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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BA4206 YM-08Summary: YM-08 is an inhibitor that crosses the blood-brain barrier. - BA4278 SangivamycinSummary: Sangivamycin (NSC65346) is a nucleoside analog.
- BA4360 RBN012759Summary: RBN012759 is a potent, selective and orally active inhibitor with values <3nM, 300-fold more selective than for monoPARPs and 1000-fold more selective than for polyPARPs.
- BA4365 iRucaparib-AP6Summary: iRucaparib-AP6 is a highly efficient and specific degrading agent.
- BA4367 BRCA1-IN-2Summary: BRCA1-IN-2 is an inhibitor of protein-protein interactions (PPIs) with cell permeability.
- BA4373 OM-153Summary: OM-153 is a potent, orally active inhibitor.
- BA4376 BasroparibSummary: Basroparib is an inhibitor.
- BA4378 4-MethoxychalconeSummary: 4'-Methoxychalcone regulates adipocyte differentiation through activation.
- BA4379 NMS-P515Summary: NMS-P515 is a potent, orally effective, stereotactic inhibitor.
- BA4380 MSC2504877Summary: MSC2504877 (M2912) is a potent, orally active inhibitor with IC values of 0.0007, 0.0008, and 0.54 μM for TNKS, TNKS2, and PARP1, respectively.