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CPTH2 is a histone acetyltransferase (HAT) inhibitor modulating the Gcn5 network. Histone Acetyltransferase (HAT) inhibitor modulating Gcn5 network. Histone acetyltransferases (HATs) act as transcriptional coactivators. Histone acetylation plays an important role in regulating the chromatin structure and is tightly regulated by two classes of enzyme, histone acetyltransferases (HAT) and histone deacetylases (HDAC). Deregulated HAT and HDAC activity plays a role in the development of a range of cancers. Consequently, inhibitors of these enzymes have potential as anticancer agents.
| Molecular Weight | 291.8 |
| Formula | C14H14ClN3S |
| CAS Number | 357649-93-5 |
| Solubility (25°C) | DMSO: ≥10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[3] Claudia Canzonetta, et al. SAGA complex and Gcn5 are necessary for respiration in budding yeast
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Curcumin (Diferuloyl), a natural phenolic compound, is a p300/CREB binding protein specific inhibitor that inhibits histone/non-histone acetylation and histone acetyltransferase-dependent chromatin transcription. Curcumin inhibited NF-κ B and MAPKs, and had anti-inflammatory, antioxidant, anti-proliferation and anti-angiogenesis effects. Curcumin induces Nrf2 protein stabilization through Keap1 cysteine modification. |
| C646
C646 is a selective inhibitor for histone acetyltransferase, and inhibits p300 with a Ki of 400 nM. C646 preferentially selective for p300 versus other acetyltransferases. |
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MG149 is a selective and potent Tip60 inhibitor with IC50 of 74 uM, similar potentcy for MOF (IC50= 47 uM); little potent for PCAF and p300 (IC50 >200 uM). MG 149 inhibits KAT8 and blocks PINK1 kinase activity. MG 149 can induce mitochondrial depolarization and promote PINK1 dependent mitochondrial clearance. |
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Histone Acetyltransferase Inhibitor II, insulin producing cells capable of secreting blood glucose regulating hormones, specially insulin, in response to physiological signals, method of production of said cells and uses thereof. |
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