An inhibitor of p300 histone acetyltransferase (KAT3B; IC50 = 1.98 µM in vitro); blocks acetylation of histones and p53 in cells treated with trichostatin A or etoposide

L002 – 5 mg

Brand:
Cayman
CAS:
321695-57-2
Storage:
-20
UN-No:
Non-Hazardous - /

L002 is an inhibitor of p300 histone acetyltransferase (KAT3B; IC50 = 1.98 µM in vitro).{29008} It has weaker inhibitory effects against PCAF and GCN5 (IC50s = 35 and 34 µM, respectively) and is specific for p300 over a panel of additional acetyltransferases, deacetylases, and methyltransferases. L002 blocks acetylation of histones and p53 in cells treated with trichostatin A or etoposide, respectively, and reduces STAT3 phosphorylation, which requires p300-mediated acetylation of STAT3.{29008} It induces growth arrest and apoptosis in certain cancer cell lines and, when administered intraperitoneally in mice, suppresses the growth of triple-negative breast cancer xenografts.{29008}  

 

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Description

An inhibitor of p300 histone acetyltransferase (KAT3B; IC50 = 1.98 µM in vitro); blocks acetylation of histones and p53 in cells treated with trichostatin A or etoposide, respectively, and reduces STAT3 phosphorylation

Formal name: 2,6-dimethyl-2,5-cyclohexadiene-1,4-dione 4-[O-[(4-methoxyphenyl)sulfonyl]oxime]

Synonyms:  ​NSC 764414|p300/CBP Inhibitor VI

Molecular weight: 321.3

CAS: 321695-57-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Acetyltransferases||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|JAK/STAT Signaling||Research Area|Cancer|Transcription Factors|STATs||Research Area|Epigenetics, Transcription, & Translation|Writers|Histone Acetylation

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