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Filtered Search Results
Medchemexpress LLC Ru.521 10Mm Dmso Solid 1Nl | HY-114180-10MM DMSO SOLID
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Ru.521 10Mm Dmso Solid 1Nl
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Apexbio Technology LLC Tasquinimod 254964-60-8 10mM (in 1mL DMSO)
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Tasquinimod (CAS 254964-60-8) is an orally bioavailable quinoline-3-carboxamide compound with antiangiogenic and antitumor properties It modulates angiogenesis primarily through dual inhibition of S100A9/TLR4 signaling in myeloid-derived suppressor cells (MDSCs) and downregulation of HIF-1 and VEGF expression in tumor and endothelial cells It also enhances thrombospondin-1 (TSP-1) expression further suppressing neovascularization Preclinical studies in human prostate cancer xenograft models indicate significant antineoplastic activity particularly in combination with docetaxel radiation therapy or androgen-depletion strategies suggesting its therapeutic potential for castration-resistant prostate cancer (CRPC)
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Apexbio Technology LLC AGN 194310 229961-45-9 10mM (in 1mL DMSO)
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AGN 194310 is a pan-retinoic acid receptor (RAR) antagonist with affinity for RAR RAR and RAR It binds these receptors with Kd values of 3 nM 2 nM and 5 nM respectively By competing with RAR agonists AGN 194310 blocks receptor-mediated cellular responses In cell-based assays AGN 194310 inhibits the proliferation and colony formation of prostate carcinoma cell lines (LNCaP PC3 DU-145) induces G1 cell cycle arrest and promotes apoptosis In addition it suppresses agonist-induced differentiation in HL60 cells AGN 194310 serves as a research tool to investigate RAR-driven signaling pathways and tumor cell growth mechanisms particularly in oncology studies examining retinoid receptor functions
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Apexbio Technology LLC PF-543 1415562-82-1 10mM (in 1mL DMSO)
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PF-543 (CAS 1415562-82-1) is a cell-permeable inhibitor targeting sphingosine kinase 1 (SphK1) an enzyme that phosphorylates sphingosine to sphingosine-1-phosphate (S1P) It displays potent inhibitory activity against SphK1 with an IC50 of 3 6 nM through sphingosine-competitive (non-ATP competitive) binding Treatment of SphK1-overexpressing head and neck cancer (1483) cells led to a ten-fold decrease in S1P levels confirming effective target engagement PF-543 is widely utilized as a research tool in studies investigating SphK1-mediated signaling pathways in cancer biology and immune cell trafficking
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Apexbio Technology LLC Riociguat 625115-55-1 10mM (in 1mL DMSO)
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Riociguat (CAS 625115-55-1) chemically known as BAY 63-2521 is a small-molecule stimulator of soluble guanylate cyclase (sGC) It directly activates sGC independently and also enhances the enzyme s sensitivity to nitric oxide (NO) leading to elevated cyclic guanosine monophosphate (cGMP) levels Elevated cGMP induces smooth muscle relaxation and vasodilation Riociguat has been examined clinically for potential therapeutic roles in chronic thromboembolic pulmonary hypertension (CTEPH) and pulmonary arterial hypertension (PAH)
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Apexbio Technology LLC ITF2357 (Givinostat) 732302-99-7 10mM (in 1mL DMSO)
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ITF2357 (Givinostat CAS 732302-99-7) is a small molecule inhibitor targeting class I and II histone deacetylases (HDAC) It suppresses hematopoietic colony formation driven by JAK2V617F mutation in chronic myeloproliferative neoplasms Mechanistically ITF2357 induces apoptosis in multiple myeloma (MM) and acute myeloid leukemia (AML) by elevating p21 expression and simultaneously reducing anti-apoptotic proteins Bcl-2 and Mcl-1 Additionally ITF2357 diminishes inflammatory cytokines (IL-1 IL-6 TNF- and IFN- ) in peripheral blood mononuclear cells and inhibits production of IL-6 and VEGF in mesenchymal stromal cells reflecting potential therapeutic applications in cancer research and inflammation regulation
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Apexbio Technology LLC Reversine 656820-32-5 10mM (in 1mL DMSO)
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Reversine (CAS 656820-32-5) is a small molecule inhibitor targeting Aurora kinases a family of serine/threonine kinases involved in mitotic progression Reversine inhibits Aurora kinase A B and C with IC50 values of 150 nM 500 nM and 400 nM respectively In vitro studies show reversine can induce dedifferentiation of murine myoblast cells and possesses regenerative potential Additionally reversine displays anti-tumor effects by suppressing the expression of Aurora kinases thus disrupting cell-cycle progression In cervical carcinoma mouse models (U14 cells) reversine combined with aspirin synergistically decreases tumor growth highlighting reversine s value for cancer biology research
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Apexbio Technology LLC E-64 66701-25-5 10mM (in 1mL DMSO)
