Dimethyl Sulfoxide
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
Medchemexpress LLC XMU-MP-9 ,10 mM 1 mL in DMSO Solution
XMU-MP-9 is a bifunctional compound that binds to the C2 domain of Nedd4-1 and the allosteric site of K-Ras. XMU-MP-9 enhances the interaction between Nedd4-1 and K-Ras, induces conformational changes in the Nedd4-1/K-Ras complex, promotes the ubiquitination and degradation of multiple K-Ras mutants, and inhibits the proliferation of cells carrying K-Ras mutants. XMU-MP-9 can be used in cancer research.
Apexbio Technology LLC Amantadine HCl 665-66-7 10mM (in 1mL DMSO)
Amantadine Hydrochloride a dopamine receptor agonist is primarily employed as a research tool in neuroscience and antiviral studies It exerts its antiparkinsonian effects by promoting dopamine release and inhibiting dopamine reuptake consequently enhancing dopaminergic neurotransmission As an antiviral agent amantadine hydrochloride inhibits influenza A virus replication through blockade of the viral matrix protein M2 ion channel In cell-based assays amantadine hydrochloride demonstrates inhibitory activity against influenza A viruses with reported IC50 values typically ranging between 0 3 to 1 5 M depending on assay conditions and viral strains Researchers commonly utilize this compound to investigate neurological pathways associated with Parkinson s disease viral infection mechanisms and drug resistance phenomena
Apexbio Technology LLC HOAt 39968-33-7 10mM (in 1mL DMSO)
HOAt (1-Hydroxy-7-azabenzotriazole) is a peptide coupling reagent frequently employed in peptide synthesis for the activation of carboxylic groups Structurally HOAt serves as an activating additive that forms reactive intermediates facilitating amide bond formation while mitigating side reactions such as racemization As reported in experimental peptide coupling studies combining HOAt with diisopropylcarbodiimide (DIC) promotes coupling reactions with improved retention of stereochemical integrity relative to traditional coupling systems utilizing other benzotriazole derivatives HOAt is thus commonly used both in segment coupling and stepwise solid-phase peptide assembly methodologies aimed at synthesizing peptides requiring minimal epimerization
Apexbio Technology LLC GSK-923295 1088965-37-0 10mM (in 1mL DMSO)
GSK-923295 (CAS 1088965-37-0) is a highly potent inhibitor targeting the centromere-associated protein E (CENP-E) a kinesin motor protein essential for proper chromosome alignment and progression from metaphase to anaphase during cell division By blocking microtubule-stimulated ATPase activity of CENP-E GSK-923295 stabilizes an ATP-bound intermediate resulting in significantly reduced enzymatic function (IC50 3 2 nM) In cellular models GSK-923295 induces mitotic arrest with morphological changes similar to CENP-E knockdown In mouse xenograft models using Colo205 colon carcinoma cells administration of GSK-923295 leads to tumor growth inhibition and increased apoptosis supporting its utility in cancer research
Apexbio Technology LLC CGP 57380 522629-08-9 10mM (in 1mL DMSO)
CGP 57380 (CAS 522629-08-9) is a specific and selective inhibitor targeting the serine/threonine kinase MNK1 an enzyme implicated in translation regulation via phosphorylation of the eukaryotic initiation factor 4E (eIF4E) It inhibits MNK1 activity in vitro with an IC50 of approximately 2 2 M CGP 57380 suppresses stimulus-induced phosphorylation of eIF4E in various cellular contexts including 293 cells vascular smooth muscle cells and macrophages reducing translation of mRNAs encoding proinflammatory mediators such as TNF- IL-6 and monocyte chemoattractant protein-1 (MCP-1) Hence CGP 57380 is valuable for investigating MNK1-mediated translational control in inflammation and cell signaling
Apexbio Technology LLC XL019 945755-56-6 10mM (in 1mL DMSO)
XL019 (CAS 945755-56-6) is a selective inhibitor targeting Janus kinase 2 (JAK2) with an IC50 of 2 2 nM JAK2 regulates signaling pathways controlling erythroid granulocytic and megakaryocytic lineage differentiation via cytokine and hematopoietic growth factor receptors including erythropoietin and thrombopoietin receptors XL019 demonstrates high selectivity for JAK2 over related kinases (e g JAK1 TYK2) In mouse models bearing HEL 92 1 7 xenografts oral administration of XL019 significantly reduced tumor growth XL019 is evaluated clinically as a candidate for treating primary myelofibrosis and secondary myelofibrosis associated with polycythemia vera or essential thrombocythemia
Apexbio Technology LLC LY2157299(Synonyms: Galunisertib, LY-2157299, LY2157299 monohydrate, LY2157299 hydrate, LY2157299 free base), 10mM (in 1mL DMSO), CAS: 700874-72-2.
