Dimethyl Sulfoxide
Apexbio Technology LLC AEBSF.HCl 30827-99-7 10mM (in 1mL DMSO)
AEBSF HCl is an irreversible serine protease inhibitor that covalently binds and inhibits several proteases including trypsin chymotrypsin plasmin and thrombin It has been applied in cellular research to study amyloid-beta (A ) production mechanisms In APP695 (K695sw)-transfected K293 cells AEBSF dose-dependently reduces A formation with an IC50 around 1 mM while in wild-type APP695-transfected HS695 and SKN695 cells it shows inhibitory effects with an IC50 of approximately 300 M Besides suppressing -cleavage AEBSF promotes -cleavage of APP In macrophage-mediated leukemic cell lysis assays incubation with AEBSF at 150 M for 6 hours achieves near-maximal protease inhibition thus impeding cell lysis
Apexbio Technology LLC PCI-32765 (Ibrutinib) 936563-96-1 10mM (in 1mL DMSO)
PCI-32765 (Ibrutinib) is a small-molecule inhibitor targeting Bruton s tyrosine kinase (BTK) a cytoplasmic kinase integral to B-cell receptor (BCR) signaling By covalently binding to BTK active sites PCI-32765 disrupts downstream signaling cascades essential for B-cell maturation and activation Dysfunction or inhibition of BTK correlates with impaired B-cell development and reduction in autoantibody production PCI-32765 is commonly utilized in biomedical research to explore BTK-dependent signaling pathways elucidate molecular mechanisms underlying B-cell mediated disorders and examine therapeutic potential in B-cell malignancies and autoimmune models
Apexbio Technology LLC Foretinib (GSK1363089) 849217-64-7 10mM (in 1mL DMSO)
Foretinib (GSK1363089 CAS 849217-64-7) is a small molecule inhibitor targeting receptor tyrosine kinases involved in angiogenesis and tumor progression notably receptors for vascular endothelial growth factor (VEGF) and hepatocyte growth factor (HGF) Foretinib inhibits tyrosine kinase activity of Met Ron KDR Flt-1 Flt-4 KIT Flt-3 Tie-2 and PDGFR / exhibiting IC50 values ranging from 0 4 to 9 6 nmol/L In cell-based assays foretinib reduces MET phosphorylation in mouse B16F10 melanoma and human PC-3 prostate cells (IC50 21 23 nmol/L) inhibits HGF-induced cell migration invasion and suppresses proliferation in B16F10 A549 and HT29 tumor cell lines Foretinib is utilized in preclinical cancer research targeting angiogenesis invasion and metastasis pathways
Apexbio Technology LLC Ifosfamide 3778-73-2 10mM (in 1mL DMSO)
Ifosfamide (CAS 3778-73-2) is an oxazaphosphorine-type alkylating agent structurally analogous to cyclophosphamide As a prodrug it undergoes hepatic activation via cytochrome P450-mediated hydroxylation generating reactive metabolites that form crosslinks within the DNA double strands This alkylation induces DNA damage subsequently inhibiting cell proliferation and promoting apoptosis in rapidly dividing cells Due to these cytostatic and cytotoxic properties Ifosfamide is widely evaluated in oncology research contexts particularly for various hematological malignancies and solid tumors
Apexbio Technology LLC Entrectinib 1108743-60-7 10mM (in 1mL DMSO)
Entrectinib (CAS 1108743-60-7) is an orally bioavailable small molecule inhibitor targeting receptor tyrosine kinases specifically anaplastic lymphoma kinase (ALK) Dysregulated ALK activity is implicated in the progression of several cancers influencing cell proliferation and survival Entrectinib has demonstrated selective inhibition of ALK-induced tumor growth in cell-based assays Additionally in xenograft models of ALK-positive non-small cell lung cancer (NSCLC) Entrectinib crosses the blood-brain barrier suppressing intracranial tumor growth and improving survival outcomes in a dose-dependent manner Currently Entrectinib is undergoing Phase I/II clinical evaluation for treating ALK-expressing solid cancers
Apexbio Technology LLC Regadenoson 313348-27-5 10mM (in 1mL DMSO)
Regadenoson is a selective low-affinity agonist targeting the adenosine A2A receptor a G protein-coupled receptor involved in vasodilation mechanisms By activating A2A receptors regadenoson induces coronary vasodilation through increased coronary blood flow (CBF) Prior in vitro binding experiments show that regadenoson displays high specificity towards the A2A subtype without significant interaction with adenosine receptor subtypes A1 A2B or A3 In animal models intravenous regadenoson administration elevates coronary artery blood flow transiently in a dose-dependent manner with minimal systemic hemodynamic changes Clinically regadenoson induces rapid increases in human coronary blood flow velocity making it suitable for diagnostic research applications related to coronary function
Apexbio Technology LLC Pirfenidone 53179-13-8 10mM (in 1mL DMSO)
