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Chromatin/Epigenetics

Epigenetics

Epigenetics means above genetics. It determines how much and whether a gene is expressed without changing DNA sequences. Epigenetic regulations include, 1. DNA methylation: the addition of methyl group to DNA, converting cytosine to 5-methylcytosine, mostly at CpG sites; 2. Histone modifications: posttranslational modificationEpigeneticss of histone proteins including acetylation, methylation, ubiquitylation, phosphorylation and sumoylation; 3. miRNAs: non-coding microRNA downregulating gene expression; 4. Prions: infectious proteins viewed as epigenetic agents capable of inducing a phenotype without changing the genome.

Products for  Chromatin/Epigenetics

  1. Cat.No. Product Name Information
  2. A4537 Fumonisin B1 Mycotoxin produced by Fusarium moniliforme. Potently inhibits sphingosine N-acyltransferase (ceramide synthase), causing an accumulation of sphingoid bases (IC50 ~ 75 nM). Also inhibits protein phosphatases; IC50 values are 80, 300, 400, 500 and 3000 μM for PP5, PP2Cα, PP2A, PP1γ2 and PP2B respectively.
  3. A4536 Fostriecin sodium salt Originally identified as an antitumor antibiotic from Streptomyces pulveraceous. Displays potent inhibition of protein phosphatase types 2A (PP2A) and 4 (PP4) with IC50 values of 1.5 nM and 3 nM respectively. Also exhibits weaker inhibition of topoisomerase II (IC50 = 40 μM) and protein phosphatase type 1 (PP1) (IC50 = 131 μM) with no apparent inhibition of protein phosphatase type 2B (PP2B). Active in vivo.
  4. A4535 DL-AP3 Competitive group I metabotropic glutamate receptor antagonist and inhibitor of phosphoserine phosphatase.
  5. A4534 Ceramide A potent modulator of cell proliferation and differentiation. Activates protein phosphatase-1 (PP1) and -2A (PP2A), as well as ceramide-activated protein phosphatase (CAPP) in vitro.
  6. A4533 Calyculin A Potent and selective cell-permeable inhibitor of protein phosphatase 1 (IC50 = 0.3 - 0.7 nM) and protein phosphatase 2A (IC50 = 0.5 - 1 nM). Displays > 10,000,000-fold selectivity over PP2B and PP2C.
  7. A4532 Calcineurin Autoinhibitory Peptide Selective inhibitor of Ca2+-calmodulin-dependent protein phosphatase (calcineurin) (IC50 ~ 10 mM). Does not inhibit PP1, PP2A or CaM kinase II (IC50 > 100 mM).
  8. A4518 UNC 926 hydrochloride Methyl-lysine reader antagonist; binds to the MBT domain of the L3MBTL1 protein (Kd = 3.9 μM). Selectively inhibits, in a dose-dependent manner, the interaction between L3MBTL13XMBT-H4K20me1 in a peptide pull down assay.
  9. A4517 ZM 449829 Potent, selective inhibitor of Janus tyrosine kinase 3 (JAK3) which binds competitively to the JAK3 ATP site. pIC50 values are 6.8, 5.0, 4.7, and < 5.0 for JAK3, EGFR, JAK1 and CDK4 respectively.
  10. A4513 Lestaurtinib Potent JAK2, FLT3 and TrkA inhibitor (IC50 values are 0.9, 3 and < 25 nM respectively) that prevents STAT5 phosphorylation (IC50 = 20 - 30 nM). Exhibits antiproliferative activity in vitro (IC50 = 30 - 100 nM in HEL92.1.7 cells) and is effective against myeloproliferative disorders in vivo.
  11. A4509 PX 12 Competitive, irreversible thioredoxin-1 (Trx-1) inhibitor (Ki = 31 μM) that attenuates expression of HIF-1α, VEGF and iNOS (IC50 values are 7.2, ~10 and 18.1 μM respectively). Exhibits antitumor activity; directly inhibits tubulin polymerization in vitro and decreases tumor microvessel density in vivo.

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