Dimethyl Sulfoxide
Apexbio Technology LLC UNC1999 10MM IN 1ML DMSO
UNC1999 (CAS 1431612-23-5) is a small molecule inhibitor targeting EZH2 and EZH1 enzymes responsible for methylating lysine 27 on histone H3 (H3K27me3) a modification associated with transcriptional suppression It inhibits EZH2 and EZH1 with IC50 values of 2 nM and 45 nM respectively binding at the enzyme s SAM cofactor binding site but not competing with histone substrate UNC1999 reduces cellular H3K27me3 levels (IC50 124 nM) and inhibits proliferation of DLBCL cells harboring EZH2 Y641N mutation (EC50 633 nM) It exhibits oral bioavailability in mouse studies supporting its utility as a research probe for investigating EZH-mediated epigenetic regulation
Apexbio Technology LLC SITAXENTAN SODIUM 1ML DMSO
Sitaxentan sodium (CAS 210421-74-2) is a small molecule compound functioning as an orally bioavailable and highly selective antagonist for endothelin receptor subtype A (ETA) By specifically inhibiting ETA receptor signaling sitaxentan sodium interferes with endothelin-1 mediated vasoconstriction and cellular proliferation pathways In biomedical research contexts it serves as a valuable tool for investigating endothelin-related physiological and pathological processes with particular relevance to studies on vascular disorders and pulmonary arterial hypertension
Apexbio Technology LLC ANIDULAFUNGIN 10MM IN 1ML DMSO
Anidulafungin (CAS 166663-25-8) also known as LY-303366 is a semisynthetic derivative of echinocandin B exhibiting antifungal activity It acts by inhibiting fungal cell wall synthesis through interference with the enzyme -(1 3)-D-glucan synthase In vitro analyses demonstrate that Anidulafungin inhibits various Candida species including C albicans C glabrata C tropicalis and C parapsilosis (MIC90 0 08 0 32 0 32 5 12 g/ml respectively) as well as Aspergillus species (MIC90 0 02 g/ml) Lack of significant efficacy was shown against Cryptococcus neoformans and Blastomyces dermatitidis This compound is useful for research exploring antifungal resistance mechanisms and therapeutics
Apexbio Technology LLC ROSIGLITAZONE 10MM IN 1ML DMSO
Rosiglitazone (CAS 122320-73-4) is a synthetic thiazolidinedione (TZD) that functions as an agonist of peroxisome proliferator-activated receptor gamma (PPAR ) a nuclear receptor highly expressed in adipose tissues Upon ligand binding PPAR forms heterodimers with retinoid X receptors promoting transcriptional activation of genes regulating adipogenesis glucose uptake lipid metabolism and insulin sensitivity Through modulating fatty acid storage in adipose tissue and secretion of adipokines rosiglitazone significantly enhances insulin sensitivity making it extensively utilized in metabolic and diabetes research particularly type II diabetes studies
Apexbio Technology LLC MESORIDAZINE 10MM IN 1ML DMSO
Mesoridazine (CAS 5588-33-0) is a dopaminergic antagonist primarily targeting dopamine D2 receptors (K d 19 nM) As an active metabolite of the atypical antipsychotic thioridazine mesoridazine demonstrates marked inhibitory effects on both pre- and postsynaptic dopamine receptors impacting dopamine and acetylcholine neurotransmission Furthermore mesoridazine engages histamine H1 (K d 1 8 nM) muscarinic acetylcholine (K d 69 nM) 1-adrenergic (K d 2 nM) and 2-adrenergic (K d 1600 nM) receptors Its receptor profile makes mesoridazine valuable for neuroscience research into antipsychotic mechanisms and neurotransmitter regulation
Apexbio Technology LLC SCRIPTAID 10MM IN 1ML DMSO
Scriptaid (CAS 287383-59-9) is a small-molecule histone deacetylase (HDAC) inhibitor originally identified through high-throughput transcriptional screening It specifically targets class I HDAC isoforms inhibiting HDAC1/HDAC3 and HDAC8 with IC50 values of approximately 0 6 M and 1 M respectively Structurally related to other hydroxamic acid-containing HDAC inhibitors such as TSA Scriptaid consists of a hydroxamic acid moiety a connecting linker and an aromatic cap group In glioblastoma (GBM) research Scriptaid shows promise by inducing apoptosis in glioma cells highlighting its potential utility for oncology-focused investigations
Apexbio Technology LLC GW9662 10MM IN 1ML DMSO
