Dimethyl Sulfoxide
Apexbio Technology LLC Didanosine 69655-05-6 10mM (in 1mL DMSO)
Didanosine is a nucleoside analogue known to inhibit reverse transcriptase enzymes by acting as a competitive inhibitor and terminator of viral DNA elongation Mechanistically didanosine is phosphorylated intracellularly to its active metabolite dideoxyadenosine triphosphate (ddATP) an analog of dATP Incorporation of ddATP into viral DNA by viral reverse transcriptase causes premature termination of DNA synthesis thereby inhibiting retroviral replication Didanosine is frequently employed as an experimental tool in studies examining antiviral activity and resistance mechanisms in retroviral infection models particularly HIV research In vitro assays commonly report IC50 values for didanosine against HIV reverse transcriptase in the range of approximately 0 5 to 10 M varying according to experimental conditions and viral strain sensitivity evaluated
Apexbio Technology LLC Argatroban 74863-84-6 10mM (in 1mL DMSO)
Argatroban is a synthetic small-molecule inhibitor acting as a direct binder to thrombin s active site thereby blocking the thrombin-mediated conversion of fibrinogen into fibrin It competitively inhibits thrombin-induced platelet activation and blood clot formation exhibiting an inhibitory constant (Ki) of approximately 19 nM Due to its specificity and direct mechanism Argatroban is frequently employed in experimental research scenarios to investigate thrombin-dependent coagulation pathways platelet aggregation studies and antithrombotic effects in various in vitro assays and animal thrombosis models
Apexbio Technology LLC Etodolac 41340-25-4 10mM (in 1mL DMSO)
Etodolac (CAS 41340-25-4) is a selective cyclooxygenase-2 (COX-2) inhibitor belonging to the class of non-steroidal anti-inflammatory drugs (NSAIDs) It exhibits inhibitory activity against COX-2 with an IC50 of 53 5 nM Etodolac is commonly utilized for research involving inflammatory conditions such as osteoarthritis and rheumatoid arthritis In isolated rabbit articular chondrocytes stimulated with TNF Etodolac prevented apoptotic cell shrinkage and suppressed caspase-3/7 activation Conversely in human malignant rhabdoid tumor cells (FRTK-1) Etodolac induced apoptosis in a dose-dependent manner increasing activities of caspase-3 -8 and -9
Apexbio Technology LLC Alfacalcidol 41294-56-8 10mM (in 1mL DMSO)
Alfacalcidol is a vitamin D analog functioning as an inhibitor of bone resorption through modulation of calcium homeostasis By binding specifically to vitamin D receptors (VDR) located in calcium-regulating tissues such as intestine bone kidney and parathyroid glands Alfacalcidol contributes to mineral metabolism and bone turnover regulation Preclinical studies using ovariectomized animal models demonstrate that Alfacalcidol at pharmacological doses not inducing hypercalcemia suppresses osteoclast-mediated bone resorption while preserving calcium balance in plasma and urine Due to these properties Alfacalcidol is frequently utilized in biomedical research to investigate mechanisms involved in osteoporosis progression and potential therapeutic interventions addressing calcium and bone metabolism disorders
Apexbio Technology LLC Eltrombopag 496775-61-2 10mM (in 1mL DMSO)
Eltrombopag is a small molecule orally bioavailable non-peptide agonist targeting the thrombopoietin (TPO) receptor also known as c-Mpl receptor Upon activating this receptor pathway eltrombopag promotes intracellular signaling leading to increased proliferation and differentiation of megakaryocyte progenitor cells thereby stimulating platelet production (thrombopoiesis) In biochemical assays eltrombopag shows potent activity exhibiting an IC50 value of approximately 0 69 M As a research tool this compound is utilized widely in studies investigating mechanisms regulating platelet homeostasis thrombocytopenia-related diseases and efforts to elucidate novel therapeutic strategies targeting hematopoietic lineage differentiation
Apexbio Technology LLC Busulfan 55-98-1 10mM (in 1mL DMSO)
Busulfan is a DNA alkylating agent widely used in biomedical research as an anticancer compound It functions by forming cross-links on guanine bases within DNA leading to DNA damage and subsequent inhibition of cell growth and proliferation In vitro studies reveal that exposure to busulfan (IC50 range approximately 7 5 120 M) promotes cellular senescence in normal human fibroblast cell lines mediated through increased reactive oxygen species (ROS) and sustained activation of MAPK signaling pathways Additionally busulfan is utilized in fertility and reproductive biology research due to its ability to induce apoptosis in male germ cells reducing germ cell populations in experimental mouse models
Apexbio Technology LLC Everolimus (RAD001) 159351-69-6 10mM (in 1mL DMSO)
