Home Epigenetics Epigenetic Reader Domain inhibitor - Histone Acetyltransferase inhibitor SGC-CBP30 For research use only.

SGC-CBP30

SGC-CBP30 is a potent CREBBP/EP300 inhibitor with IC50 of 21 nM and 38 nM in cell-free assays, respectively. Exhibits 40-fold and 250-fold selectivity for CBP over the first BRD of BRD4 (BRD4(1)) and BRD4(2) respectively.

SGC-CBP30 Chemical Structure

SGC-CBP30 Chemical Structure

CAS No. 1613695-14-9

Purity & Quality Control

SGC-CBP30 Related Products

Signaling Pathway

Epigenetic Reader Domain Signaling Pathways

Epigenetic Reader Domain Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
RKO Function assay 24 hrs Inhibition of doxorubicin-stimulated p53 (unknown origin) expressed in human RKO cells preincubated for 24 hrs followed by addition of doxorubicin for 16 hrs by luciferase reporter assay, IC50 = 1.5 μM. 26572217
AMO1 Function assay 6 hrs Inhibition of CBP/EP300 in human AMO1 cells assessed as reduction in MYC expression after 6 hrs by quantigene plex assay, EC50 = 2.7 μM. 27190605
HEK293 Function assay Inhibition of Halo-tagged histone H3.3 binding to NanoLuc luciferase conjugated CBP (unknown origin) expressed in HEK293 cells after overnight incubation by BRET assay, IC50 = 2.8 μM. 27682507
RKO Function assay 24 hrs Inhibition of p53-induced (unknown origin) expressed in human RKO cells assessed as reduction in p53-induced p21 activation measured after 24 hrs by luciferase reporter gene assay, IC50 = 1.54 μM. ChEMBL
Click to View More Cell Line Experimental Data

Biological Activity

Description SGC-CBP30 is a potent CREBBP/EP300 inhibitor with IC50 of 21 nM and 38 nM in cell-free assays, respectively. Exhibits 40-fold and 250-fold selectivity for CBP over the first BRD of BRD4 (BRD4(1)) and BRD4(2) respectively.
Features CREBBP/EP300-selective chemical probe.
Targets
CREBBP [1]
(Cell-free assay)		 EP300 [1]
(Cell-free assay)
21 nM 38 nM
In vitro
In vitro

As a CREBBP/EP300-selective chemical probe, SGC-CBP30 shows moderate cytotoxicity in U2OS cells and HeLa cells. [1]
Cell Research Cell lines COLO-320-HSR cells
Concentrations 20 μM
Incubation Time 6 h
Method

Cells were then treated for 6 hours with 20μM SGC-SCP30 or DMSO.
Experimental Result Images Methods Biomarkers Images PMID
Western blot IKZF1 / IKZF3 / p-STAT3 / STAT3 / IRF4 / Myc 30741931
Growth inhibition assay Cell viability 30741931

Chemical Information & Solubility

Molecular Weight 509.04 Formula

C28H33ClN4O3
CAS No. 1613695-14-9 SDF Download SGC-CBP30 SDF
Smiles CC1=C(C(=NO1)C)C2=CC3=C(C=C2)N(C(=N3)CCC4=CC(=C(C=C4)OC)Cl)CC(C)N5CCOCC5
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (196.44 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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% DMSO % % Tween 80 % ddH2O
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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
The recommend formulation of SGC-CBP30 (Cat S7256) for in vivo studies on your website is “2% DMSO+30% PEG 300+5% Tween 80+ddH2O”. Is this a suspension or clear solution?

Answer:
S7256 SGC-CBP30 in 2% DMSO+30% PEG 300+5% Tween 80+ddH2O at 5mg/ml is a clear solution.

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