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I-CBP112

Name: I-CBP112
Brand: TargetMol
SKU: T3969
Price: 29 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T3969Cas No. 1640282-31-0

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

I-CBP112

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Purity: 98.18%

Catalog No. T3969Cas No. 1640282-31-0

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

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$29	In Stock	In Stock
2 mg	$48	In Stock	In Stock
5 mg	$98	In Stock	In Stock
10 mg	$173	In Stock	In Stock
25 mg	$329	In Stock	In Stock
50 mg	$473	In Stock	In Stock
100 mg	$648	-	In Stock
200 mg	$873	-	In Stock
1 mL x 10 mM (in DMSO)	$98	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:98.18%

Appearance:Viscous

Color:Yellow

Resource Download

COA HPLC HNMR LCMS

Product Introduction

Bioactivity

Description	I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor targeting the CBP/p300 bromodomains.
Targets&IC50	CBP-p300 (Leukemia cells):5.5±1.1 μM (IC50), CBP-p300 (Prostate cancer cells):9.1±1.2 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 markedly diminishes the leukemia-initiating potential of MLL-AF9+ AML cells in a dose-dependent manner [both 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].

Chemical Properties

Molecular Weight	468.59
Formula	C₂₇H₃₆N₂O₅
Cas No.	1640282-31-0
Smiles	CCC(=O)N1CCOc2c(C1)cc(cc2OC[C@H]1CCCN(C)C1)-c1ccc(OC)c(OC)c1
Relative Density.	1.129 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 55 mg/mL (117.37 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.27 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1341 mL	10.6703 mL	21.3406 mL	106.7031 mL
5 mM	0.4268 mL	2.1341 mL	4.2681 mL	21.3406 mL
10 mM	0.2134 mL	1.0670 mL	2.1341 mL	10.6703 mL
20 mM	0.1067 mL	0.5335 mL	1.0670 mL	5.3352 mL
50 mM	0.0427 mL	0.2134 mL	0.4268 mL	2.1341 mL
100 mM	0.0213 mL	0.1067 mL	0.2134 mL	1.0670 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

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

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