Muristerone A is a natural analog of 20-hydroxyecdysone (Item No. 16145). It is an agonist of the ecdysteroid receptor (Kd = 1 nM), a nuclear receptor that heterodimerizes with a retinoid X receptor ortholog and regulates arthropod development.{26923,26924,26920} Muristerone A is used as an agonist in ecdysone-inducible gene expression systems in mammalian cells.{26921,26316} However, it inhibits apoptosis in the human colon carcinoma cell line RKO by inducing the upregulation of Bcl-xL, suggesting limitations in its use in certain types of studies.{26922}
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A natural analog of 20-hydroxyecdysone and agonist of the ecdysteroid receptor (Kd = 1 nM); used as an agonist in ecdysone-inducible gene expression systems in mammalian cells
Formal name: 2β,3β,5β,11α,14,20,22R-heptahydroxy-cholest-7-en-6-one
Synonyms: Mur A
Molecular weight: 496.6
CAS: 38778-30-2
Purity: ≥95%
Formulation: A solid
Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Endocrinology & Metabolism|Hormones & Receptors|RARs, RORs, & RXRs
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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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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