SGC-CBP30
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
SGC-CBP30是一个选择性的CREBBP和EP300抑制剂，IC50值分别为21和38 nM[1]。
EP300 (E1A结合蛋白p300)由EP300基因编码，在调控细胞生长和分裂，促进细胞成熟并承担专门的功能以及抑制肿瘤细胞的生长方面起重要作用。CREBBP（CREB-结合蛋白）由CREBBP基因编码，参与许多不同转录因子的转录共激活[2]。
参考文献：
[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.
- 1. Te Zhang, Wenjie Xia, et al. "Super-enhancer hijacking LINC01977 promotes malignancy of early-stage lung adenocarcinoma addicted to the canonical TGF-β/SMAD3 pathway." J Hematol Oncol. 2022 Aug 18;15(1):114. PMID: 35982471
- 2. Te Zhang, Xuming Song, et al. "Aberrant super-enhancer landscape reveals core transcriptional regulatory circuitry in lung adenocarcinoma." Oncogenesis. 2020 Oct 17;9(10):92. PMID: 33070167
- 3. 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
- 4. 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
| Storage | Store at 4°C |
| M.Wt | 509.04 |
| Cas No. | 1613695-14-9 |
| Formula | C28H33ClN4O3 |
| Synonyms | SGCCBP30,SGC CBP30 |
| Solubility | ≥20.05 mg/mL in DMSO; ≥25.7 mg/mL in EtOH with ultrasonic; ≥4.67 mg/mL in H2O with ultrasonic |
| Chemical Name | 4-[(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 |
| SDF | Download SDF |
| Canonical SMILES | CC1=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 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 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。溶液形式一般不宜长期储存，请尽快用完。 |
| 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。 |
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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. |
|
| 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 | ||||
质量控制和MSDS
- 批次:
化学结构
相关生物数据
相关生物数据
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