Home Epigenetics p300/CBP inhibitor I-CBP112

research use only

I-CBP112 p300/CBP inhibitor

Cat.No.S6758

I-CBP112 is a potent and selective CBP/p300 inhibitor with dissociation constant (KD) of 151 ± 6 nM and 167 ± 8 nM for CBP and p300, respectively.
I-CBP112 p300/CBP inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 468.59

Jump to

Quality Control

Batch: Purity: 99.33%
99.33

Solubility

In vitro
Batch:

DMSO : 94 mg/mL (200.6 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 94 mg/mL

Ethanol : 94 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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

mg/kg
g
μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO
%
% Tween 80
% ddH2O
% DMSO
+
%

Calculation results:

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.

Chemical Information, Storage & Stability

Molecular Weight 468.59 Formula

C27H36N2O5

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1640282-31-0 -- Storage of Stock Solutions

Synonyms N/A Smiles CCC(=O)N1CCOC2=C(C1)C=C(C=C2OCC3CCCN(C3)C)C4=CC(=C(C=C4)OC)OC

Mechanism of Action

Targets/IC50/Ki
CBP
(Cell-free assay)
151 nM(Kd)
p300
(Cell-free assay)
167 nM(Kd)
In vitro

Exposure of human and mouse leukemic cell lines to I-CBP112 resulted in substantially impaired colony formation and induced cellular differentiation without significant cytotoxicity. This compound significantly reduced the leukemia-initiating potential of MLL-AF9+ AML cells in a dose-dependent manner in vitro and in vivo. It is an acetyl-lysine competitive inhibitor displacing H3K56ac from the CBP binding site with an IC50 value of 170 nM.
References

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.