SGC-CBP30
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.
- 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 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
HeLa cells and RKO cells |
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Preparation method |
Limited solubility. General tips for obtaining a higher concentration: Please warm the tube at 37°C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months. |
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Reaction Conditions |
37°C |
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Applications |
In HeLa cells, treatment of SAHA-treated cells with 0.1 μM SGC-CBP30 reduces FRAP recovery times back to unstimulated levels. In RKO cells, SGC-CBP30 effectively inhibits the Doxorubicin induced p53 activity in a dose-dependent manner. |
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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. |
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| Description | SGC-CBP30 is a potent inhibitor of CREBBP/EP300 with IC50 values of 21 nM and 38 nM, respectively. | |||||
| Targets | CREBBP | EP300 | ||||
| IC50 | 21 nM | 38 nM | ||||
Quality Control & MSDS
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