LY2157299 (CAS 700874-72-2) is a small-molecule antagonist that selectively targets the transforming growth factor-beta type I receptor (T RI) By blocking signaling through T RI it prevents phosphorylation of downstream effectors Smad2 and Smad3 thereby interfering with the TGF- signaling pathway Preclinical studies indicate LY2157299 inhibits 1-integrin activation reduces tumor cell invasion lowers connective tissue growth factor (CTGF) production and suppresses angiogenesis Currently in phase II clinical trials LY2157299 is being investigated primarily for therapeutic potential against hepatocellular carcinoma and glioblastoma
Apexbio Technology LLC Rimonabant 168273-06-1 10mM (in 1mL DMSO)
Rimonabant (SR141716) is a selective antagonist targeting the cannabinoid type 1 (CB1) receptor It exhibits affinity for CB1 receptors with a Ki of approximately 1 8 nM contrasting with a lower affinity for CB2 receptors (Ki 514 nM) Through blocking CB1 receptor signaling this compound is primarily utilized experimentally to investigate behaviors associated with appetite control energy balance and substance consumption Studies using animal models demonstrate that administration of Rimonabant reduces intake of palatable foods and beverages as well as sucrose and alcohol consumption highlighting its relevance in obesity feeding behavior and addiction-related research contexts
Apexbio Technology LLC EMD638683 1181770-72-8 10mM (in 1mL DMSO)
EMD638683 (CAS 1181770-72-8) is a selective inhibitor of serum- and glucocorticoid-inducible kinases (SGKs) including isoforms SGK1 SGK2 and SGK3 SGK1 regulates key cellular processes such as ion transport survival proliferation and responses to steroid hormones EMD638683 shows inhibitory activity against SGK1 SGK2 and SGK3 (IC50 3 M) significantly reducing SGK-dependent phosphorylation of NDRG1 in vitro It demonstrates limited off-target interactions inhibiting only MSK1 and PRK2 at 1 M while sparing numerous other kinases In cell models EMD638683 influences mitochondrial polarization and caspase activity exhibiting antitumor effects in colorectal tumor cells and antihypertensive activity in vivo
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 Tadalafil 171596-29-5 10mM (in 1mL DMSO)
Tadalafil (CAS 171596-29-5) also known as IC351 is a selective inhibitor of phosphodiesterase type 5 (PDE5) a primary phosphodiesterase isoenzyme responsible for hydrolyzing cyclic guanosine monophosphate (cGMP) in pulmonary vasculature By competitively and reversibly inhibiting PDE5 tadalafil elevates intracellular cGMP levels thereby inducing vasodilation and attenuating pathological pulmonary arterial constriction Due to high selectivity tadalafil shows minimal inhibition of other PDE isoforms such as PDE1 PDE4 PDE6 PDE7 PDE8 PDE9 and PDE10 It is commonly studied in pulmonary arterial hypertension research and utilized clinically for erectile dysfunction
Apexbio Technology LLC GW3965 HCl 405911-17-3 10mM (in 1mL DMSO)
GW3965 HCl is a selective non-steroidal agonist targeting liver X receptors (LXR and LXR ) nuclear transcription factors involved in cholesterol and lipid metabolism Activation of LXRs modulates cholesterol homeostasis by enhancing cholesterol efflux from macrophages stimulating hepatic bile acid synthesis and reducing intestinal cholesterol absorption GW3965 recruits steroid receptor coactivator-1 (SRC-1) to human LXRR in vitro and functions as a full agonist on cellular assays for both LXR and LXR receptors In animal studies oral administration elevated plasma HDL cholesterol levels and increased expression of the cholesterol transporter ABCA1 in macrophages GW3965 is useful in research investigating cholesterol metabolism atherosclerosis and vascular responses mediated by Angiotensin II signaling