(S)-1-(imidazo[1,2-a]pyridin-6-yl)ethan-1-amine hydrochloride cas 1259603-82-1

1. Basic Information
· CAS Number: 1259603-82-1
· Chemical Name: (±)-N-(3-((3-(2-(1H-indole-3-yl)ethyl)-1,2,4-oxadiazole-5-yl)methyl)phenyl)benzofuran-2-carboxamide
· Chinese Reference: (±)-N-(3-((3-(2-(1H-indole-3-yl)ethyl)-1,2,4-oxadiazole-5-yl)methyl)phenyl)benzofuran-2-carboxamide
· Molecular Formula: C₂₉H₂₂N₄O₃
· Molecular Weight: 474.51 g/mol
· Alternate Names: SGC-CBP30, CBP30
2. Main Function and Target Sites
SGC-CBP30 is an efficient and selective inhibitor of CREB-binding protein and the EP300 bromodomain.
· Main targets:
· CBP and EP300: These are two highly homologous transcriptional co-activator proteins. They play a crucial role in regulating gene expression by recognizing and binding to acetylated lysine residues on histones through their bromine domains. This process is a key step in "reading" epigenetic signals.
· Mechanism of action:
· SGC-CBP30 can bind to the bromine domains of CBP/EP300 proteins with high affinity, thereby preventing their binding to acetylated histones.
· By inhibiting this interaction, it interferes with the gene transcription program mediated by CBP/EP300, especially those related to inflammation, cell proliferation, and differentiation.
3. Key Features
· High selectivity: Compared to other bromodomain proteins (such as BRD2, BRD3, BRD4, BRDT), SGC-CBP30 exhibits extremely high selectivity towards CBP and EP300 (selectivity exceeding 100 times). This makes it an ideal tool for studying the specific functions of CBP/EP300.
· Cellular activity: It can effectively inhibit the function of CBP/EP300 at the cellular level and reduce the expression of its target genes.
· Research application: As a probe molecule, it is used to explore the role of CBP/EP300 in various physiological and pathological processes.
4. Research and Potential Application Areas
The SGC-CBP30 is mainly used for basic scientific research to elucidate the biological functions of CBP/EP300, and it shows potential therapeutic value in the following areas:
1. Cancer research:
· CBP/EP300 is abnormally active in various cancers (such as leukemia, multiple myeloma, prostate cancer, etc.). SGC-CBP30 is used to study whether inhibiting CBP/EP300 can inhibit the growth and survival of tumor cells.
· It has been proven to be able to inhibit the proliferation of acute myeloid leukemia cells.
2. Immunology and inflammatory diseases:
· CBP/EP300 is an important regulatory factor for the differentiation of T helper cell 17. Th17 cells are closely related to autoimmune diseases (such as multiple sclerosis, rheumatoid arthritis, psoriasis).
· SGC-CBP30 can effectively inhibit the differentiation of Th17 cells in mice and humans, indicating its great potential in treating autoimmune diseases.
3. Fibrosis diseases:
· Studies have shown that CBP/EP300 is involved in the process of tissue fibrosis. SGC-CBP30 is used in preclinical models to explore its anti-fibrotic effect.
4. Basic biological research:
· As a chemical tool for exploring the functions of CBP/EP300 in epigenetics, gene transcription regulation and signal transduction pathways.