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经验配方 C₂₄H₁₉N₃O₆ 描述 概述 A reversible, cell-permeable pyrazolone p300/CBP HAT inhibitor (Ki = 400 nM), which competes with acetyl-CoA for the p300 Lys-CoA binding pocket. This compound demonstrates 86% inhibition against p300 at 10 nM, but elicits less than 10% inhibition against serotonin N-acetyltransferase, PCAF histone acetyltransferase, GCN5 histone acetyletransferase, Rtt109 histone acetyletransferase, Sas histone acetyl transferase, and MOZ histone acetyltransferase in a chemical screening assay. Treatment of C3H 10T1/2 mouse fibroblasts with 25 µM of compound results in an inhibitory effect against basal and TSA-inducible acetylation of histones H3 and H4. It is also shown to inhibit human cell growth in both melanoma and non-small-cell-lung (NSCL) cancer cell lines at 10 µM with similar or higher potency compared with that of the peptide-based bisubstrate p300/CBP HAT inhibitor Lys-CoA-Tat at 25 µM. 产品目录编号 382113 品牌系列 Calbiochem®
同义词 4-(4-{[5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl]methylidene}-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid, p300/CBP Inhibitor IV, Histone Acetyltransferase Inhibitor V, HAT Inhibitor V 参考 参考 Bowers, EM., et al. 2010. Chem Biol 17, 471. 产品信息 形式 Brick red solid Hill配方 C₂₄H₁₉N₃O₆ 化学配方 C₂₄H₁₉N₃O₆ Molar Mass 445.42 结构配方图像 生物信息 纯度 ≥99% by HPLC (sum of isomers) 理化信息 溶解度 DMSO 储存和货运信息 货运代码 Shipped with Blue Ice or with Dry Ice
毒性 Standard Handling
储存 -20°C
避光 Protect from light
无需冷冻 No
特殊指南 Following reconstitution, aliquot and freeze (-20°C. Stock solutions are stable for up to 3 months at -20°C. 包装信息 惰性气体下包装 Packaged under inert gas
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