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
- 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.
- 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.
- A4535 DL-AP3 Competitive group I metabotropic glutamate receptor antagonist and inhibitor of phosphoserine phosphatase.
- 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.
- 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.
- 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).
- 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.
- 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.
- 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.
- 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.