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Tocris/SGC-CBP30/4889/10/10 mg

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货号: 4889/10

品牌: Tocris

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Description: Potent CBP/p300 BRD inhibitor

Chemical Name: 2-[2-(3-Chloro-4-methoxyphenyl)ethyl]-5-(dimethyl-1,2-oxazol-4-yl)-1-[(2S)-2-(morpholin-4-yl)propyl]-1H-1,3-benzodiazole

Purity: ≥98% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Potent CBP/p300 bromodomain (BRD) inhibitor (K_d values are 21 and 32 nM for CBP and p300 BRDs respectively). Exhibits 40-fold and 250-fold selectivity for CBP over the first BRD of BRD4 (BRD4(1)) and BRD4(2) respectively. Accelerates FRAP recovery in cells at a concentration of 1 μM.

Licensing Information

This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the SGC-CBP30 probe summary on the SGC website.

External Portal Information

Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of SGC-CBP30 is reviewed on the chemical probes website.

Compound Libraries

SGC-CBP30 is also offered as part of the Tocriscreen Plus and Tocriscreen Epigenetics Toolbox. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	509.04
Formula	C₂₈H₃₃ClN₄O₃
Storage	Store at +4°C
Purity	≥98% (HPLC)
PubChem ID	72201027
InChI Key	GEPYBHCJBORHCE-SFHVURJKSA-N
Smiles	CC1=C(C(C)=NO1)C2=CC=C3C(N=C(CCC4=CC(Cl)=C(OC)C=C4)N3C[C@@H](N5CCOCC5)C)=C2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solubility	Soluble to 100 mM in DMSO and to 100 mM in ethanol

Solubility

Soluble to 100 mM in DMSO and to 100 mM in ethanol

Preparing Stock Solutions

The following data is based on the product molecular weight 509.04. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.96 mL	9.82 mL	19.64 mL
5 mM	0.39 mL	1.96 mL	3.93 mL
10 mM	0.2 mL	0.98 mL	1.96 mL
50 mM	0.04 mL	0.2 mL	0.39 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Gallenkamp et al (2014) Bromodomains and their pharmacological inhibitors. ChemMedChem 9 438 PMID: 24497428

Hay et al (2014) Discovery and optimization of small-molecule ligands for the CBP/p300 bromodomains. J.Am.Chem.Soc. 136 9308 PMID: 24946055

Hammitzsch et al (2015) CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses. Proc.Natl.Acad.Sci.U.S.A. 112 10768 PMID: 26261308

Keywords: SGC-CBP30, supplier, SGCCBP30, CREBBP, CBP, EP300, p300, bromodomains, inhibitors, inhibits, chemical, probes, epigenetics, SGC, potent, selective, active, in, cells, permeable, structural, genomics, consortium, Bromodomains, Histone, Acetyltransferases, Bromodomains, Tocris Bioscience

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