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SGC-CBP30

现货
Catalog No.
A4491
CREBBP/EP300 bromodomain抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,500.00
现货
10mg
¥ 1,400.00
现货
50mg
¥ 4,700.00
现货

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Background

SGC-CBP 30 is a selective inhibitor of CREBBP and EP300 with IC50 value of 21 nM and 38 nM, respectively [1].
EP300 (E1A binding protein p300) is encoded by EP300 gene and plays an important role in regulating cell growth and division, prompting cells mature and assume specialized functions, and preventing tumor cells growth. CREBBP (CREB-binding protein) is encoded by CREBBP gene and involves in the transcriptional coactivation of many different transcription factors [2].
References:
[1]. Duncan A. Hay, Oleg Fedorov, Sarah Martin, et al. Discovery and Optimization of Small-Molecule Ligands for the CBP/p300 Bromodomains [J]. J. Am. Chem. Soc., 2014, 136 (26), pp 9308–9319.
[2]. van Belzen M, Bartsch O, Lacombe D, et al. Rubinstein-Taybi syndrome (CREBBP, EP300) [J]. Eur J Hum Genet. 2011 Jan; 19(1):preceeding 118-20.

文献引用

1. Li N, Yang L, et al. "BET bromodomain inhibitor JQ1 preferentially suppresses EBV-positive nasopharyngeal carcinoma cells partially through repressing c-Myc." Cell Death Dis. 2018 Jul 9;9(7):761. PMID:29988031
2. Alonso, Victoria Lucia, et al. "Overexpression of bromodomain factor 3 in Trypanosoma cruzi (TcBDF3) affects differentiation of the parasite and protects it against bromodomain inhibitors." FEBS Journal (2016). PMID:27007774

Chemical Properties

StorageStore at 4°C
M.Wt509.04
Cas No.1613695-14-9
FormulaC28H33ClN4O3
SynonymsSGCCBP30,SGC CBP30
Solubility≥20.05mg/mL in DMSO, ≥25.7 mg/mL in EtOH with ultrasonic, ≥4.67 mg/mL in H2O with ultrasonic
Chemical Name4-[(2S)-1-[2-[2-(3-chloro-4-methoxyphenyl)ethyl]-5-(3,5-dimethyl-1,2-oxazol-4-yl)benzimidazol-1-yl]propan-2-yl]morpholine
SDFDownload SDF
Canonical SMILESCC1=C(C(=NO1)C)C2=CC3=C(C=C2)N(C(=N3)CCC4=CC(=C(C=C4)OC)Cl)CC(C)N5CCOCC5
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

HeLa和RKO细胞

制备方法

溶解度有限。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。

反应条件

37℃

实验结果

在SAHA处理的HeLa细胞中,0.1 μM SGC-CBP30将FRAP恢复时间降至未刺激的水平。在RKO细胞中,SGC-CBP30以剂量依赖性方式有效抑制Doxorubicin诱导的p53活性。

References:

1. Hay DA, Fedorov O, Martin S et al. Discovery and optimization of small-molecule ligands for the CBP/p300 bromodomains. J Am Chem Soc. 2014 Jul 2;136(26):9308-19.

生物活性

描述 SGC-CBP30是一种有效的CREBBP和EP300抑制剂,IC50值分别为21和38 nM。
靶点 CREBBP EP300        
IC50 21 nM 38 nM        

质量控制

化学结构

SGC-CBP30

相关生物数据

SGC-CBP30

相关生物数据

SGC-CBP30

相关生物数据

SGC-CBP30