Home Tools
Log in
Cart

I-CBP112

Catalog No. T3969   CAS 1640282-31-0

I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor targeting the CBP/p300 bromodomains.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
I-CBP112 Chemical Structure
I-CBP112, CAS 1640282-31-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 51.00
2 mg In stock $ 80.00
5 mg In stock $ 163.00
10 mg In stock $ 289.00
25 mg In stock $ 549.00
50 mg In stock $ 789.00
100 mg In stock $ 1,080.00
1 mL * 10 mM (in DMSO) In stock $ 169.00
Bulk Inquiry
Get quote
Select Batch  
Purity: 99.1%
Contact us for more batch information
Biological Description
Chemical Properties
Storage & Solubility Information
Description I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor targeting the CBP/p300 bromodomains.
Targets&IC50 CBP/p300, Prostate cancer cell:9.1±1.2 μM (IC50), CBP/p300, Leukemia cell:5.5±1.1 μM (IC50)
In vitro Exposure to I-CBP112 in human and mouse leukemic cell lines significantly reduces colony formation and initiates cellular differentiation, without notable cytotoxic effects. When primary cells from the BioMAP panel were treated with I-CBP112, it elicited a distinctive cytokine and marker protein expression profile. Importantly, I-CBP112 markedly increases acetylation levels at histone H3K18 and H3K23 sites by p300, tripling H3K18ac levels. This compound not only enhances CBP-mediated acetylation at these locations but also at H4K5. The half-maximal effective concentration (EC50) for I-CBP112's action on p300 and CBP to increase H3K18 acetylation is approximately 2 μM.
In vivo I-CBP112 significantly reduces the leukemia-initiating potential of MLL-AF9+ AML cells in a dose-dependent manner in vitro and in vivo.
Kinase Assay TGase 2 from guinea pig liver is preincubated for 10 min with various concentrations of GK13 or GK921 in 0.1 mL of reaction buffer, with or without 10 mM CaCl2, followed by the addition of 0.4 mL of substrate solution containing 2
Cell Research I-CBP112 is dissolved in DMSO and diluted with appropriate medium before use. Cells (6000 KG1a and 13000 LNCaP cells/well) are plated in 96-well flat-bottom plates approximately 24 h prior to drug treatment. After 24 h, 10–20% fetal bovine serum-containing medium is replaced with 2.5% serum medium, and cells are treated with I-CBP112 in 0.18% DMSO; 0.18% DMSO is shown to have negligible cell growth effects under the conditions used in our experiments. After being exposed to I-CBP112 for 66 h, cells are subjected to a final concentration of 0.476% [3H]thymidine per well and allowed to proliferate for an additional 6 h (exposure to I-CBP112 for a total of 72 h). Cells are harvested, and the counts of 3H in each well are taken relative to those treated with vehicle alone to quantify the effect of the ligand on proliferation[1].
Molecular Weight 468.59
Formula C27H36N2O5
CAS No. 1640282-31-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 55 mg/mL (117.37 mM)

TargetMolReferences and Literature

1. Zucconi BE, et al. Modulation of p300/CBP Acetylation of Nucleosomes by Bromodomain LigandI-CBP112. Biochemistry. 2016 Jul 12;55(27):3727-34. 2. Picaud S, et al. Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy. Cancer Res. 2015 Dec 1;75(23):5106-19.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Hypertension Compound Library PPI Inhibitor Library NO PAINS Compound Library Bioactive Compounds Library Max Chromatin Modification Compound Library Epigenetics Compound Library Bioactive Compound Library Histone Modification Compound Library Hematonosis Compound Library Inhibitor Library

Related Products

Related compounds with same targets
Crebinostat Acetaminophen MOZ-IN-3 CTX-0124143 EML 425 C646 A-485 PF-CBP1 hydrochloride

TargetMolDose Conversion

You can also refer to dose conversion for different animals. More

TargetMol In vivo Formulation Calculator (Clear solution)

Step One: Enter information below
Dosage
mg/kg
Average weight of animals
g
Dosing volume per animal
ul
Number of animals
Step Two: Enter the in vivo formulation
% DMSO
%
% Tween 80
% ddH2O
Calculate Reset

TargetMolCalculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculation
Molecular Weight Calculator
=
X
X

Molarity Calculator allows you to calculate the

  • Mass of a compound required to prepare a solution of known volume and concentration
  • Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Concentration of a solution resulting from a known mass of compound in a specific volume
See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

X
=
X

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

=
/

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

I-CBP112 1640282-31-0 Chromatin/Epigenetic Epigenetic Reader Domain Histone Acetyltransferase Inhibitor HATs I CBP112 inhibit I-CBP 112 HAT ICBP112 I-CBP-112 inhibitor

 

TargetMol