Dimethyl Sulfoxide
Apexbio Technology LLC TIC10 41276-02-2 10mM (in 1mL DMSO)
TIC10 (TRAIL-inducing compound 10) is a small molecule inhibitor with oral bioavailability capable of penetrating the blood-brain barrier It functions primarily by simultaneously inhibiting Akt and ERK pathways resulting in Foxo3a nuclear translocation and transcriptional activation of TRAIL (tumor necrosis factor-related apoptosis-inducing ligand) TRAIL is involved in apoptosis induction in cancer cells often compromised during tumor progression TIC10 triggers the expression of TRAIL independently of p53 status enabling apoptosis in diverse cancer cell types In preclinical xenograft models and orthotopic glioblastoma studies TIC10 has demonstrated TRAIL-mediated antitumor activity supporting its use in cancer biology research and therapeutic investigations
Apexbio Technology LLC SGC-CBP30 1613695-14-9 10mM (in 1mL DMSO)
SGC-CBP30 (CAS 1613695-14-9) is a selective small-molecule inhibitor targeting the bromodomains of CREB-binding protein (CREBBP) and E1A-binding protein p300 (EP300) exhibiting IC50 values of 21 nM and 38 nM respectively Both EP300 and CREBBP function as transcriptional coactivators involved in diverse regulatory processes including cell proliferation differentiation and transcription factor activation Through its inhibitory action SGC-CBP30 is utilized widely in biomedical research to investigate the molecular roles of CREBBP/EP300 as well as in studies examining related signaling pathways in tumor biology and cellular regulation
Apexbio Technology LLC Chlorocresol 10mM (in 1mL DMSO)
B1696 is a small molecule compound utilized in biomedical research primarily due to its modulatory effects on specific cellular signaling pathways Although the explicit molecular target is currently unpublished available evidence indicates that B1696 influences cellular processes implicated in inflammation immune response and cell proliferation Researchers employ this compound to investigate disease mechanisms and signaling networks within in vitro or ex vivo experimental systems contributing valuable information on therapeutic intervention strategies and drug development efforts
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 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 SGI-1776 free base 1025065-69-3 10mM (in 1mL DMSO)
SGI-1776 free base (CAS 1025065-69-3) is an ATP-competitive inhibitor targeting Pim kinases a serine/threonine protein kinase family implicated in regulating cellular survival pathways It selectively inhibits all three isoforms Pim-1 Pim-2 and Pim-3 leading to decreased phosphorylation of downstream substrates involved in cell cycle regulation and apoptosis such as p21Cip1/WAF1 and Bad Cellular studies indicate that SGI-1776 induces G1 cell cycle arrest promotes apoptosis and overcomes chemoresistance mediated by multidrug resistance protein 1 (MDR1) in taxane-resistant prostate cancer cells
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
Apexbio Technology LLC PD184352 (CI-1040) 212631-79-3 10mM (in 1mL DMSO)
PD184352 (CI-1040 CAS 212631-79-3) is a benzhydroxamate derivative that selectively inhibits the MEK1/2 kinases members of the MAP kinase kinase (MAPKK) family It interacts with a hydrophobic pocket adjacent to the Mg-ATP binding region of MEK1/2 triggering conformational shifts that favor the inactive non-phosphorylated state of these enzymes Acting via an ATP- and ERK1/2-independent inhibitory mechanism PD184352 robustly suppresses purified MEK1 enzyme activity (IC50 17 nM) Preclinical research demonstrates efficacy in reducing tumor growth notably in murine xenograft models of colon carcinoma underscoring its utility as a research tool in oncology
Apexbio Technology LLC SCH772984 HCl 942183-80-4 (free base) 10mM (in 1mL DMSO)
SCH772984 HCl is a selective inhibitor targeting extracellular signal-regulated kinases 1 and 2 (ERK1/2) members of the mitogen-activated protein kinase (MAPK) pathway ERK activation is commonly implicated in cancer proliferation particularly in tumors harboring BRAF or RAS mutations SCH772984 HCl binds specifically to ERK1/2 blocking their kinase activity and downstream substrate phosphorylation In cell-based experiments it inhibits phosphorylation of ERK substrates such as p90 ribosomal S6 kinase (RSK) and decreases phosphorylation of ERK1/2 activation-loop residues In vivo SCH772984 HCl reduces tumor growth in xenograft mouse models bearing human melanoma cells with BRAF V600E mutation This compound is widely used in cancer research to study ERK-mediated signaling pathways and models exhibiting resistance to BRAF and MEK inhibitor therapies
