A p300 acetyltransferase inhibitor
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L002

Item No. 17778

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS(pH 7.2) (1:2): 0.25 mg/mlEthanol: 1 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $90

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    10 mg

    $132

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    25 mg

    $306

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    50 mg

    $567

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    Cayman Chemical
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    Product Description

    L002 is an inhibitor of p300 histone acetyltransferase (KAT3B; IC50 = 1.98 µM in vitro).1 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 STAT3.1 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.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yang, H., Pinello, C.E., Luo, J., et al. Small-molecule inhibitors of acetyltransferase p300 identified by high-throughput screening are potent anticancer agents. Mol. Cancer Ther. 12(5), 610-620 (2013).

    Product Citations

    Kanada, F., Takamura, Y., Miyake, S., et al. Histone acetyltransferase and Polo-like kinase 3 inhibitors prevent rat galactose-induced cataract. Sci. Rep. 9(1), 20085 (2019).