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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. A4508 ML 228 HIF pathway activator (EC50 values are 1.23 and 1.4 μM for HRE gene reporter assay and HIF-1α nuclear translocation assay respectively); acts via chelation of iron, independently of PHD. Also exhibits > 80% inhibition of the human A3 receptor, dopamine transporter, μ receptor, hERG and 5-HT2B receptor, and rat sodium channel site 2, at a concentration of 10 μM.
  3. A4507 KC7F2 Inhibitor of HIF-1α. Thought to act via down-regulation of HIF-1α protein synthesis; reduces phosphorylation of eIF4E binding protein 1 (4EBP1) and p70 S6K in hypoxic conditions. Also blocks hypoxia-induced HIF-1α accumulation in a range of human cancer cell lines. Inhibits the expression of HIF target genes, such as carbonic anhydrase IX and MMP2.
  4. A4505 Chetomin Chetomin, an antibiotic metabolite of chaetomium cochliodes, is an inhibitor of HIF-1 by weaken transcription of HIF-1 and recently is raised interests as a cancer chemotherapeutic agent.[1]
  5. A4501 Tubacin

    Tubacin is a potent, selective, reversible, and cell-permeable inhibitor of HDAC6 with an IC50 value of 4 nM.

  6. A3821 SRT2104 (GSK2245840) 6-phenylimidazo[2,1-b]thiazole derivatives; sirtuin modulator.
  7. A3760 Reversine Reversine, a small synthetic purine analogue (2,6-disubstituted purine), has been shown to be effective in tumor suppression. These effects of reversine are due to the inhibition of Aurora A and B.
  8. A3556 LKB1 (AAK1 dual inhibitor)

    LKB1 is a selective inhibitor of Pim-1 kinase with Kd value of 35 nM [1].

  9. A3338 CX-6258 hydrochloride hydrate CX-6258 is a potent, orally efficacious pan-Pim kinases Inhibitor with excellent biochemical potency and kinase selectivity. in vitro: CX-6258 inhibited Flt-3 and Pim-3 (IC50=0.134 and 0.016 uM). At 0.5 uM of CX-6258, only Pim-1, Pim-2, Pim-3, and Flt-3 of the 107 kinases tested were inhibited by more than 80%, showing excellent selectivity. CX-6258 was also shown to be a reversible inhibitor of Pim-1 (Ki=0.005 uM).
  10. A3337 CX-6258 CX-6258 is a potent, orally efficacious pan-Pim kinases Inhibitor with excellent biochemical potency and kinase selectivity. in vitro: CX-6258 inhibited Flt-3 and Pim-3 (IC50=0.134 and 0.016 uM). At 0.5 uM of CX-6258, only Pim-1, Pim-2, Pim-3, and Flt-3 of the 107 kinases tested were inhibited by more than 80%, showing excellent selectivity. CX-6258 was also shown to be a reversible inhibitor of Pim-1 (Ki=0.005 uM).
  11. A3214 AZD1152 AZD1152 is a highly selective inhibitor of Aurora kinases with IC50 values of 1.37 μM and 0.37 nM for Aurora A and Aurora B, respectively [1].

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