A reversible, cell-permeable pyrazolone p300/CBP HAT inhibitor (Ki = 400 nM), which competes with acetyl-CoA for the p300 Lys-CoA binding pocket. Demonstrates 86% inhibition against p300 at 10 nM. Less than 10% inhibition against serotonin N-acetyltransferase, PCAF, GCN5, Rtt109, Sas, and MOZ HATs in a chemical screening assay. Treatment of C3H 10T1/2 mouse fibroblasts at 25 uM results in an inhibitory effect against basal and TSA-inducible acetylation of histones H3 and H4. Shown to inhibit human cell growth in melanoma and non-small cell-lung cancer cell lines at 10 uM with similar or higher potency than peptide-based bisubstrate p300/CBP HAT inhibitor Lys-CoA-Tat at 25 uM.
Arbor Assays公司成立于2007年，位于密歇根州的安娜堡，公司的三位主创始人均为有多年科研经验的生命和临床科学家。其宗旨是为临床使用的重要生物分子建立高质量的检测和免疫测试产品。在生物领域建立健全的免疫检测和酶活性试剂盒以定量生物分子。
Arbor Assays公司的主要产品包括：
DetectX® Kits
Inhibitors & Activators
AbX® Antibodies & Affinity Resins
Detection Systems
Components & Ancillary Reagents
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