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
- Aurora Kinase(35)
- DNA Methyltransferase(14)
- Histone Acetyltransferases(21)
- Histone Demethylases(33)
- Histone Methyltransferase(53)
- MBT Domains(1)
- Protein Ser/Thr Phosphatases(34)
- RNA Polymerase(7)
- Sphingosine Kinase-2(1)
- Polycomb repressive complex(2)
- Cat.No. Product Name Information
- 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.
- 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.
- 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.
Tubacin is a potent, selective, reversible, and cell-permeable inhibitor of HDAC6 with an IC50 value of 4 nM.
- A3821 SRT2104 (GSK2245840) 6-phenylimidazo[2,1-b]thiazole derivatives; sirtuin modulator.
- 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.
LKB1 (AAK1 dual inhibitor)
LKB1 is a selective inhibitor of Pim-1 kinase with Kd value of 35 nM .
- 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).
- 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).
- 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 .