Everolimus (RAD001) is an orally bioavailable small-molecule inhibitor targeting mammalian target of rapamycin (mTOR) an integral serine/threonine kinase regulating cell proliferation metabolism and survival within the PI3K/Akt pathway Everolimus binds intracellularly to the immunophilin FKBP12 the resulting complex subsequently interacts directly with mTOR inhibiting its kinase activity thereby reducing downstream phosphorylation of S6 kinase 1 (S6K1) and the eukaryotic initiation factor 4E-binding protein (4EBP) Functionally Everolimus exerts immunosuppressive properties used clinically to prevent organ transplant rejection and demonstrates antitumor activity against several malignancies including renal cell carcinoma and basal cell carcinoma Commonly utilized in cancer research Everolimus inhibits mTOR with IC50 values reported in the low nanomolar range ( 1 3 nM)
Apexbio Technology LLC SRT1720 HCl 1001645-58-4 10mM (in 1mL DMSO)
SRT1720 HCl is a small molecule activator of SIRT1 exerting more potent activation than resveratrol It functions through a SIRT1- and PGC-1 -dependent mechanism modulating mitochondrial oxidative metabolism and insulin sensitivity The compound has demonstrated activity in regulating cell growth and apoptosis in multiple myeloma (MM) cells without notably affecting normal cell viability Its antitumor properties relate to activation of caspase-8 caspase-9 caspase-3 and PARP enhancement of reactive oxygen species generation induction of ATM/CHK2 signaling suppression of NF- B signaling and reduction of VEGF-induced migration SRT1720 is utilized in biomedical research to investigate metabolic pathways tumor biology and potential sensitization effects to chemotherapy agents
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 Evacetrapib (LY2484595) 1186486-62-3 10mM (in 1mL DMSO)
Evacetrapib (LY2484595 CAS 1186486-62-3) is a potent and selective inhibitor targeting cholesteryl ester transfer protein (CETP) a regulator of lipid metabolism Evacetrapib exhibits inhibitory activity with IC50 values of 5 5 nM in assays containing recombinant human CETP and 26 nM within human plasma CETP assays In vivo oral administration at 30 mg/kg in human CETP/ApoAI double-transgenic mice significantly reduces CETP activity and elevates HDL-cholesterol concentration (ED50 5 mg/kg) Evacetrapib does not elevate blood pressure nor induce aldosterone or cortisol synthesis in model systems highlighting its potential in cardiovascular research related to coronary artery disease
Apexbio Technology LLC PF-562271 HCl 939791-41-0 10mM (in 1mL DMSO)
PF-562271 HCl (CAS 939791-41-0) is a potent ATP-competitive reversible inhibitor targeting focal adhesion kinase (FAK) and its homolog proline-rich tyrosine kinase 2 (Pyk2) It inhibits FAK and Pyk2 enzymatic activity with reported IC50 values of 1 5 nmol/L and 14 nmol/L respectively FAK is a non-receptor tyrosine kinase regulating cell adhesion migration and growth while Pyk2 shares structural similarity to FAK In animal models of cancer PF-562271 reduces tumor progression and metastatic spread with dose-dependent suppression of FAK phosphorylation (EC50 93 ng/mL) Thus PF-562271 serves as an important tool for investigating FAK/Pyk2-mediated pathways in oncology research
Apexbio Technology LLC LY2109761 700874-71-1 10mM (in 1mL DMSO)
LY2109761 (CAS 700874-71-1) is a selective small-molecule inhibitor targeting type I and type II transforming growth factor-beta (TGF- ) receptors (T RI/II) with Ki values of 38 nM and 300 nM respectively Acting through ATP-binding site competition in the TGF- receptor I kinase domain (IC50 69 nM) LY2109761 inhibits downstream signaling pathways implicated in tumor development and metastasis In preclinical studies LY2109761 reduced proliferation migration invasion and promoted apoptosis across various cancer cell types including pancreatic carcinoma glioblastoma and myelomonocytic leukemia It also lowered radiotherapy-induced pulmonary fibrosis in animal models illustrating its broad research utility
Apexbio Technology LLC GSK2126458(Synonyms: Omipalisib, GSK-2126458, GSK 2126458, Omipalisib (GSK2126458)), 10mM (in 1mL DMSO), CAS: 1086062-66-9.
GSK2126458 (CAS 1086062-66-9) is a small molecule inhibitor targeting PI3K and mTOR pivotal regulators in cell growth proliferation and tumor progression GSK2126458 demonstrates potent inhibitory activity against PI3K (Ki 19 pM) In colon cancer cells combined use with DDR1-IN-1 enhances its antiproliferative effects Additionally the compound induces G1 phase arrest in BT474 breast cancer cells and sensitizes nasopharyngeal carcinoma (NPC) cell lines to radiation therapy In vivo studies show that combining GSK2126458 with radiation or with MEK and BRAF inhibitors suppresses tumor growth GSK2126458 also influences cellular autophagy pathways highlighting its utility in oncology-focused biomedical research