Dimethyl Sulfoxide
Apexbio Technology LLC LY2874455(Synonyms: LY-2874455, LY 2874455, FGFR inhibitor LY2874455, Fibroblast growth factor receptor inhibitor LY2874455), 10mM (in 1mL DMSO), CAS: 1254473-64-7.
LY2874455 (CAS 1254473-64-7) is a small molecule inhibitor targeting fibroblast growth factor receptors (FGFRs) proteins functioning through ligand-induced receptor dimerization and tyrosine kinase activation By blocking FGFR phosphorylation and downstream signaling pathways LY2874455 inhibits proliferation and migration in FGFR-dependent cancer cell models LY2874455 shows inhibition of FGFR phosphorylation in FGFR1- FGFR2- and FGFR3-expressing cancer cell lines and xenografts demonstrating antitumor efficacy across various FGFR-driven tumor types It serves as a valuable tool molecule in oncology research investigating FGFR-mediated cancers
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 GW5074 220904-83-6 10mM (in 1mL DMSO)
GW5074 (CAS 220904-83-6) is a synthetic small molecule inhibitor targeting c-Raf kinase with an IC50 of approximately 9 nM GW5074 displays selectivity for c-Raf showing little or no inhibitory activity against various other kinases including cdk1 cdk2 c-src p38 MAP kinase VEGFR2 c-fms and JNK In neuronal cells GW5074 decreases phosphorylation at serine 259 of c-Raf resulting in c-Raf activation At concentrations below 1 M GW5074 confers neuroprotection by sustaining Akt phosphorylation preventing GSK3 activation and thus reducing apoptosis In vivo GW5074 mitigates neurodegeneration in a 3-nitropropionic acid-induced Huntington s disease model demonstrating promise for neurodegenerative research applications
Apexbio Technology LLC PTC-209 315704-66-6 10mM (in 1mL DMSO)
PTC-209 (CAS 315704-66-6) is a small-molecule inhibitor targeting BMI-1 identified through Gene Expression Modulation by Small molecules (GEMS) technology It acts by suppressing BMI-1 expression at the transcriptional level displaying an IC50 of approximately 0 5 M In HCT116 cells PTC-209 reduces both UTR-mediated and endogenous BMI-1 expression It selectively restricts cell proliferation in certain tumor and stem cell types including U937 HT1080 and human hematopoietic stem cells without affecting viability in cell lines such as HEK293 and HT1080 Thus PTC-209 is primarily utilized in studies exploring cancer stem cell growth and oncogenesis involving BMI-1 and the PRC1 complex
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 Probenecid 57-66-9 10mM (in 1mL DMSO)
Probenecid is an inhibitor targeting organic anion transporters multidrug resistance-associated proteins (MRPs) and pannexin-1 channels showing an IC50 of 150 M for pannexin-1 inhibition MRPs a class of ATP-binding cassette (ABC) transporters mediate efflux of diverse molecules across cellular membranes contributing to drug resistance Probenecid counteracts MRP-mediated drug resistance in multidrug-resistant tumor cell lines enhancing cellular sensitivity to chemotherapeutic agents like daunorubicin and vincristine In animal research Probenecid protects neurons against ischemia/reperfusion-induced injury suppressing inflammation-associated enzyme activity and reducing glial cell activation
Apexbio Technology LLC Batimastat (BB-94)(Synonyms: BB-94, Batimastat, MMP inhibitor BB-94), 10mM (in 1mL DMSO), CAS: 130370-60-4.
