Dimethyl Sulfoxide
Apexbio Technology LLC RN486 1242156-23-5 10mM (in 1mL DMSO)
RN486 (CAS 1242156-23-5) is a reversible and selective inhibitor of Bruton s tyrosine kinase (BTK) an enzyme prominently expressed in immune cells including B lymphocytes and macrophages BTK participates critically in B-cell receptor (BCR) and Fc receptor (FcR) signaling pathways influencing B-cell differentiation proliferation and antibody production RN486 exhibits potent inhibitory effects (IC50 4 0 nM) and effectively diminishes signaling events B-cell activation and IgG synthesis in cellular assays In animal models RN486 suppresses autoimmune and inflammatory responses reducing disease progression in lupus (NZB NZW mice) and arthritis indicating its utility in autoimmune research
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 Mitomycin C 10mM (in 1mL DMSO)
Mitomycin C (CAS 50-07-7) is an antibiotic compound derived from Streptomyces caespitosus or Streptomyces lavendulae exhibiting anti-cancer properties by interfering with DNA synthesis Its mode of action involves direct formation of covalent adducts with DNA impeding DNA replication In PC3 cells mitomycin C presents an EC50 of approximately 0 14 M Moreover it can potentiate apoptosis induced by TRAIL (TNF-related apoptosis-inducing ligand) through mechanisms independent of p53 modulating apoptosis-related protein expression and caspase activation Due to its cytotoxic mechanism mitomycin C continues to serve as a useful compound in cancer research particularly in apoptosis signaling studies
Apexbio Technology LLC THZ2 1604810-84-5 10mM (in 1mL DMSO)
THZ2 (CAS 1604810-84-5) is a selective inhibitor of cyclin-dependent kinase 7 (CDK7) demonstrating an IC50 of 13 9 nM CDK7 a serine/threonine kinase bound and activated by cyclins regulates cell cycle progression and transcriptional control through phosphorylation of RNA polymerase II (RNAPII) In triple-negative breast cancer (TNBC) cell models THZ2 reduces cellular proliferation induces apoptotic cell death without affecting cell-cycle distribution and inhibits colony formation at low-nanomolar concentrations (IC50 10 nM) In xenograft mouse models THZ2 suppresses tumor growth without noticeable toxicity Thus THZ2 is useful in research investigating CDK7-mediated oncogenic mechanisms in cancer
Apexbio Technology LLC Ezetimibe 163222-33-1 10mM (in 1mL DMSO)
Ezetimibe (CAS 163222-33-1) is a cholesterol absorption inhibitor that targets the intestinal cholesterol transporter Niemann-Pick C1 Like 1 (NPC1L1) It reduces intestinal uptake of cholesterol and dietary carotenoids including - and -carotene lycopene lutein and -cryptoxanthin through downregulating transport proteins such as SR-BI ABCA1 NPC1L1 and transcription factors including SREBP-1/-2 and LXR- In ApoE-deficient mouse models ezetimibe significantly decreases plasma cholesterol levels and attenuates atherosclerotic lesion formation Clinically it lowers LDL cholesterol total cholesterol and triglycerides while elevating HDL cholesterol
Apexbio Technology LLC Betaxolol HCl 63659-19-8 10mM (in 1mL DMSO)
Betaxolol HCl (CAS 63659-19-8) is a selective inhibitor targeting the adrenergic receptor It demonstrates antagonist activity by competitively binding and inhibiting this receptor subtype which plays a significant role in cardiovascular regulation Betaxolol exhibits an IC value of approximately 6 M indicative of moderate inhibitory potency In biomedical research betaxolol serves as a pharmacological tool to investigate receptor signaling pathways and their involvement in conditions such as hypertension arrhythmias and cardiovascular disorders
Apexbio Technology LLC ICG 001 847591-62-2 10mM (in 1mL DMSO)
ICG 001 is a small molecule inhibitor of the canonical Wnt/ -catenin signaling pathway Mechanistically it competes with -catenin for interaction with CREB-binding protein (CBP) thereby selectively disrupting CBP/ -catenin-mediated transcriptional activity driven by the TCF/ -catenin complex (IC50 3 M) Experimental studies demonstrated its use in assessing CBP-dependent biological functions regulated by Wnt signaling Research applications include investigating CBP/ -catenin roles in cancer cell proliferation such as colorectal cancer cells (HCT-116 SW480) glioblastoma stem cell growth and fibrotic responses in pulmonary and dermal experimental models Additionally ICG 001 is under evaluation in clinical studies aiming at treatment of colorectal cancer and leukemia
