Chemicals

Isoprenoid compounds are a diverse group of natural products which are essential components in all cells. Isoprenoids are biosynthesized from the simple precursors isopentenyl diphosphate (IPP) and dimethylallyl diphosphate (DMAPP). Eukaryotes fungi and some gram-positive bacteria produce IPP through the mevalonate (MVA) pathway whereas gram-negative and some gram-positive bacteria utilize the non-mevalonate or 2-C-methyl-D-erythritol-4-phosphate (MEP) pathway. 4-Diphosphocytidyl-2-C-methyl-D-erythritol (CDP-ME) is an intermediate in the non-mevalonate pathway. It is formed from MEP by CDP-ME Synthase and phosphorylated at the 2-position by CDP-ME kinase to CDP-MEP.

Isoprenoid compounds are a diverse group of natural products which are essential components in all cells. Isoprenoids are biosynthesized from the simple precursors isopentenyl diphosphate (IPP) and dimethylallyl diphosphate (DMAPP). Eukaryotes fungi and some gram-positive bacteria produce IPP through the mevalonate (MVA) pathway whereas gram-negative and some gram-positive bacteria utilize the non-mevalonate or 2-C-methyl-D-erythritol-4-phosphate (MEP) pathway. 2-C-Methyl-D-erythritol 2 4-cyclophosphate (cMEPP) is an intermediate in the non-mevalonate pathway. It is formed by from MECDP Synthase from CDP-MEP and converted to 1-hydroxy-2-methyl-2-buten-4-yl diphosphate (HDMAPP) by IspG (GcpE).

Isoprenoid compounds are a diverse group of natural products which are essential components in all cells. Isoprenoids are biosynthesized from the simple precursors isopentenyl diphosphate (IPP) and dimethylallyl diphosphate (DMAPP). Eukaryotes fungi and some gram-positive bacteria produce IPP through the mevalonate (MVA) pathway whereas gram-negative and some gram-positive bacteria utilize the non-mevalonate or 2-C-methyl-D-erythritol-4-phosphate (MEP) pathway. 1-Hydroxy-2-methyl-2-buten-4-yl 4-diphosphate (HDMAPP or HMBPP) is an intermediate in the non-mevalonate pathway and is biosynthesized from 2-C-Methyl-D-erythritol 2 4-cyclophosphate (cMEPP) by IspG (GcpE). It is the substrate for IspH (LytB) yielding IPP and DMAPP. In addition HDMAPP is the most potent VγVδ T-cell activator identified.

Isopentenyl thiolodiphosphate (ISPP) is an analog of IPP in which the non-bridging oxygen has been replaced by sulfur resulting in a less-reactive compound.

Dimethylallyl thiolodiphosphate (DMASPP) is an analog of DMAPP in which the non-bridging oxygen has been replaced by sulfur resulting in a less-reactive compound. Powered by Bioz See more details on Bioz

Geranyl thiolodiphosphate (GSPP) is an analog of GPP in which the non-bridging oxygen has been replaced by sulfur resulting in a less-reactive compound. GSPP is turned over by avian farnesyl diphosphate synthase (FPPase) more slowly than FPP and acts as a competitive inhibitor (KI = 24.8 μM). Powered by Bioz See more details on Bioz

Farnesyl thiolodiphosphate (FSPP) is an analog of FPP in which the non-bridging oxygen has been replaced by sulfur resulting in a less-reactive compound. Powered by Bioz See more details on Bioz

Echelon's fluorogenic Autotaxin (ATX) substrate FS-3 (L-2000) is a doubly labeled analog of LPC wherin the fluorophore is quenched through intramolecular energy transfer. Hydrolysis of the substrate produces an increase in fluorescence.Autotaxin which has lysophospholipase D (lysoPLD) activity cleaves choline from lysophosphatidylcholine forming lysophosphatidic acid (LPA) a potent mitogen that as been implicated in the pathophysiology of ovarian cancer. LysoPLD/ATX has been demonstrated to increase cell motility neovascularization proliferation and aggressiveness of tumors and is upregulated in numerous cancer lineages (non-small cell lung glioma mammary carcinoma renal cell carcinoma hepatocellular carcinoma). In addition dysregulation of the ATX/LPA pathway is central to the pathophysiology of idiopathic pulmonary fibrosis rheumatoid arthritis and other inflammatory diseases. Modulation of ATX activity through small-molecules is a target with high potential for novel ca

ATX-Red AR-2 is an in vivo imaging probe for visualizing and measuring ATX activity. It is an analog of the autotaxin substrate lysophosphatidylcholine (LPC) and contains a near-infrared fluor (Licor IRDye® 800CW) and quencher (Licor IRDye® QC-1). The design is modeled after FS-3 a fluorogenic ATX substrate that is predictive of ATX activity. In the parent compound fluorescence is quenched through intramolecular energy transfer but when autotaxin cleaves ATX-Red AR-2 fluorescence increases. This activation mechanism is specific to autotaxin in vitro and in vivo.Autotaxin which has lysophospholipase D (lysoPLD) activity cleaves choline from lysophosphatidylcholine forming lysophosphatidic acid (LPA) a potent mitogen that as been implicated in the pathophysiology of ovarian cancer. LysoPLD/ATX has been demonstrated to increase cell motility neovascularization proliferation and aggressiveness of tumors and is upregulated in numerous cancer lineages (non-small cell lung glioma