Chromatin/Epigenetics
Epigenetics is the heritable modifications in gene expression that is not associated with changes in DNA sequence. Epigenetic modifications occur mostly on DNA or on the histone octamer. There are several types of epigenetics modifications, DNA methylation by DNA-methyl transferase (DNMT) and covalent modification of histones (e.g. acetylation, methylation, phosphorylation and ubiquitination). Histone acetylation by histone acetyltransferases (HATs) is involved in transcriptional activation, whereas histone deacetylation by histone deacetylases (HDACs) is connected with transcriptional repression. Histone demethylation is associated with lysine-specific demethylase (LSD) and JmjC domain containing histone demethylase (JHDM).
The nucleosome is consisted of four histone proteins (H2A, H2B, H3, and H4), they are primary building block of chromatin. The addition and removal of specific chemical groups refers to as epigenetic marks, it regulates chromatin structure and affects gene expression. Moreover, RNA is intimately involved in the formation of a repressive chromatin state.
Epigenetic mechanism responds to environmental changes at the cellular level and thus influences cellular plasticity. Chromatin and epigenetic regulation play a significant role in the programming of the genome during development and stress response, defects in epigenetics can lead to cancer, inflammation and metabolic disorders etc.
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BA4383 ART-IN-1Summary: An inhibitor. - BA4384 PARP1-IN-11Summary: PARP1-IN-11 is a potent inhibitor.
- BA4385 2-Methylquinazolin-4-olSummary: 2-Methylquinazolin-4-ol is a potent, competitive inhibitor.
- BA4386 PARP1-IN-7Summary: PARP1-IN-7 is an inhibitor.
- BA4387 Tankyrase-IN-2Summary: Tankyrase-IN-2 is a potent and selective inhibitor (values of 10 nM, 7 nM, and 710 nM for TNKS1, TNKS2, respectively).
- BA4388 AmelparibSummary: Amelparib is a potent, orally active, water-soluble inhibitor.
- BA4390 PARP-2-IN-1Summary: PARP-2-IN-1 is a potent and selective inhibitor.
- BA4392 G244-LMSummary: G244-LM is a potent and specific inhibitor.
- BA4393 AZ3391Summary: AZ3391 is a potent inhibitor.
- BA4394 TNKS-2-IN-2Summary: TNKS-2-IN-2 is a potent and selective inhibitor.