Pirfenidone (CAS 53179-13-8) is a small molecule antifibrotic agent exhibiting anti-inflammatory properties Mechanistically pirfenidone reduces levels of pro-inflammatory mediators notably TNF- via translational regulation independent of MAPK pathway activation It suppresses TGF- -mediated signaling and extracellular matrix protein production contributing to decreased fibrotic responses in cellular and animal models In vivo pirfenidone administration mitigates fibrosis and inflammatory cytokine expression in tissues such as lung liver and kidney Clinically pirfenidone is investigated primarily for idiopathic pulmonary fibrosis demonstrating reductions in fibrosis progression and improved functional parameters
Apexbio Technology LLC XL335 629664-81-9 10mM (in 1mL DMSO)
XL335 (CAS 629664-81-9) is a selective orally bioavailable agonist of the farnesoid X receptor (FXR) displaying an EC50 of approximately 4 nM In Hep3B liver cancer cells XL335 activation of FXR reduces interleukin-6-induced C-reactive protein (CRP) expression at both mRNA and protein levels In vivo studies indicate that XL335 diminishes lipopolysaccharide (LPS)-stimulated inflammatory responses and fructose-induced hepatic inflammation by suppressing acute-phase proteins (e g SAP SAA3) and adipose differentiation-related protein (ADRP) Thus XL335 serves as a valuable tool for investigating FXR-mediated pathways involved in liver inflammation and metabolic disorders
Apexbio Technology LLC LDC000067 1073485-20-7 10mM (in 1mL DMSO)
LDC000067 (CAS 1073485-20-7) also known as LDC067 is a selective inhibitor of cyclin-dependent kinase 9 (CDK9) CDK9 partners with cyclin T to form positive transcription elongation factor b (P-TEFb) which regulates RNA polymerase II by phosphorylating its C-terminal domain thus controlling gene transcription elongation LDC000067 inhibits CDK9 activity with an IC50 of approximately 44 10 nM Compared to other CDKs LDC000067 demonstrates notable selectivity showing 55-fold higher specificity against CDK2 and over 230-fold greater selectivity relative to CDK6 and CDK7 By selectively blocking CDK9 this ATP-competitive inhibitor reduces cellular transcription of short-lived mRNAs associated with proliferation and apoptosis such as MYC and MCL1 Thus LDC000067 is applicable in transcription regulation and cancer-related pathway studies
Apexbio Technology LLC Q-VD-OPh 1135695-98-5 10mM (in 1mL DMSO)
Q-VD-OPh is a pan-caspase inhibitor targeting caspases including 1 3 8 and 9 with IC50 values ranging from approximately 25 to 400 nM By blocking multiple caspase-mediated apoptotic pathways including caspase-9/3 caspase-8/10 and caspase-12 pathways Q-VD-OPh prevents apoptotic cell death induced by agents such as actinomycin D In research contexts this inhibitor serves as a tool to investigate apoptosis mechanisms across diverse cell types and species including human mouse and rat It is also used to enhance cell viability upon thawing from cryopreservation under standard cryoprotectant conditions
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 JIB-04 199596-05-9 10mM (in 1mL DMSO)
JIB-04 (CAS 199596-05-9) is a selective small-molecule inhibitor targeting Jumonji histone demethylases specifically suppressing enzymes including JARID1A JMJD2 family members (JMJD2A-E) and JMJD3 Structurally categorized as a pyridine hydrazone derivative JIB-04 inhibits demethylase activity independently of competitive binding with -ketoglutarate In vitro assays revealed IC50 values ranging from 230 nM to 1100 nM across various Jumonji enzymes Additionally JIB-04 demonstrates preferential inhibition of cancer cell proliferation versus normal cells notably in lung and prostate cancer cell lines and effectively reduces tumor growth in mouse xenograft models highlighting its relevance for cancer research
Apexbio Technology LLC (+)-Apogossypol 66389-74-0 10mM (in 1mL DMSO)
( )-Apogossypol (CAS 66389-74-0) is a pan-BCL-2 family protein antagonist exhibiting activity against anti-apoptotic proteins including Bcl-2 Bcl-xL and Mcl-1 By binding directly to these targets it inhibits their anti-apoptotic functions thereby promoting apoptosis Reported EC50 values for binding to Mcl-1 Bcl-2 and Bcl-xL are 2 6 M 2 8 M and 3 69 M respectively This compound is utilized in research focused on apoptosis signaling pathways and cancer drug screening involving the BCL-2 protein family
Apexbio Technology LLC (-)-Huperzine A 102518-79-6 10mM (in 1mL DMSO)
(-)-Huperzine A (CAS 102518-79-6) known as HupA is an alkaloid compound serving as an inhibitor of acetylcholinesterase (AChE) with an IC50 value of 82 nmol/L By suppressing AChE activity HupA reduces the enzymatic breakdown of neurotransmitter acetylcholine potentially alleviating symptoms associated with Alzheimer s disease Furthermore HupA acts as a non-competitive antagonist at NMDA receptors attenuating NMDA-induced currents in rat hippocampal neurons Studies demonstrate sustained AChE inhibition lasting up to 360 minutes following systemic administration Consequently HupA has significant applications in neuropharmacological research targeting cognitive disorders and neuroprotection
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