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PF-CBP1

Name: PF-CBP1
Brand: TargetMol
SKU: T3973
Price: 29 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T3973Cas No. 1962928-21-7

PF-CBP1 HCl is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP). It inhibits CREBBP (IC50: 125 nM) and p300 bromodomains (IC50: 363 nM).

PF-CBP1

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Purity: 99.45%

Catalog No. T3973Cas No. 1962928-21-7

PF-CBP1 HCl is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP). It inhibits CREBBP (IC50: 125 nM) and p300 bromodomains (IC50: 363 nM).

Pack Size	Price	USA Warehouse	Global Warehouse
10 mg	$46	In Stock	In Stock
25 mg	$91	In Stock	In Stock
50 mg	$165	In Stock	In Stock
100 mg	$243	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$29	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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Purity:99.45%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	PF-CBP1 HCl is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP). It inhibits CREBBP (IC50: 125 nM) and p300 bromodomains (IC50: 363 nM).
Targets&IC50	CREBBP:125 nM, p300 BD:363 nM
In vitro	PF-CBP1 modulates key inflammatory genes in primary macrophages, downregulates RGS4 in neurons (a target linked to Parkinson's disease), and exhibits 139-fold selectivity over BRD4 in biochemical assays and >105-fold selectivity by ITC. PF-CBP1 is a potent EP300 inhibitor with no cytotoxicity in macrophages and no hepatotoxicity in cell-based models at non-toxic concentrations.
Cell Research	Cells are pretreated with the probes PF-CBP1, ISOX-INACT, or ISOX-DUAL starting at 10 μM concentrations, and then serially diluted to 0.1 μM. After 30 min, the cells are treated with LPS to induce gene transcription and the expression levels of interleukin-6 (IL-6), IL-1β, and interferon-β (IFN-β)(which are known to be induced after 4 h of LPS exposure) are analyzed by RT-PCR. Probe PF-CBP1 moderately reduces LPS-induced IL-6 and IFN-β expression at 10 μM, and a decrease in IL-1β expression is evident at 3 μM. (Only for Reference)

Chemical Properties

Molecular Weight	488.62
Formula	C₂₉H₃₆N₄O₃
Cas No.	1962928-21-7
Smiles	C(CN1CCOCC1)N2C=3C(N=C2CCC4=CC=C(OCCC)C=C4)=CC(=CC3)C=5C(C)=NOC5C
Relative Density.	1.20 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: 50 mg/mL (102.33 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0466 mL	10.2329 mL	20.4658 mL	102.3290 mL
5 mM	0.4093 mL	2.0466 mL	4.0932 mL	20.4658 mL
10 mM	0.2047 mL	1.0233 mL	2.0466 mL	10.2329 mL
20 mM	0.1023 mL	0.5116 mL	1.0233 mL	5.1165 mL
50 mM	0.0409 mL	0.2047 mL	0.4093 mL	2.0466 mL
100 mM	0.0205 mL	0.1023 mL	0.2047 mL	1.0233 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