321695-57-2

Usage

Uses

Used in Pharmaceutical Industry:
NSC764414 is used as an inhibitor of p300 histone acetyltransferase for its potential in cancer treatment. It modulates the acetylation of histones and p53, reducing STAT3 phosphorylation and inducing growth arrest and apoptosis in certain cancer cell lines.
Used in Cancer Research:
NSC764414 is used as a research tool for studying the role of p300 histone acetyltransferase in various cellular processes, including the acetylation of histones and p53, and its involvement in cancer development and progression.
Used in Drug Development:
NSC764414 is used as a lead compound in the development of novel therapeutics targeting p300 histone acetyltransferase, with potential applications in the treatment of various types of cancer, particularly triple-negative breast cancer.

Biochem/physiol Actions

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.