiline increased ROS levels and reduced mitochondrial membrane potential Reported IC50 values for growth inhibition range approximately 1-10 M depending on cell lines and experimental conditions
Apexbio Technology LLC Pexidartinib (PLX3397) 1029044-16-3 10mM (in 1mL DMSO)
Pexidartinib (PLX3397 CAS 1029044-16-3) is a small molecule inhibitor targeting colony-stimulating factor 1 receptor (CSF-1R) a receptor tyrosine kinase involved in macrophage recruitment and activation Through inhibition of CSF-1R activity this compound reduces macrophage infiltration and accumulation demonstrated by diminished macrophage levels in B16F10 melanoma models without affecting Gr-1 myeloid-derived suppressor cells In vivo studies using GL261 glioma models in C57 mice indicate decreased microglial infiltration upon oral dosing with PLX3397 Clinically combined treatment with Pexidartinib and paclitaxel is under evaluation in advanced solid tumors and breast cancer trials
Apexbio Technology LLC G007-LK 1380672-07-0 10mM (in 1mL DMSO)
G007-LK (CAS 1380672-07-0) is a small molecule inhibitor that selectively targets tankyrase 1 and 2 (TNKS1/2) enzymes within the poly(ADP-ribose) polymerase family that modulate protein complexes through ADP-ribosylation G007-LK inhibits TNKS1 and TNKS2 with IC50 values of 46 nM and 25 nM respectively reducing their auto-poly(ADP-ribosylation) activity Treatment with G007-LK decreases -catenin levels in APC-mutated colorectal cancer cells by promoting formation of -catenin degradation complexes In xenograft mouse models using COLO-320DM cells G007-LK administration suppresses tumor growth dose-dependently indicating its utility in oncology research focusing on the Wnt/ -catenin pathway
Apexbio Technology LLC Dronedarone 141626-36-0 10mM (in 1mL DMSO)
Dronedarone (CAS 141626-36-0) is a benzofuran derivative structurally related to amiodarone designed to manage cardiac arrhythmias It exerts its pharmacological effects primarily through multichannel blockade inhibiting sodium potassium and calcium ion currents and demonstrating anti-adrenergic properties By prolonging action potential duration and refractory periods dronedarone contributes to the stabilization and restoration of regular cardiac rhythm In biomedical research contexts dronedarone serves as a valuable tool for exploring arrhythmogenesis mechanisms and developing therapeutic approaches for atrial fibrillation and atrial flutter
Apexbio Technology LLC Cyclophosphamide monohydrate 6055-19-2 10mM (in 1mL DMSO)
Cyclophosphamide monohydrate is an alkylating cytotoxic agent exhibiting antitumor activity primarily via metabolic activation As a prodrug it undergoes hepatic biotransformation mediated by cytochrome P450 enzymes forming active alkylating metabolites such as 4-hydroxycyclophosphamide which exert cytotoxic effects through interactions with cellular DNA Cyclophosphamide also reversibly inhibits acetylcholinesterase (AChE) displaying an IC50 of approximately 511 M It is widely utilized in experimental cancer studies particularly in pediatric oncology where alterations in drug metabolism or drug-drug interactions impacting cyclophosphamide clearance and therapeutic outcomes have been explored
Apexbio Technology LLC Golvatinib (E7050) 928037-13-2 10mM (in 1mL DMSO)
Golvatinib (E7050 CAS 928037-13-2) is a small-molecule inhibitor targeting the tyrosine kinases c-Met and VEGFR-2 Golvatinib inhibits phosphorylation of c-Met in MKN45 gastric cancer cells and VEGFR-2 in human umbilical vein endothelial cells (HUVECs) with IC50 values of 14 nM and 16 nM respectively Additionally it suppresses proliferation of various tumor cells including MKN45 EBC-1 Hs746T and SNU-5 and inhibits tumor growth in xenograft models via reduction of c-Met and VEGFR-2-mediated pathways Golvatinib is utilized in cancer research to explore targeted antitumor efficacy related to angiogenesis and oncogenic signaling
Apexbio Technology LLC Panobinostat (LBH589) 404950-80-7 10mM (in 1mL DMSO)
Panobinostat (LBH589) is a histone deacetylase (HDAC) inhibitor targeting class I II and IV HDAC enzymes regulating gene expression through histone hyperacetylation In vitro studies indicate panobinostat induces apoptosis and growth arrest in Ph-negative acute lymphoblastic leukemia (ALL) cell lines T-cell (MOLT-4) and pre-B cell (Reh) via caspase activation PARP cleavage and downregulation of c-Myc accompanied by H3K9 and H4K8 hyperacetylation and elevation of cell-cycle regulators (p21 p27) Panobinostat has shown anti-proliferative effects in various cancer models including cutaneous T-cell lymphoma and multiple myeloma (IC50 5-30 nM) and serves as a research tool in studies assessing epigenetic regulation and tumor biology
