L002

L002 is an inhibitor of p300 histone acetyltransferase (KAT3B, IC50 = 1.98 µM in vitro). 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. 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.Formal Name: 2,6-dimethyl-2,5-cyclohexadiene-1,4-dione 4-[O-[(4-methoxyphenyl)sulfonyl]oxime]. CAS Number: 321695-57-2. Synonyms: p300/CBP Inhibitor VI, NSC 764414. Molecular Formula: C15H15NO5S. Formula Weight: 321.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS(pH 7.2) (1:2): 0.25 mg/ml, Ethanol: 1 mg/ml. lambdamax: 245, 281 nm. SMILES: COC1=CC=C(S(O/N=C2C=C(C)C(C(C)=C\2)=O)(=O)=O)C=C1. InChi Code: InChI=1S/C15H15NO5S/c1-10-8-12(9-11(2)15(10)17)16-21-22(18,19)14-6-4-13(20-3)5-7-14/h4-9H,1-3H3. InChi Key: VEWFTYOFWIXCIO-UHFFFAOYSA-N.