Anti-IDH1 Antibody Prodrug, Protease Activated (A2E8)

CAT#: VS-1025-YC24

The Anti-IDH1 Antibody Prodrug, Protease Activated (A2E8) is an antibody prodrug comprised of a recombinant mouse antibody targeting human IDH1, linked to a masking peptide that conceals the active antigen-binding site via a protease-cleavable linker. The mask peptide is recombinantly attached to the amino terminus of either the light or heavy chain of the antibody, designed to block access to the antigen-binding site and physically prevent the antibody from binding to IDH1 protein. Once the masking peptide is cleaved by matrix metalloproteinases (MMPs), the prodrug is activated, allowing the unmasked monoclonal antibody component to bind to IDH1 effectively. IDH1 (Isocitrate Dehydrogenase 1) is a metabolic enzyme that becomes an oncogene through specific point mutations (most commonly R132H) in lower-grade gliomas and acute myeloid leukemia. This mutation produces an onco-metabolite, 2-hydroxyglutarate (2-HG), which disrupts epigenetic regulation. Inhibitors targeting the mutant IDH1 are a novel therapeutic strategy.

Gene Expression
Figure 1 IF staining of human cell line A-431 Figure 2 Liver Figure 3 Testis Figure 4 Prostate Figure 5 RNA cell line category: Cell line enhanced (Hep G2, RT4)

Specifications

  • Host Animal
  • Mouse
  • Applications
  • In situ zymography (ISZ), Cytotoxicity assay (Cyt), Functional assay
  • Specificity
  • Human IDH1
  • Target
  • IDH1
  • Species Reactivity
  • Human
  • Isotype
  • IgG
  • Clone
  • A2E8
  • Masking Approach
  • Affinity mask
  • Mask
  • A synthetic peptide
  • Protease Cleavable Linker
  • MMP-cleavable linker
  • Protease Substrate
  • MMPs
  • Purification
  • Protein A purified
  • Buffer
  • PBS, pH 7.4
  • Preservative
  • No preservatives
  • Storage
  • Store at 4°C short term. For long term storage, store at -20°C, avoiding freeze/thaw cycles.

Target

  • Introduction
  • Isocitrate dehydrogenases catalyze the oxidative decarboxylation of isocitrate to 2-oxoglutarate. These enzymes belong to two distinct subclasses, one of which utilizes NAD(+) as the electron acceptor and the other NADP(+). Five isocitrate dehydrogenases have been reported: three NAD(+)-dependent isocitrate dehydrogenases, which localize to the mitochondrial matrix, and two NADP(+)-dependent isocitrate dehydrogenases, one of which is mitochondrial and the other predominantly cytosolic. Each NADP(+)-dependent isozyme is a homodimer. The protein encoded by this gene is the NADP(+)-dependent isocitrate dehydrogenase found in the cytoplasm and peroxisomes. It contains the PTS-1 peroxisomal targeting signal sequence. The presence of this enzyme in peroxisomes suggests roles in the regeneration of NADPH for intraperoxisomal reductions, such as the conversion of 2, 4-dienoyl-CoAs to 3-enoyl-CoAs, as well as in peroxisomal reactions that consume 2-oxoglutarate, namely the alpha-hydroxylation of phytanic acid. The cytoplasmic enzyme serves a significant role in cytoplasmic NADPH production. Alternatively spliced transcript variants encoding the same protein have been found for this gene.
  • Alternative Names
  • IDH; IDP; IDCD; IDPC; PICD; HEL-216; HEL-S-26
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