Dimethyl Sulfoxide
Apexbio Technology LLC Trichostatin A (TSA) 58880-19-6 10mM (in 1mL DMSO)
Trichostatin A (TSA CAS 58880-19-6) is a histone deacetylase (HDAC) inhibitor and antifungal antibiotic isolated from microbial sources TSA acts by reversibly inhibiting HDAC enzymes in a noncompetitive manner leading to increased acetylation of histones particularly histone H4 In mammalian cell cultures TSA treatment results in G1 and G2 phase arrest induction of differentiation and reversion of transformed cellular phenotypes In human breast cancer cell lines TSA inhibits proliferation (IC50 124 4 120 4 nM) and induces hyperacetylation of histone proteins highlighting its utility as a tool compound for investigating epigenetic regulation and oncology-related mechanisms
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 Acetaminophen 103-90-2 10mM (in 1mL DMSO)
Acetaminophen (paracetamol) is a cyclooxygenase-2 (COX-2) inhibitor widely employed in biomedical studies for investigating analgesic and antipyretic mechanisms Its inhibition of COX-2 enzyme activity occurs with an IC50 of approximately 25 8 M Experimental use includes inducing cellular hepatotoxicity models where acetaminophen exposure triggers glutathione depletion impaired glutathione peroxidase activity and ferroptosis-mediated cell death This makes acetaminophen useful in examining oxidative stress hepatic cell injury and associated cellular response mechanisms in vitro and in animal studies Additionally acetaminophen-mediated toxicity is applicable in screening protective agents or evaluating ferroptosis inhibitors in pharmacological research
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 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 E 64d 88321-09-9 10mM (in 1mL DMSO)
E-64d is a membrane-permeable cysteine protease inhibitor derived from E-64c acting via covalent modification of the proteolytic active site thiol group It demonstrates inhibitory activity primarily against calpain a calcium-dependent cysteine protease involved in diverse cellular processes E-64d readily penetrates intact cells allowing researchers to inhibit intracellular protease activity without disruption In intact platelet models short incubation with E-64d results in persistent suppression of calpain activity even after removal of extracellular inhibitor by washing Experimentally it is commonly utilized to investigate calpain s role in physiological and pathological events particularly in platelets and cellular apoptosis pathways The typical reported IC50 value of E-64d against calpain is approximately 0 5 1 M
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 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 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 JNK-IN-8 1410880-22-6 10mM (in 1mL DMSO)
JNK-IN-8 (CAS 1410880-22-6) is a potent and specific inhibitor of c-Jun N-terminal kinase (JNK) isoforms JNK1 JNK2 and JNK3 It functions by forming a covalent bond with a conserved cysteine residue in JNKs inducing conformational alteration in the kinase activation loop consequently impairing substrate binding Its IC50 values for JNK1 JNK2 and JNK3 are 4 67 nM 18 7 nM and 0 98 nM respectively In cellular assays JNK-IN-8 prevention of c-Jun phosphorylation demonstrates robust selectivity towards the JNK signaling pathway thus making it valuable as a research tool in studying stress-related cellular responses and apoptosis
Apexbio Technology LLC MK 0893 870823-12-4 10mM (in 1mL DMSO)
MK 0893 is a small molecule antagonist targeting both the glucagon receptor (GCGR) and insulin-like growth factor-1 receptor (IGF-1R) It competitively and reversibly inhibits glucagon binding to GCGR subsequently reducing receptor-mediated cAMP production In cell-based assays utilizing CHO cells expressing human GCGR MK 0893 showed nanomolar-level inhibitory potency with a receptor binding IC50 around 6 6 nM and a cellular cAMP inhibition IC50 near 15 7 nM Additionally MK 0893 exhibits potent inhibitory activity on IGF-1R demonstrated in IGF-1-driven mouse xenograft tumor models Therefore MK 0893 serves as a relevant pharmacological tool in research related to type 2 diabetes and IGF-1R-mediated oncogenic signaling pathways
Apexbio Technology LLC CP-724714 537705-08-1 10mM (in 1mL DMSO)
CP-724714 (CAS 537705-08-1) is a small molecule inhibitor selectively targeting erbB2 (Her2) and EGFR kinases with notable potency against erbB2 kinase (IC50 10 3 nM) and considerably lower activity toward EGFR kinase (IC50 6 400 2 100 nM) In cellular assays CP-724714 induces G1 cell-cycle arrest and decreases erbB2 phosphorylation in Her2-overexpressing BT-474 breast cancer cells In animal xenograft models (BT-474 MDA-MB-453) it reduces erbB2 receptor phosphorylation and downstream signaling resulting in tumor growth inhibition and apoptosis induction CP-724714 advanced into phase I clinical trials for Her2-driven breast cancer research
Apexbio Technology LLC TG100-115 677297-51-7 10mM (in 1mL DMSO)
TG100-115 (CAS 677297-51-7) is a selective inhibitor targeting phosphoinositide 3-kinase isoforms PI3K and PI3K with IC50 values of 83 nM and 235 nM respectively exhibiting negligible inhibition towards PI3K and PI3K Research in murine models demonstrates that treatment with TG100-115 significantly reduces eosinophil accumulation bronchoalveolar IL-13 cytokine levels mucus deposition and leukocyte infiltration associated with allergic asthma decreasing airway hyperresponsiveness by approximately 50% Moreover this compound attenuates neutrophil infiltration and TNF induction following exposure to cigarette smoke and LPS suggesting its utility as an investigational tool for asthma and inflammatory pulmonary diseases
Apexbio Technology LLC GDC-0449 (Vismodegib) 879085-55-9 10mM (in 1mL DMSO)
GDC-0449 (Vismodegib CAS 879085-55-9) is a small molecule that selectively inhibits the Hedgehog (Hh) signaling pathway by binding to the Smoothened (SMO) receptor thus preventing downstream activation of Hh target genes implicated in cellular proliferation and differentiation This compound emerged from screening small-molecule libraries followed by medicinal chemistry optimization Preclinical evaluation demonstrated antitumor activity in murine models of medulloblastoma and xenograft models derived from human colon and pancreatic cancers Currently GDC-0449 is under investigation for locally advanced and metastatic solid tumors
Apexbio Technology LLC Epirubicin HCl 56390-09-1 10mM (in 1mL DMSO)
Epirubicin HCl is an anthracycline antibiotic with antitumor activity targeting DNA topoisomerase II (TOPII) It functions by stabilizing TOPII-DNA cleavable complexes resulting in increased DNA double-strand breaks subsequent activation of DNA damage responses and initiation of apoptosis pathways Consequently epirubicin is frequently utilized in anticancer research particularly against osteosarcoma cells Studies demonstrate epirubicin induces apoptosis in osteosarcoma models yet it can also activate resistance pathways such as NF- B affecting therapeutic efficacy The reported IC50 values of epirubicin in osteosarcoma cell lines typically range between approximately 0 1 to 2 M based on experimental conditions This compound is thus actively employed in oncology research exploring DNA-damaging agents or combination therapy strategies in cell-based assays and animal models