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E-64 is a selective inhibitor targeting cysteine proteases isolated originally from Aspergillus cultures Structurally classified as an L-trans-epoxysuccinyl peptide it irreversibly inhibits proteases such as papain ficin and bromelain by covalent binding to the active-site cysteine residue Its inhibitory activity additionally extends to mammalian cysteine proteases including cathepsins B H and L as well as calcium-dependent protease calpain with reported IC50 values ranging approximately between 10-100 nM depending on specific enzyme assays and conditions In research laboratories E-64 is primarily utilized for mechanistic studies active-site titration assays and quantitative evaluation of cysteine protease concentrations and enzyme kinetics
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Apexbio Technology LLC (+)-Bicuculline 485-49-4 10mM (in 1mL DMSO)
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( )-Bicuculline is a competitive antagonist of gamma-aminobutyric acid type A (GABA A) receptors frequently employed as a pharmacological tool to elucidate the functional roles of inhibitory neurotransmission mediated by GABA A By antagonizing GABA binding this compound prevents chloride ion influx leading to reductions in neuronal inhibitory postsynaptic potentials (IPSPs) Additionally ( )-Bicuculline blocks small conductance calcium-activated potassium (SK) channels affecting neuronal excitability and firing patterns It is commonly utilized in electrophysiological studies such as patch-clamp or extracellular recordings to investigate synaptic transmission neuroplasticity mechanisms and epileptic activity models ( )-Bicuculline inhibits GABA A receptors with an IC 50 typically reported in the low micromolar range (approximately 2 5 M)
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Apexbio Technology LLC ABT-263 (Navitoclax) 923564-51-6 10mM (in 1mL DMSO)
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ABT-263 (Navitoclax CAS 923564-51-6) is an orally bioavailable small molecule inhibitor targeting anti-apoptotic proteins of the Bcl-2 family including Bcl-2 Bcl-xl and Bcl-w By disrupting interactions between these anti-apoptotic factors and pro-apoptotic proteins (Bim Bad Bak) ABT-263 promotes activation of caspase-dependent apoptotic pathways resulting in programmed cell death This compound is utilized extensively in oncology research to explore apoptotic mechanisms and evaluate antitumor efficacy in various cancer models
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Apexbio Technology LLC Micafungin sodium 208538-73-2 10mM (in 1mL DMSO)
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Micafungin sodium is an antifungal agent that acts by inhibiting the synthesis of 1 3- -D-glucan an essential polymer for fungal cell wall integrity particularly in Candida albicans In addition to antifungal activities micafungin has been studied for its capacity to suppress biofilm formation by Pseudomonas aeruginosa via downregulation of genes encoding structural biofilm elements such as algC and pelC and the 1 3- -D-glucan-encoding gene ndvB Micafungin has demonstrated synergy with other antifungal compounds in animal models in murine models of systemic Aspergillus fumigatus infection micafungin administration resulted in increased survival rates Micafungin is utilized in biomedical research to investigate antifungal mechanisms combination therapies and inhibition of pathogen biofilms Reported inhibitory activity (IC50) for fungal glucan synthase typically falls within the nanomolar range
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Apexbio Technology LLC vinblastine 865-21-4 10mM (in 1mL DMSO)
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Vinblastine is a naturally-derived alkaloid isolated from Catharanthus roseus It functions as a microtubule inhibitor by binding specifically to tubulin disrupting microtubule polymerization and thereby arresting mitosis at metaphase Due to this mechanism vinblastine is widely investigated for antitumor activities and is commonly employed in biomedical research to study cell division cytoskeletal dynamics and therapeutic interventions in oncology Vinblastine should be stored under sealed dry and cool conditions to maintain molecular integrity and biological activity
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Apexbio Technology LLC Santacruzamate A (CAY10683) 1477949-42-0 10mM (in 1mL DMSO)
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Santacruzamate A (CAY10683 CAS 1477949-42-0) is a selective histone deacetylase (HDAC) inhibitor originally identified in the marine cyanobacterium cf Symploca sp Its mechanism of action involves targeting HDAC enzymes particularly demonstrating high selectivity towards HDAC2 (IC 0 112 nM) when compared with HDAC6 (IC 433 nM) and minimal potency against HDAC4 (IC 1 M) In cellular assays Santacruzamate A reduces growth of tumor cell lines such as HCT-116 colon cancer cells (GI 28 M) and HuT-78 cutaneous T-cell lymphoma cells (GI 1 3 M) It is valuable in epigenetics and oncology research for selectively modulating HDAC2 activity
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Apexbio Technology LLC ANA 12 219766-25-3 10mM (in 1mL DMSO)
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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
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Apexbio Technology LLC TG003 300801-52-9 10mM (in 1mL DMSO)
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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
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