Batimastat (BB-94 CAS 130370-60-4) is a synthetic small-molecule inhibitor targeting matrix metalloproteinases (MMPs) Structurally a polypeptide-like analogue of collagen substrates batimastat contains a peptidic backbone and a hydroxamate moiety that binds the catalytic zinc atom of MMPs It inhibits several MMP subtypes markedly including MMP-1 MMP-2 MMP-3 MMP-7 and MMP-9 with reported IC50 values of 3 4 20 6 and 4 nM respectively In preclinical studies batimastat demonstrates inhibitory effects on tumor growth and angiogenesis across various tumor models including ovarian and colon carcinoma xenografts making it relevant for cancer research and therapeutic development
Apexbio Technology LLC Aprepitant 170729-80-3 10mM (in 1mL DMSO)
Aprepitant (MK-0869) is a highly selective antagonist of the neurokinin-1 (NK-1) receptor functioning by competitively inhibiting substance P (SP) an undecapeptide belonging to the tachykinin family from activating NK-1 receptors Its binding affinity for human NK-1 receptors is indicated by a dissociation constant (Kd) of approximately 86 pM In cellular models overexpressing NK-1 receptors including glioma (GAMG) neuroblastoma (SKN-BE2 IC50 19 6 M IMR-32 IC50 27 7 M KELLY IC50 30 4 M) retinoblastoma (Y-79 IC50 23 M WERI-Rb-1 IC50 31 2 M) pancreatic cancer (PA-TU-8902 IC50 27 4 M CAPAN-1 IC50 22 7 M) and colon cancer (SW-403 IC50 30 5 M) aprepitant application has been reported to inhibit tumor cell proliferation in vitro
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 Meropenem 96036-03-2 10mM (in 1mL DMSO)
Meropenem is a broad-spectrum -lactam antibiotic within the carbapenem subclass characterized by bactericidal activity against both gram-positive and gram-negative organisms It primarily acts by binding to penicillin-binding proteins (PBPs) mainly PBP2 of Escherichia coli and Pseudomonas aeruginosa and PBP1 of Staphylococcus aureus thus disrupting cell wall synthesis and bacterial growth In vitro studies indicate Meropenem inhibition is effective at MIC 4 mg/L (susceptible strains) intermediate at 8 mg/L and resistant at 16 mg/L Meropenem demonstrates greater potency against gram-negative bacteria compared to Imipenem with typical IC50 values around 0 25 mg/L for anaerobic strains It is typically used in microbiological research to investigate antibiotic susceptibility bacterial resistance mechanisms and interactions with drug metabolism
Apexbio Technology LLC Meptazinol HCl 59263-76-2 10mM (in 1mL DMSO)
Meptazinol HCl also chemically known as WY-22811 hydrochloride is a centrally acting analgesic agent characterized as a partial agonist at the 1 opioid receptor Structurally it belongs to the synthetic opioid family and interacts selectively with opioid receptors in the central nervous system to modulate pain transmission Its partial agonist properties allow for analgesic activity with generally reduced risk of respiratory depression compared to full opioid agonists making it a useful compound in pharmacological studies examining opioid receptor activation modulation and analgesic effects In biomedical research settings Meptazinol HCl is commonly employed to investigate pain management mechanisms opioid receptor signaling pathways receptor selectivity profiles and analgesia-related side effect mitigation
Apexbio Technology LLC KPT-185 1333151-73-7 10mM (in 1mL DMSO)
KPT-185 (CAS 1333151-73-7) is an irreversible selective inhibitor of chromosome region maintenance 1 (CRM1) a nuclear export receptor essential for nuclear-cytoplasmic transport KPT-185 binds covalently at Cys528 of CRM1 thereby inhibiting CRM1-mediated nuclear export of tumor suppressor proteins Studies demonstrate that KPT-185 impairs proliferation and colony formation in acute myeloid leukemia (AML) cell lines exhibiting IC50 values ranging from 100 500 nM inducing G1 cell cycle arrest apoptosis and differentiation of AML blasts Additionally KPT-185 reduces growth and promotes apoptosis in pancreatic cancer models (Colo-357 HPAC BxPC-3) highlighting its potential in cancer research
Cayman Chemical PerphenazIn SulfoxIde 10mg
An active metabolite of perphenazine; selectively binds to dopamine D2 and α1-ARs over α2-ARs (Kis= 5.9, 24, and 683 nM, respectively) in rat brain; increases thrombin-induced increases in phosphatidylinositol levels in isolated human platelets at 5 µM
Apexbio Technology LLC BIBR 1532 321674-73-1 10mM (in 1mL DMSO)
BIBR 1532 (CAS 321674-73-1) is a selective non-nucleosidic inhibitor of telomerase exhibiting an IC50 of approximately 93 nM It targets human telomerase reverse transcriptase (hTERT) reducing enzymatic activity and causing telomere shortening Mechanistically BIBR 1532 suppresses cancer cell proliferation and induces apoptosis by modulating c-Myc and hTERT transcription elevating pro-apoptotic signaling through p73 Bax/Bcl-2 ratio and caspase-3 activation It has demonstrated inhibitory effects on proliferation and survival in several leukemia cell lines including pre-B acute lymphoblastic leukemia and acute promyelocytic leukemia (NB4) highlighting its utility in oncology research