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Microcystin-LR

ALX-350-012

144 citations

  • ALX-350-012-M001   —   1 mg
    $661.00
  • ALX-350-012-C100   —   100 µg
    $150.00
  • ALX-350-012-C500   —   500 µg
    $372.00
  • Highly pure, potent, and selective inhibitor of PP1 and PP2A
  • Hepatotoxin and tumor promoter
  • Cited in several water quality-related research articles

Microcystin-LR (MC-LR) is an heptapeptide ester hepatotoxin and tumor promoter. MC-LR is an equally potent and selective inhibitor of protein phosphatase 1 (PP1) and 2A (PP2A). PP2B is less sensitive and PP2C is not inhibited up to 4µM. It is useful for affinity-purification of PP2A. The product is not cell-permeable except in liver cells, which appear to have a functional uptake system. It is absorbed by hepatocytes via the multi-specific organic anion transporter. It does not induce any effects on mouse skin or human fibroblasts due to cell membranes impermeability. It, also, has no effect on protein kinases. It is less toxic than the more hydrophobic analogs MC-LF (Prod. No. ALX-350-081), -LW (Prod. No. ALX-350-080), and -LY (Prod. No. ALX-350-148). It frequently contaminates fresh-water lakes and ponds and causes livestock poisonings. Ozonation leads to complete loss of toxicity and toxins from contaminated samples.

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Cyanobacteria are photosynthetic prokaryotes mostly present in freshwater ecosystems. The increasingly frequent appearance of cyanobacteria blooms in lakes and rivers is linked to climate changes and human activities. Microcystins are a group of cyclic heptapeptide hepatotoxins produced by a number of cyanobacterial genera. The most notable of which, and namesake, is the widespread genus Microcystis. Structurally, all microcystins consist of the generalized structure cyclo(-D-Ala1-X2-D-MeAsp3-Y4-Adda5-D-Glu6-Mdha7-). X and Y are variable L-amino acids, D-MeAsp is D-erythro-β-methylaspartic acid and Mdha is N-methyldehydroalanine. Adda is the cyanobacteria unique C20 β-amino acid 3-amino-9-methoxy-2,6,8-trimethyl-10-phenyl-deca-4,6-dienoic acid. Substitutions of the variable L-amino acids at positions 2 and 4 give rise to at least 21 known primary microcystin analogs and alterations in the other constituent amino acids result in more than 90 reported mycrocystins to date.

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Regulatory Status

RUO – Research Use Only