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APExBIO

SGC-CBP30

In stock
Catalog No.
A4491
Inhibitor of CREBBP/EP300 bromodomain,potent
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$150.00
In stock
10mg
$140.00
In stock
50mg
$470.00
In stock

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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.

Product Citation

Chemical Properties

StorageStore at 4°C
M.Wt509.04
Cas No.1613695-14-9
FormulaC28H33ClN4O3
SynonymsSGCCBP30,SGC CBP30
Solubility≥20.05mg/mL in DMSO
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
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Protocol

Cell experiment [1]:

Cell lines

HeLa cells and RKO cells

Preparation method

Limited solubility. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reaction Conditions

37oC

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.

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.

Biological Activity

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        

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