GW9662 (CAS 22978-25-2) is an antagonist of peroxisome proliferator-activated receptor gamma (PPAR ) a nuclear receptor involved in various biological processes including tumor growth and inflammation GW9662 irreversibly blocks PPAR activity by covalently modifying cysteine residues at its ligand-binding site (IC50 3 3 M) In cellular assays GW9662 inhibits proliferation of breast cancer cell lines (MCF7 MDA-MB-231 MDA-MB-468 IC50 20 30 M) Additionally GW9662 reverses the protective impact of lipopolysaccharide on kidney ischemia/reperfusion injury demonstrating its utility for studying PPAR -mediated pathways in oncology and inflammation models
Apexbio Technology LLC LY2874455 10MM IN 1ML DMSO
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 LY2157299 10MM IN 1ML DMSO
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 CANAGLIFLOZIN 10MM IN 1ML DMSO
Canagliflozin (CAS 842133-18-0) is a selective inhibitor of sodium-glucose cotransporter 2 (SGLT2) a transporter responsible for renal glucose reabsorption By inhibiting SGLT2 activity Canagliflozin decreases renal glucose reabsorption resulting in increased urinary glucose excretion In CHO cells expressing human rat or mouse SGLT2 Canagliflozin potently inhibits sodium-dependent glucose uptake with IC50 values of 4 4 3 7 and 2 0 nM respectively Animal studies using db/db mice and Zucker diabetic fatty (ZDF) rats demonstrate dose-dependent reductions in blood glucose as well as decreased respiratory exchange ratio and body weight Canagliflozin is suitable for in vivo research through oral administration
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 Efavirenz 154598-52-4 10mM (in 1mL DMSO)
Efavirenz is a non-nucleoside reverse transcriptase inhibitor targeting human immunodeficiency virus type-1 (HIV-1) reverse transcriptase (RT) It functions by binding specifically to an allosteric site of HIV-1 RT thereby inhibiting viral RNA-dependent DNA polymerase activity essential for HIV replication Efavirenz exhibits inhibitory activity against wild-type HIV-1 RT with reported IC95 values ranging from approximately 1 5 to 3 nM and retains inhibitory potency against several known NNRTI-resistant RT variants Due to its molecular mechanism and specificity Efavirenz is frequently utilized in antiviral studies particularly HIV research investigating RT inhibition and HIV resistance mechanisms
Apexbio Technology LLC c-Myc tag Peptide 2918768-02-0 10mM (in 1mL DMSO)
c-Myc tag peptide is a synthetic peptide with the amino acid sequence EQKLISEEDL corresponding to residues 410-419 at the C-terminal region of human c-Myc protein It serves as an epitope tag for recombinant protein expression enabling specific recognition and purification of fusion proteins using anti-c-Myc antibodies In immunoassays the peptide competitively binds to anti-c-Myc antibodies confirming antibody-antigen binding specificity and facilitating analysis of fusion proteins in Western blotting immunoprecipitation and immunofluorescence experiments c-Myc itself encodes a transcription factor regulating cellular processes such as proliferation growth apoptosis differentiation and stem-cell renewal pathways and is frequently overexpressed in cancers
Apexbio Technology LLC GW441756 504433-23-2 10mM (in 1mL DMSO)
GW441756 (CAS 504433-23-2) is a small-molecule inhibitor targeting TrkA kinase and LRRK2 It inhibits TrkA kinase activity with an IC50 of 320 nM potentially modulating downstream signaling involved in cellular proliferation differentiation and apoptosis Selectivity studies indicated limited inhibitory effects on other kinases such as cRaf1 and CDK2 with respective IC50 values above 12 M and 7 M GW441756 induced dose-dependent anti-proliferative and pro-apoptotic effects in the human sarcoma cell line HTB114 It also inhibited LRRK2-mediated phosphorylation at Ser935 (IC50 2 2 M) without significant cytotoxicity (IC50 20 M) GW441756 serves as a research tool in oncology and neurobiology
Apexbio Technology LLC Stattic 19983-44-9 10mM (in 1mL DMSO)
Stattic (CAS 19983-44-9) is a small-molecule inhibitor specifically targeting signal transducer and activator of transcription 3 (STAT3) It suppresses STAT3 activation by blocking its dimerization nuclear translocation and subsequent transcriptional activity In vitro studies demonstrate Stattic inhibits proliferation in multiple head and neck squamous cell carcinoma (HNSCC) cell lines including UM-SCC-17B OSC-19 Cal33 and UM-SCC-22B with reported IC50 values ranging from approximately 2 3 to 3 5 M Additionally Stattic downregulates STAT3-mediated hypoxia-inducible factor-1 (HIF-1) expression resulting in enhanced radiosensitivity in HNSCC cells and shows activity in mouse xenograft tumor models Therefore Stattic serves as a research tool for investigating STAT3-associated signaling pathways and cancer biology