Dimethyl Sulfoxide
Apexbio Technology LLC NVP-AEW541 475489-16-8 10mM (in 1mL DMSO)
NVP-AEW541 (CAS 475489-16-8) is a selective small-molecule inhibitor targeting the insulin-like growth factor-I receptor (IGF-IR) kinase activity Structurally classified as a pyrrolo[2 3-d]pyrimidine derivative NVP-AEW541 effectively inhibits IGF-IR autophosphorylation disrupting downstream IGF-IR mediated signaling cascades It exhibits an IC50 of approximately 0 086 M against IGF-IR kinase In vitro research has demonstrated that treatment of ECC-1 and USPC-1 endometrial cancer cell lines with NVP-AEW541 leads to altered cell cycle progression induction of apoptosis and suppression of proliferation Furthermore NVP-AEW541 has been shown to enhance radiosensitivity specifically in PTEN wild-type cancer cell lines indicating its potential utility as an adjunctive therapeutic agent in oncology research
Apexbio Technology LLC SCR7 1533426-72-0 10mM (in 1mL DMSO)
SCR7 (CAS 1533426-72-0) is a small-molecule inhibitor targeting DNA ligase IV and to a lesser extent DNA ligase III It interacts with the DNA-binding domain of DNA ligase IV thereby diminishing its affinity for double-strand breaks (DSBs) and effectively blocking nonhomologous end-joining (NHEJ)-mediated DNA repair In cell culture models expressing inducible Cas9 SCR7-mediated transient inhibition of NHEJ promotes increased homologous-directed repair (HDR) by facilitating accumulation in the S/G2 phase SCR7 treatment in mice transiently impairs lymphocyte development due to the reversible inhibition of DNA ligase IV activity during V(D)J recombination Thus SCR7 serves as a useful tool in genome editing research to enhance precise gene editing efficiency
Apexbio Technology LLC Triptolide 38748-32-2 10mM (in 1mL DMSO)
Triptolide (CAS 38748-32-2) is a biologically active diterpenoid originally isolated from the traditional Chinese herb Tripterygium wilfordii It exerts inhibitory effects by suppressing interleukin-2 expression in activated T cells and impeding NF- B-mediated transcriptional activation Triptolide inhibits invasion and migration of ovarian cancer cells via reducing matrix metalloproteinases MMP-7 and MMP-19 expression and enhancing E-cadherin expression Additionally it induces RNA polymerase II degradation leading to apoptosis and reduced proliferation in cancer cell lines and rheumatoid arthritis synovial fibroblasts Consequently triptolide serves as a valuable tool for immunology oncology and inflammation research
Apexbio Technology LLC ANA 12 219766-25-3 10mM (in 1mL DMSO)
ANA 12 (CAS 219766-25-3) is a potent and selective antagonist of tropomyosin receptor kinase B (TrkB) the receptor for neurotrophins BDNF and NT-4/5 It binds non-competitively to extracellular sites on TrkB exhibiting IC50 values of 45 6 nM (high-affinity site) and 41 1 M (low-affinity site) ANA 12 inhibits BDNF-induced TrkB activation effectively blocking downstream signaling pathways including PLC- PI3K and MAPK In mouse models ANA 12 administration reduces endogenous brain TrkB activity and demonstrates antidepressant and anxiolytic properties supporting its use for researching psychiatric disorders and neuronal signaling
Apexbio Technology LLC Disulfiram 97-77-8 10mM (in 1mL DMSO)
Disulfiram (CAS 97-77-8) is a small molecule compound recognized as a copper ionophore facilitating intracellular transport of Cu ions It inhibits inflammasome-dependent pyroptotic cell death IL-1 secretion and gasdermin D (GSDMD)-mediated pore formation in liposomes within human and murine cellular models Mechanistically disulfiram elevates intracellular reactive oxygen species (ROS) concentrations in the presence of copper initiating copper-dependent cell death Additionally disulfiram disrupts the ubiquitin-proteasome protein degradation pathway in tumor cells impairing cellular waste clearance and inducing apoptosis Research demonstrates its potential anti-cancer activity particularly synergistically enhanced by copper supplementation and cardioprotective effects against ischemia-reperfusion-induced damage
Apexbio Technology LLC AZD7762(Synonyms: AZD-7762, AZD 7762, 860352-01-8), 10mM (in 1mL DMSO), CAS: 860352-01-8.
AZD7762 (CAS No 860352-01-8) is an ATP-competitive inhibitor targeting the checkpoint kinases Chk1 and Chk2 regulatory enzymes activated upon DNA damage that control cell-cycle progression through phosphorylation of CDC25 phosphatases By competitively binding the ATP-binding pocket of Chk1 AZD7762 blocks Chk1-mediated phosphorylation of CDC25C exhibiting an IC50 of approximately 5 nM and Ki of 3 6 nM This inhibition prevents DNA damage-induced cell cycle arrest and interrupts DNA repair mechanisms promoting apoptosis in tumor cells Consequently AZD7762 acts as a chemosensitizing agent enhancing the cytotoxic effects of DNA-damaging therapies in oncology research
Apexbio Technology LLC Ramelteon(Synonyms: Rozerem, TAK-375, Ramelteon, Melatonin receptor agonist, MT1/MT2 agonist), 10mM (in 1mL DMSO), CAS: 196597-26-9.
