Ciclesonide-d7 is intended for use as an internal standard for the quantification of ciclesonide (CIC; Item No. 18227) by GC- or LC-MS. Ciclesonide is a prodrug form of the glucocorticoid receptor agonist desisobutyryl-CIC (des-CIC).{29504} CIC binds to the glucocorticoid receptor with a Ki value of 37 nM.{29502} It is selective for the glucocorticoid receptor over the estrogen, progesterone, and testosterone receptors. CIC inhibits eosinophil influx into the lung (ED50 = 0.49 mg/kg) and reduces sephadex-induced lung edema (ED50 = 0.72 mg/kg) in a rat model of ovalbumin-sensitized and -challenged airway inflammation. Formulations containing CIC have been used in the maintenance treatment of asthma and in the treatment of allergic rhinitis.
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An internal standard for the quantification of ciclesonide by GC- or LC-MS
Formal name: (11β,16α)-16,17-[[(R)-cyclohexylmethylene]bis(oxy)]-11-hydroxy-21-[2-(methyl-d3)-1-oxopropoxy-2,3,3,3-d4]-pregna-1,4-diene-3,20-dione
Synonyms: CIC-d7
Molecular weight: 547.7
CAS: 1225382-70-6
Purity: ≥99% deuterated forms (d1-d7)
Formulation: A 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 maintenance of embryonic stem cells in culture typically requires feeder cells and various exogenous factors found in serum. Murine embryonic stem (mES) cells can be maintained in the absence of feeder cells and serum but require the leukemia inhibitor factor (LIF) and bone morphogenic protein (BMP) to prevent differentiation and promote self-renewal. SC-1 is a small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state.{14533} The activity of SC-1 is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.{14533} Inhibition of RasGAP increases Ras signaling via the PI3-kinase pathway which promotes self-renewal, whereas inhibition of ERK blocks differentiation.
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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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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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