SET domain-containing protein 8 (SET8) is a methyltransferase that selectively mono-methylates histone H4 at lysine residue 20, an event proven to have an important role in chromatin structure and transcriptional activation. It is also a regulator of p53, mono-methylating lysine 382 of the tumor suppressor. UNC0379 is a substrate-competitive inhibitor of the lysine methyltransferase SET8 (IC50 = 7.3 µM; Kd = 18.3 µM).{26523} It is selective for SET8 over 15 other methyltransferases, including G9a and GLP (IC50s = >100 µM).{26523}
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A selective inhibitor of the lysine methyltransferase SET8 (IC50 = 7.3 µM; Kd = 18.3 µM)
Formal name: 6,7-dimethoxy-2-(1-pyrrolidinyl)-N-[5-(1-pyrrolidinyl)pentyl]-4-quinazolinamine
Synonyms:
Molecular weight: 413.6
CAS: 1620401-82-2
Purity: ≥95%
Formulation: A crystalline solid
Product Type|Biochemicals|Small Molecule Inhibitors|Methyltransferases||Research Area|Epigenetics, Transcription, & Translation|Writers|Histone Methylation
The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}
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The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}
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