Quinolines and derivatives

Apexbio Technology LLC Avasimibe 166518-60-1 200mg

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Avasimibe (CAS 166518-60-1) is an orally bioavailable inhibitor of acyl-coenzyme A cholesterol acyltransferase (ACAT) an enzyme involved in cholesterol esterification It exhibits potent inhibition with an IC50 of approximately 60 nM In cell-based studies avasimibe reduces intracellular cholesterol esters in a dose-dependent manner without elevating free cholesterol levels suggesting an advantageous safety profile Additionally avasimibe reduces synthesis and secretion of Apo B 100 a constituent of very low-density lipoprotein (VLDL) in HepG2 cells and increases bile acid synthesis in rat hepatocytes Beyond dyslipidemic modulation and anti-atherogenic activities it influences amyloid precursor protein (APP) trafficking reducing its maturation and subsequent amyloid-beta (A ) peptide generation providing avenues for Alzheimer s disease research

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Apexbio Technology LLC Baricitinib (LY3009104, INCB028050) 1187594-09-7 200mg

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Baricitinib (LY3009104 INCB028050 CAS 1187594-09-7) is an orally bioavailable ATP-competitive inhibitor targeting Janus kinases JAK1 and JAK2 It also exhibits moderate inhibition of TYK2 and weaker inhibition against JAK3 In biochemical assays baricitinib inhibits JAK1 and JAK2 with IC50 values of 5 9 nM and 5 7 nM respectively At concentrations below 50 nM baricitinib suppresses intracellular signaling mediated by several pro-inflammatory cytokines notably IL-6 and IL-23 Due to its mechanistic profile baricitinib is actively explored in inflammatory disease research such as rheumatoid arthritis

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Medchemexpress LLC Pictilisib (dimethanesulfonate) | 957054-33-0 | 99.7% | 705.85 | 200 MG

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Pictilisib dimethanesulfonate is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).

• Potent inhibitor of PI3Kα/δ with IC50 of 3 nM
• Modest selectivity against p110β (11-fold) and p110γ (25-fold)
• Reduces tumor cell viability in breast cancer cell lines
• Inhibits Akt phosphorylation and downstream targets of Akt signaling
• Shows high efficacy of antitumor activity in ZD1839-resistant non-small cell lung cancer (NSCLC) cell lines (A549 and H460)
• Highly efficacious in combination with U0126 in inducing cell growth inhibition, G0-G1 arrest, and cell apoptosis
• Reduces secreted VEGF after hypoxic/anoxic exposure
• Leads to tumor stasis in animal models
• Results in tumor regressions during treatment leading to enhanced antitumor responses
• Reduces tumor growth and PI3K and HIF-1 pathway activity in tumor-bearing mice

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Apexbio Technology LLC Resiquimod (R-848) 144875-48-9 100mg

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Resiquimod (R-848) is an immunomodulatory small molecule structurally related to imiquimod It functions primarily by activating immune responses via inducing cytokine release In vitro studies with human peripheral blood mononuclear cells (PBMC) indicate that Resiquimod promotes dose-dependent production of cytokines including interferon-alpha (IFN- ) tumor necrosis factor (TNF) interleukin-1 (IL-1 ) and interleukin-6 (IL-6) Mechanistically Resiquimod increases intracellular IL-1 levels and both monocytes and B-cells respond by secreting IFN upon stimulation In addition it elevates mRNA expression of IFN- TNF and IL-8 in treated PBMC relative to untreated controls Resiquimod demonstrates antiviral and antitumor activities in preclinical animal models frequently utilized as an immune response potentiator and Toll-like receptor (TLR) agonist in biomedical investigations (IC50 values typically range in low micromolar)

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Apexbio Technology LLC NVP-BSK805 2HCl 1092499-93-8 (free base) 200mg

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NVP-BSK805 2HCl is a selective ATP-competitive inhibitor targeting Janus kinase 2 (JAK2) JAK2 part of the JAK kinase family mediates signaling through cytokine receptor systems including type II cytokine GM-CSF receptor gp130 and single-chain receptor families By competitively binding the ATP-binding site of JAK2 NVP-BSK805 inhibits downstream STAT5 phosphorylation and JAK-mediated signaling It displays greater than 20-fold selectivity for JAK2 versus other JAK family members (JAK1 JAK3 TYK2) Cell-based assays demonstrate antiproliferative activity against cells expressing JAK2V617F mutations NVP-BSK805 is commonly employed in vitro and in vivo to investigate JAK2-mediated cellular responses oncogenesis and associated signaling pathways

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eMolecules​ EMOLECULES INC

5000841218 AZIDO-PEG10-AMINE 1G

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