Ramelteon (CAS 196597-26-9) is a potent orally active agonist selective for MT1 and MT2 melatonin receptors Structurally characterized by its S-enantiomer and ether functional group ramelteon exhibits high binding affinity toward MT1 and MT2 receptors with reported Ki values of 14 pM and 112 pM respectively whereas affinity for the MT3 receptor is considerably lower (Ki 2650 nM) By activating MT1 and MT2 receptors ramelteon suppresses cAMP production in human cells expressing these receptors with IC50 values of 21 2 pM/L (MT1) and 53 4 pM/L (MT2) Given its receptor selectivity and minimal side-effect profile ramelteon is frequently utilized in research investigating circadian rhythms and sleep disorders
Apexbio Technology LLC Romidepsin (FK228, depsipeptide) 128517-07-7 10mM (in 1mL DMSO)
Romidepsin (FK228 depsipeptide CAS 128517-07-7) is a small-molecule inhibitor targeting histone deacetylases (HDACs) Initially isolated from Chromobacterium violaceum romidepsin preferentially inhibits class I enzymes HDAC1 and HDAC2 over class II HDAC4 and HDAC6 Inhibition of HDAC activity by romidepsin results in increased histone acetylation promoting transcriptional activation of tumor suppressor genes Mechanistically this compound can trigger cellular differentiation cell-cycle arrest apoptosis and altered gene expression in various malignancies Romidepsin serves as a research tool to investigate epigenetic regulation and has notable anticancer properties in cell models such as neuroblastoma and cutaneous T-cell lymphoma
Apexbio Technology LLC TG003 300801-52-9 10mM (in 1mL DMSO)
TG003 (CAS 300801-52-9) is a selective inhibitor targeting the Cdc2-like kinase (Clk) family and casein kinase 1 (CK1) Specifically it demonstrates notable potency against mClk1 mClk2 and mClk4 with IC50 values of approximately 20 nM 200 nM and 15 nM respectively TG003 competitively binds with ATP at Clk1 modulating Clk-mediated phosphorylation of serine/arginine-rich (SR) proteins involved in alternative mRNA splicing Studies using HeLa cellular extracts and animal models have shown that TG003 alters splice site selection and pre-mRNA processing suggesting potential utility for investigating RNA splicing regulatory mechanisms
Apexbio Technology LLC A-740003(Synonyms: A740003, A 740003, P2X7 Receptor Antagonist A-740003, A-740003 P2X7 Antagonist, 861393-28-4), 10mM (in 1mL DMSO), CAS: 861393-28-4.
A-740003 (CAS 861393-28-4) is a selective and competitive antagonist targeting the P2X7 receptor a member of the ATP-gated ionotropic P2X receptor family involved in immune cell signaling cytokine secretion apoptosis and cellular proliferation The antagonist displays IC50 values of 18 nM and 40 nM against mouse and human P2X7 receptors respectively In human THP-1 macrophage-like cells A-740003 inhibits pore formation assessed by Yo-Pro uptake assay (IC50 92 nM) and reduces interleukin-1 secretion (IC50 156 nM) This compound is employed in research investigating P2X7-mediated inflammatory pathways and neuropathic pain mechanisms
Apexbio Technology LLC Fenretinide 65646-68-6 10mM (in 1mL DMSO)
Fenretinide (4-HPR) is a synthetic retinoic acid analog which acts primarily through inhibition of focal adhesion kinase (FAK) and modulation of related signaling cascades Fenretinide induces apoptosis in various tumor cell lines such as prostate ovarian cervical endometrial breast small-cell lung carcinoma and malignant hematopoietic cells Mechanistically Fenretinide promotes apoptotic cell death through reactive oxygen species (ROS)-mediated DNA fragmentation and disrupts tumor cell migration and invasion via interference with the FAK/AKT/GSK3 signaling axis and destabilization of -catenin Fenretinide is frequently utilized as a chemopreventive agent in oncology research particularly for investigating mechanisms of growth inhibition and cell migration suppression
Apexbio Technology LLC GSK343 1346704-33-3 10mM (in 1mL DMSO)
GSK343 (CAS 1346704-33-3) is a selective SAM-competitive inhibitor targeting the histone lysine methyltransferase EZH2 which is the catalytic component of polycomb repressive complex 2 (PRC2) responsible for trimethylation of histone H3 at lysine 27 (H3K27me3) By competitively inhibiting EZH2 s methyltransferase activity GSK343 disrupts H3K27me3-mediated transcriptional silencing It shows potent inhibitory activity against EZH2 (IC50 4 nM) moderate inhibition against EZH1 (240 nM) but minimal impact on other SAM-dependent enzymes In vitro studies with various cancer cell models confirm its ability to reduce H3K27 trimethylation limit proliferation induce apoptosis promote autophagy and enhance chemosensitivity highlighting its utility as a research tool to study EZH2-related mechanisms
Apexbio Technology LLC BI6727 (Volasertib)(Synonyms: Volasertib, BI-6727, BI 6727, Plk inhibitor BI6727, Polo-like kinase inhibitor BI6727), 10mM (in 1mL DMSO), CAS: 755038-65-4.
BI6727 (Volasertib CAS 755038-65-4) is a selective inhibitor of Polo-like kinases (Plk) primarily targeting Plk1 with an IC50 of 0 87 nM and showing lower potency towards Plk2 (IC50 5 nM) and Plk3 (IC50 56 nM) Plk1 regulates the G2/M cell cycle transition and is commonly overexpressed in various tumor types representing a potential therapeutic target BI6727 inhibits proliferation across multiple tumor cell lines including colorectal (HCT116 EC50 23 nM) lung (NCI-H460 EC50 21 nM) melanoma (BRO EC50 11 nM) and hematologic cancer (GRANTA EC50 15 nM) In vivo BI6727 administration induced apoptosis and reduced tumor growth in mouse HCT116 and NCI-H460 xenograft models