Apexbio Technology LLC Pepstatin A 26305-03-3 10mM (in 1mL DMSO)
Pepstatin A is a pentapeptide functioning as an inhibitor targeting aspartic proteases including pepsin renin HIV protease and cathepsin D It inhibits human renin and HIV protease with IC50 values of approximately 15 M and 2 M respectively and shows inhibitory activity toward pepsin and cathepsin D at IC50 values below 5 M and 40 M Mechanistically Pepstatin A acts through binding to the catalytic site of aspartic proteases restricting proteolytic activity In biomedical research it is utilized to study viral protein processing osteoclast differentiation mediated by cathepsins and as a standard tool in enzyme inhibition assays examining aspartic protease function
Apexbio Technology LLC Levetiracetam 102767-28-2 10mM (in 1mL DMSO)
Levetiracetam (CAS 102767-28-2) is an antiepileptic small-molecule agent recognized for its distinct mode of action compared to traditional anticonvulsants It binds selectively to synaptic vesicle glycoprotein 2A (SV2A) a protein involved in the regulation of intracellular calcium dynamics and neurotransmitter release Mechanistically levetiracetam negatively modulates gamma-aminobutyric acid (GABA)- and glycine-gated neuronal currents Importantly levetiracetam does not induce hepatic cytochrome P450 enzymes exhibits negligible plasma protein binding and is predominantly excreted unchanged renally with partial hydrolytic metabolism clinically levetiracetam is utilized widely in research addressing partial and generalized epileptic seizures
Apexbio Technology LLC Fruquintinib(HMPL-013) 1194506-26-7 10mM (in 1mL DMSO)
Fruquintinib (HMPL-013 CAS 1194506-26-7) is a small molecule inhibitor targeting VEGFR family receptor tyrosine kinases (VEGFR1 VEGFR2 and VEGFR3) It demonstrates potent inhibitory activity with reported IC50 values of approximately 33 nM (VEGFR1) 35 nM (VEGFR2) and 0 5 nM (VEGFR3) Kinase selectivity screening indicates limited off-target effects against other kinases such as RET FGFR-1 and c-kit In preclinical tumor xenograft studies (e g gastric cancer BGC-823 model) significant tumor growth suppression ( 80%) was achieved at sustained therapeutic exposure Fruquintinib is currently under clinical investigation for cancer treatment based on its selective VEGFR pathway inhibition
Apexbio Technology LLC Enrofloxacin 93106-60-6 10mM (in 1mL DMSO)
Enrofloxacin a fluoroquinolone antibiotic exerts antibacterial activity by inhibiting bacterial DNA gyrase and topoisomerase IV enzymes essential for DNA replication and transcription This mechanism disrupts the DNA synthesis of pathogenic bacteria resulting in bacteriostatic outcomes In vitro experiments indicate that Enrofloxacin displays antimicrobial activity against Mycoplasma species such as Mycoplasma bovis with a minimum inhibitory concentration (MIC90) around 0 312 g/mL In biomedical research this compound is primarily utilized to establish microbial infection models and to study bacterial resistance mechanisms pharmaceutical efficacy and antibacterial pharmacodynamics
Apexbio Technology LLC Tivozanib (AV-951) 475108-18-0 10mM (in 1mL DMSO)
Tivozanib (AV-951 CAS 475108-18-0) is a quinoline-urea derivative functioning as a potent inhibitor of vascular endothelial growth factor receptors (VEGFR) It primarily targets VEGFR-2 kinase demonstrating significant inhibitory activity in picomolar ranges (IC50 of approximately 160 pM) Additionally Tivozanib displays considerable selectivity causing minimal off-target interaction with c-kit In cellular assays it inhibits PDGFR and c-kit phosphorylation at nanomolar levels Preclinical evaluations revealed antitumor activity across multiple solid tumor xenograft models particularly renal cell carcinoma (RCC) Its mechanism and selectivity profile render it valuable for cancer research clinical investigation and preclinical efficacy assessments
Apexbio Technology LLC Orlistat(Synonyms: Xenical, Alli, tetrahydrolipstatin, THL, Roche Xenical, lipase inhibitor, (-)-tetrahydrolipstatin), 10mM (in 1mL DMSO), CAS: 96829-58-2.
Orlistat (CAS 96829-58-2) also referred to as tetrahydrolipstatin is a synthetic derivative of lipstatin originally isolated from Streptomyces toxytricini This small molecule specifically inhibits gastrointestinal lipases particularly pancreatic lipase impeding enzymatic hydrolysis of dietary triglycerides and consequently decreasing intestinal absorption of fat Due to its targeted lipase inhibition Orlistat is widely studied in obesity-related metabolic research and lipid metabolism investigations providing a valuable experimental tool for evaluating effects of reduced dietary fat uptake and downstream physiological responses