Quinidine-d3 is intended for use as an internal standard for the quantification of quinidine (Item No. 20356) by GC- or LC-MS. Quinidine is a stereoisomer of the antimalarial agent quinine (Item No. 23958) and a class Ia antiarrhythmic agent.{37790,37791} Quinidine blocks the voltage-gated sodium (Nav) channel Nav1.5 in a use-dependent manner.{37790} It decreases the amplitude and duration of action potentials in isolated canine ventricular myocytes.{37792} Quinidine inhibits KKr, peak INa, and late INa (IC50s = 4.5, 11, and 12 µM, respectively) and can induce torsade de pointes in isolated rabbit hearts when used at a concentration of 1 µM.{37791} It induces QT prolongation in dogs.{37793} Quinidine also binds to M2 muscarinic acetylcholine receptors (Ki = 7.5 µM for human recombinant receptors expressed in HM2-B10 cells).{37794} Formulations containing quinidine have been used in the treatment of atrial fibrillation and ventricular arrhythmias.
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An internal standard for the quantification of quinidine by GC- or LC-MS
Formal name: 6′-(methoxy-d3)-cinchonan-9S-ol
Synonyms: (+)-Quinidine-d3|β-Quinidine-d3
Molecular weight: 327.4
CAS: 1267657-68-0
Purity: ≥99% deuterated forms (d1-d3)
Formulation: A solid
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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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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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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The PtdIn phosphates play an important role in the generation and transduction of intracellular signals.{8344,4096,14518} PtdIns-(3,4,5)-P3-biotin is an affinity probe which allows the PIP3 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(3,4,5)-P3-biotin to serve as a general probe for any protein with a high affinity binding interaction with inositol-(3,4,5)-triphosphate phospholipids, such as phosphatidylinositol 3-kinase, PTEN, or PH-domain-containing proteins.
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