SML0759

L002

≥98% (HPLC)

• Sinônimo(s): 4-[O-[(4-Methoxyphenyl)sulfonyl]oxime]-2,6-dimethyl-2,5-cyclohexadiene-1,4-dione, NSC764414
• Fórmula empírica (Notação de Hill): C₁₅H₁₅NO₅S
• Número CAS: 321695-57-2
• Peso molecular: 321.35
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Ensaio: ≥98% (HPLC)
• Formulário: powder
• cor: white to beige
• solubilidade: DMSO: 20 mg/mL, clear
• temperatura de armazenamento: 2-8°C
• cadeia de caracteres SMILES: [S](=O)(=O)(ON=C2C=C(C(=O)C(=C2)C)C)c1ccc(cc1)OC
• 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
• chave InChI: VEWFTYOFWIXCIO-UHFFFAOYSA-N

Descrição

Ações bioquímicas/fisiológicas

L002 (NSC764414) is an inhibitor of acetyltransferase p300, a lysine acetyltransferase that catalyzes acetyl group attachment to lysine residues of a variety of proteins including histones and p53, and acts as a critical coactivator of several oncogenic transcription factors involved in cancer cell survival and proliferation including STAT3, NF-kB, and hypoxia-inducible factor-1α (HIF-1α). L002 (NSC764414) was discovered from compounds assayed for cytotoxicity to the triple-negative breast cancer (TNBC) cell line MDA-MB-231 but not to the human mammary epithelial cells, then further screened for inhibition of p300. L002 has an in vitro IC₅₀ of 1.98 μM for p300 with lesser inhibition of the GNAT (GCN5-related N-acetyltransferase) family, and no inhibition against the MYST family of histone acetyltransferases (HATs), histone deacetylases (HDACs), or histone methyltransferases (HMTs). L002 potently suppressed tumor growth and histone acetylation of MDA-MB-468 xenografts and leukemia and lymphoma cell lines.

L002 (NSC764414) is an inhibitor of acetyltransferase p300.

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable