Lysosphingomyelin is an endogenous bioactive sphingolipid and a constituent of lipoproteins.{18803,18804} It is produced by the removal of the acyl group from sphingomyelin by a deacylase and acts as a precursor in the biosynthesis of sphingosine-1-phosphate (S1P; Item No. 62570). D-erythro Lysosphingomyelin is an agonist of the S1P receptors S1P1, S1P2, and S1P3 (EC50s = 167.7, 368.1, and 482.6 nM, respectively, for the human receptors).{37413} It is also an agonist of the orphan receptor ovarian cancer G protein-coupled receptor 1 (ORG1) that induces calcium accumulation in cells overexpressing OGR1 (EC50 = ~35 nM).{59108} Levels of D-erythro lysosphingomyelin are increased in skin isolated from patients with atopic dermatitis, as well as postmortem brain from patients with Niemann-Pick disease type A, but not type B.{18804,59109} L-threo lysosphingomyelin is also an S1P1-3 agonist (EC50s = 19.3, 131.8, and 313.3 nM, respectively).{37413} This product is a mixture of D-erythro and L-threo lysosphingomyelin. [Matreya, LLC. Catalog No. 1321]
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A mixture of the bioactive sphingolipids D-erythro and L-threo lysosphingomyelin
Formal name: 2-[[[(2-amino-3-hydroxy-4-octadecen-1-yl)oxy]hydroxyphosphinyl]oxy]-N,N,N-trimethyl-ethanaminium, inner salt
Synonyms: D-erythro/L-threo Lyso SM(18:1)|D-erythro/L-threo Sphingosine-1-Phosphocholine (d18:1)|D-erythro/L-threo-Sphingosylphosphorylcholine
Molecular weight: 464.6
CAS: 82970-80-7
Purity: ≥98%
Formulation: A 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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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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