Apexbio Technology LLC LB42708 226929-39-1 10mM (in 1mL DMSO)
LB42708 (CAS 226929-39-1) is a selective small-molecule inhibitor of farnesyltransferase (FTase) belonging to a non-peptidic pyrrole-based class It blocks FTase-mediated farnesylation of H-Ras N-Ras and K-Ras4B demonstrated by low nanomolar IC50 values (0 8 nM 1 2 nM and 2 nM respectively) LB42708 shows minimal inhibitory effect on geranylgeranyltransferase I In vitro studies indicate inhibition of Ras-driven signaling pathways decreasing Ras activation and subsequently suppressing VEGF-stimulated endothelial proliferation and migration Researchers use LB42708 in oncology and inflammation studies exemplified by reduced tumor growth in Ras-mutant HCT116 and wild-type Caco-2 xenograft models
Apexbio Technology LLC WZ4002 1213269-23-8 10mM (in 1mL DMSO)
WZ4002 (CAS 1213269-23-8) is an irreversible EGFR tyrosine kinase inhibitor that selectively targets mutant epidermal growth factor receptor (EGFR) variants It potently inhibits autophosphorylation of EGFR mutants including T790M L858R/T790M delE746 A750/T790M L858R and delE746 A750 at low nanomolar Ki values Compared to wild-type EGFR mutant EGFR demonstrates greater sensitivity to WZ4002 at lower concentrations limiting off-target toxicity in normal tissues WZ4002 serves as a research tool for studying EGFR-driven tumorigenesis and therapeutic resistance in oncology models
Apexbio Technology LLC ML347 1062368-49-3 10mM (in 1mL DMSO)
ML347 (CAS 1062368-49-3) is a potent and selective inhibitor of bone morphogenetic protein (BMP) type I receptors specifically targeting ALK2 Mechanistically ML347 selectively inhibits ALK2 kinase activity with an IC50 of 32 nM while also inhibiting ALK1 with a comparable IC50 of 46 nM Notably ML347 displays approximately 300-fold selectivity for ALK2 over ALK3 and lacks inhibitory activity against closely related kinases such as ALK6 and KDR In the BMP4-induced C2C12BRA cell-based assay ML347 exhibits inhibitory activity with an IC50 of 152 nM As a selective ALK2 inhibitor ML347 serves as a valuable probe in BMP pathway research
Apexbio Technology LLC LY2835219 1231930-82-7 10mM (in 1mL DMSO)
LY2835219 (CAS 1231930-82-7) is a selective orally bioavailable inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6) It targets CDK4 and CDK6 with reported IC50 values of 2 nM and 10 nM respectively thereby reducing phosphorylation of the retinoblastoma protein (Rb) This mechanism leads to cell-cycle arrest during the G1 phase and subsequent inhibition of tumor cell proliferation LY2835219 demonstrates the capacity to cross the blood-brain barrier indicating its potential utility in research involving primary or metastatic intracranial tumors
Apexbio Technology LLC Dioscin 19057-60-4 10mM (in 1mL DMSO)
Dioscin (CAS 19057-60-4) is a steroidal saponin isolated primarily from Dioscorea nipponica Makino Structurally it belongs to glycosidic steroid derivatives known for modulating various biological pathways Dioscin exerts bioactivity predominantly through regulation of cellular signaling cascades such as apoptosis induction anti-inflammatory responses and oxidative stress reduction Studies suggest that dioscin interacts with signaling pathways including PI3K/Akt ERK/MAPK and NF- B Due to these activities dioscin is commonly investigated for its potential anti-inflammatory anticancer and antioxidant effects making it relevant for biomedical research focused on chronic inflammation and cancer therapeutics
Apexbio Technology LLC YO-01027 (Dibenzazepine, DBZ) 209984-56-5 10mM (in 1mL DMSO)
YO-01027 (Dibenzazepine DBZ CAS 209984-56-5) is a potent inhibitor targeting -secretase a multimeric aspartyl protease involved in the proteolytic cleavage of type I integral membrane proteins notably amyloid precursor protein-like (APPL) proteins and Notch receptors YO-01027 interacts with the N-terminal regions of presenilin dose-dependently inhibiting cleavage of APPL and Notch proteins Research indicates that YO-01027 modulates cell differentiation by suppressing Notch signaling pathways influencing cellular transitions and mucin (MUC16) synthesis illustrating its utility in cell biology and therapeutic studies of Notch-related signaling processes