Rhein-13C4 is intended for use as an internal standard for the quantification of rhein (Item No. 17345) by GC- or LC-MS. Rhein is an anthraquinone derivative that has been found in R. rhabarbarum and a metabolite of diacerein (Item No. 11710) that has diverse biological activities, including anticancer, antioxidant, and anti-inflammatory activities.{46596,46597,28413,28415} It induces cell cycle arrest at the S phase and inhibits the proliferation of HepG2 cells when used at concentrations of 40 and 100 µM, respectively.{46597} Rhein (100 and 200 µM) also inhibits proliferation of MCF-7 and MDA-MB-435s breast cancer cells under normoxic and hypoxic conditions.{28413} It reduces controlled cortical impact-induced decreases in catalase and superoxide dismutase (SOD) activity and malondialdehyde (MDA), glutathione, and glutathione disulfide levels in the brain in a rat model of traumatic brain injury when administered at a dose of 12 mg/kg.{46596} Rhein (50 mg/kg per day) reduces increased serum TNF-α, IL-1β, and amylase levels, as well as reduces pancreatic glandular atrophy and fibrosis, in a mouse model of chronic pancreatitis induced by cerulein.{28415}
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An internal standard for the quantification of rhein by GC- or LC-MS
Formal name: 9,10-dihydro-4,5-dihydroxy-9,10-dioxo-2-anthracene-1,3,4-13C3-carboxylic acid-13C
Synonyms: Rheic Acid-13C4
Molecular weight: 288.2
CAS: 1189928-10-6
Purity: ≥95%
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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The tetracycline repressor (TetR) is a transcriptional regulator which normally binds tightly to its palindromic tetO operator DNA, blocking gene expression.{17508} Tet causes the repressor to dissociate from the DNA, allowing transcription to occur. A novel reverse TetR (revTetR) requires tetracycline as a co-repressor to bind tetO and block transcription.{17509,17510} Anhydrotetracycline (hydrochloride) is a powerful effector in both the tetracycline repressor (TetR) and reverse TetR (revTetR) systems, binding the Tet repressor 35-fold more strongly than Tet.{17508,17511} Moreover, anhydrotetracycline poorly binds the 30S ribosomal subunit, compared to Tet,{17512} so it does not act as a general inhibitor of translation and is a poor antibiotic. Perhaps related to this, the concentration of anhydrotetracycline that inhibits eukaryotic cell growth is more than a 1,000-fold above the dose that alters transcription through TetR.{17508}
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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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