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Powder: -20°C, 3 years.In solvent: -80°C, 6 months; -20°C, 1 month.
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货期：询盘
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MedChemExpress LLC
- CAS号：
1889284-33-6
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5 mg
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CBP/p300-IN-5
CAS No. : 1889284-33-6
MCE 国际站：CBP/p300-IN-5
产品活性：P300/CBP-IN-5 是一种有效的 p300/CBP 组蛋白乙酰转移酶 (histone acetyltransferase) 抑制剂，其 IC50 值为 18.8 nM。详细信息请参考专利文献 WO2016044770A1 中的 Example 715。
研究领域：Epigenetics
作用靶点：Histone Acetyltransferase
In Vitro: P300/CBP-IN-5 inhibits p300 LnCap-FGC cellls proliferation with an IC50 of 14.8 nM. P300/CBP-IN-5 inhibits H3K27Ac with an IC50 value of 4.6 nM in PC-3 cells.
In Vivo: The effect of P300/CBP-IN-5 (Example 715) on tumor growth is evaluated in subcutaneous, SuDHL-8 (B-cell lymphoma) and 22RV1 (prostate) xenograft tumors implanted in SCID female mice. Human cancer cells are inoculated subcutaneously into the right hind flank of female SCID mice on study day 0. Administration of P300/CBP-IN-5 (7.5 mg/kg/day) is initiated at the time of size match. P300/CBP-IN-5 induces significant tumor growth inhibition in multiple xenograft tumor models (the tumor growth inhibition of 62% in SuDHL-8 xenograft tumor model; 48% in 22RV1 xenograft tumor model).
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文献和实验质乙酰化修饰研究进展）目前，对于 p53 的乙酰化修饰已经研究得较为清楚，在 p300/CBP 的催化下，p53 的 C 端 DNA 结合调控区域上发生多个赖氨酸位点的乙酰化修饰，从而激活 p53 上特异 DNA 结合区域的活化。还比如 AP-1，ATF-5，BMAL1，CBP,Cytokeratin，E2F-4,EF-1,HMG-1,Hsp90,Hsp70,ku-70,stat3,Ub,NF-E4,NF-Kb-p65 P73,Nrf2,P300,PTEN,Ref-1 等，修饰后的蛋白质可以对细胞
v468.chapter 1 经典 Wnt/b-Catenin 信号通路 （英文完整版）
represstarget genes by recruiting transcriptional co-repressors (Groucho/TLE) to their promoters and/or enhancers. B Wnt on : interaction of a Wnt ligand with its specific receptor complex containing a Frizzled family member and low-density lipidreceptor (LRP)-5
19734881. ^ Wang XJ, Reyes JL, Chua NH, Gaasterland T (2004). "Prediction and identification of Arabidopsis thaliana microRNAs and their mRNA targets". Genome Biol. 5 (9): R65. doi:10.1186/gb-2004-5-9-r65. PMC 522872. PMID 15345049. http://genomebiology
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