Apexbio Technology LLC AICAR 10mM (in 1mL DMSO)
A8184 is a small molecule developed primarily as a biomedical research tool It functions through modulation of specific cellular signaling pathways implicated in disease states enabling researchers to probe biological targets and cellular mechanisms By influencing these pathways A8184 provides a methodological approach for dissecting cellular responses and clarifying mechanisms involved in pathological conditions This compound is suited for controlled in vitro studies aimed at elucidating disease pathways and evaluating potential therapeutic avenues in biomedical research contexts
Apexbio Technology LLC GSK3787 188591-46-0 10mM (in 1mL DMSO)
GSK3787 is an irreversible antagonist targeting peroxisome proliferator-activated receptor beta/delta (PPAR- / ) Structurally it acts through covalent modification by binding specific cysteine residues within the ligand-binding domain of PPAR- / thereby disrupting receptor activation and subsequent co-regulator interactions Due to receptor selectivity GSK3787 preferentially inhibits PPAR- / relative to PPAR- Experimental evidence in rodent models demonstrates that oral administration of GSK3787 counteracts agonist-induced gene expression such as Angptl4 and Adrp by reducing recruitment of activated PPAR- / to target gene promoters indicating potential utility in studying PPAR- / -mediated regulatory pathways related to lipid metabolism and gene transcription in vitro and in vivo
Apexbio Technology LLC Cinobufagin 470-37-1 10mM (in 1mL DMSO)
Cinobufagin (CAS 470-37-1) is a steroidal cardiac glycoside recognized for its inhibitory effect on the Na /K -ATPase pump Its inhibitory potency is approximately comparable to that of ouabain By impeding Na /K -ATPase activity cinobufagin disrupts ionic gradients altering intracellular calcium homeostasis and influencing cardiac and cellular functions In biomedical research cinobufagin serves as a valuable pharmacological tool to investigate ion transport mechanisms and explore related signaling pathways implicated in cellular physiology and pathology
Apexbio Technology LLC GDC-0994 1453848-26-4 10mM (in 1mL DMSO)
GDC-0994 (CAS 1453848-26-4) is a selective small-molecule inhibitor targeting extracellular signal-regulated kinases 1 and 2 (ERK1/2) components of the MAP kinase signaling cascade downstream of RAS/RAF/MEK ERK1/2 mediates cell proliferation and differentiation frequently activated due to oncogenic mutations in RAS and BRAF GDC-0994 shows inhibition of ERK1 and ERK2 with IC50 values of 1 1 and 0 3 nM respectively In preclinical models bearing KRAS or BRAF mutant tumor xenografts oral administration of GDC-0994 suppresses ERK phosphorylation and downstream signaling demonstrating significant anti-tumor activity GDC-0994 is a potent tool for studying ERK signaling in cancer research
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
Apexbio Technology LLC Purmorphamine 483367-10-8 10mM (in 1mL DMSO)
Purmorphamine (CAS 483367-10-8) is a synthetic small molecule agonist targeting the Smoothened (Smo) protein a critical component of the Hedgehog (Hh) signaling pathway By binding and activating Smo Purmorphamine induces downstream modulation of key pathway targets such as Gli1 and Patched In vitro studies demonstrated activation with an IC50 value of approximately 1 5 M during competitive assays with the antagonist cyclopamine and an EC50 of about 1 M for alkaline phosphatase (ALP) expression in C3H10T1/2 multipotent cells This agent has been applied in research contexts for inducing osteogenic differentiation with implications for studying bone regeneration and neural degeneration processes
Apexbio Technology LLC Pifithrin-α (PFTα) 63208-82-2 10mM (in 1mL DMSO)
Pifithrin- (PFT CAS 63208-82-2) is a synthetic water-soluble inhibitor targeting the tumor suppressor protein p53 Initially identified by its ability to block activation of p53-responsive genes PFT reduces apoptosis in transformed mouse embryonic fibroblasts (expressing E1a and ras) in a p53-dependent manner Additionally PFT prevents DNA damage-induced growth arrest in human diploid fibroblasts and promotes G2-phase cell cycle arrest following -irradiation It also decreases the expression of pluripotency marker Nanog affecting self-renewal potential in embryonic stem cells without compromising viability Thus PFT serves as a valuable research tool to investigate p53-mediated cellular pathways