R-Palmitoyl-(2-methyl) ethanolamide (RP-2ME) is a metabolically stable analog of the anti-inflammatory endogenous cannabinoid, palmitoyl ethanolamide (PEA). PEA is an endogenous cannabinoid found in brain, liver, and other mammalian tissues.{2415} PEA has also been isolated from egg yolk, and found to have anti-anaphylactic and anti-inflammatory activity in vitro.{1633} RP-2ME is a synthetic analog of PEA which incorporates an (R)-methyl group vicinal to the alcohol on the ethanolamine moiety. RP-2ME inhibits FAAH-mediated hydrolysis of AEA by 54% at a concentration of 100 µM.{9113} It also has weak CB receptor affinity, in that 100 µM inhibits agonist binding (1 nM CP 55,940 or WIN 55,212-2) only 26% and 15.5% at the human CB1 and CB2 receptors, respectively.{9113}
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A metabolically stable analog of the anti-inflammatory endogenous CB, PEA; inhibits FAAH-mediated hydrolysis of AEA by 54% at a concentration of 100 µM; has weak CB receptor affinity, in that 100 µM inhibits agonist binding (1 nM CP 55,940 or WIN 55,212-2) only 26% and 15.5% at the human CB1 and CB2 receptors, respectively
Formal name: N-(2R-hydroxypropyl)-hexadecanamide
Synonyms: RP-2ME
Molecular weight: 313.5
CAS: 179951-56-5
Purity: ≥98%
Formulation: A crystalline solid
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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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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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 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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