GMQ is an activator of acid-sensing ion channel 3 (ASIC3).{54008} It evokes rapid inward currents with little desensitization in CHO cells expressing ASIC3 (EC50 = 67 µM at neutral pH). It is also an inhibitor of the GABAA receptor (IC50 = 0.39 µM in primary rat hippocampal neurons).{54009} GMQ has stimulatory effects on large-conductance calcium-activated potassium (BKCa) channels in GH3 rat pituitary cells and on non-selective cation currents in Rolf B1.T olfactory sensory neurons.{54010} It increases paw licking time in Asic3+/+ and, to a lesser extent, Asic3-/- mice when administered at a dose of 100 µM, an effect that can be blocked by the ASIC inhibitor amiloride (Item No. 14409).{54008}
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An ASIC3 activator (EC50 = 67 µM for evoking rapid inward currents in ASIC3-expressing CHO cells at neutral pH); an inhibitor of the GABAA receptor (IC50 = 0.39 µM in primary rat hippocampal neurons); increases paw licking time in Asic3+/+ and, to a lesser extent, Asic3-/- mice at 100 µM
Formal name: N-(4-methyl-2-quinazolinyl)-guanidine, monohydrochloride
Synonyms:
Molecular weight: 237.7
CAS: 5361-15-9
Purity: ≥95%
Formulation: A crystalline solid
The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}
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The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}
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1,2-Dipalmitoyl-sn-glycero-3-PC (DPPC) is a zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers, bilayers, and liposomes for use in a variety of applications.{14480,24261,14478,14479} It has been used in the formation of proteoliposomes for implantation of γ-glutamyl transpeptidase into human erythrocyte membranes.{14478} Incorporation of glycosphingolipid antigens into DPPC-containing liposomes increases the immunogenicity of the antigens in mice.{14479}
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Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. (R)-Roscovitine is a potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM.{14988} It also inhibits Cdk7/cyclin H, Cdk5/p35, and cell division cycle (cdc)/cyclin B with IC50 values of 0.49, 0.16, and 0.65 µM, respectively.{14987,14988,14991} (R)-Roscovitine inhibits the growth of rapidly proliferating cells with an average IC50 value of 15.2 µM against a panel of 19 human tumor cell lines.{14988} In murine models of polycystic kidney disease, (R)-roscovitine effectively inhibited disease progression at doses of 50-100 mg/kg.{14564}
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