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. Synonyms: 2,6-dimethyl-2,5-cyclohexadiene-1,4-dione 4-[O-[(4-methoxyphenyl)sulfonyl]oxime] CAS No: 321695-57-2 Molecular Formula: C15H15NO5S Molecular Weight: 321.3 Solubility: DMF (30mg/ml) DMSO (30mg/ml) DMSO:PBS(pH 7.2) (1:2) (0.25mg/ml) Ethanol (1mg/ml) Purity: 98% Form: Supplied as a crystalline solid Storage and Stability: May be stored at 4C. For long-term storage, aliquot and store at 4C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.
Molekulargewicht:
321.3
CAS Nummer:
[321695-57-2]
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