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GNE-272

Name: GNE-272
Brand: TargetMol
SKU: T15400
Price: 107 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T15400Cas No. 1936428-93-1

GNE-272 is a potent and highly selective inhibitor of the CBP/EP300 bromodomains. This product inhibits CBP and EP300 with IC50 values of 0.02 μM and 0.03 μM, respectively, exhibiting 650-fold selectivity over BRD4 (IC50 = 13 μM). In cell-based assays, it effectively inhibits MYC expression (EC50 = 0.91 μM) without significant off-target activity against various kinases, receptors, or cytochrome P450 isoforms. As a selective in vivo probe, GNE-272 serves as a vital pharmacological tool for studying CBP/EP300 functions in acute myeloid leukemia (AML) and other cancers.

GNE-272

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Catalog No. T15400Cas No. 1936428-93-1

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$107	-	In Stock
25 mg	$728	6-8 weeks	6-8 weeks
50 mg	$946	6-8 weeks	6-8 weeks
100 mg	$1,490	6-8 weeks	6-8 weeks

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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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Appearance:Solid

Color:White

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Product Introduction

Bioactivity

Description	GNE-272 is a potent and highly selective inhibitor of the CBP/EP300 bromodomains. This product inhibits CBP and EP300 with IC50 values of 0.02 μM and 0.03 μM, respectively, exhibiting 650-fold selectivity over BRD4 (IC50 = 13 μM). In cell-based assays, it effectively inhibits MYC expression (EC50 = 0.91 μM) without significant off-target activity against various kinases, receptors, or cytochrome P450 isoforms. As a selective in vivo probe, GNE-272 serves as a vital pharmacological tool for studying CBP/EP300 functions in acute myeloid leukemia (AML) and other cancers.
Targets&IC50	BRD4:13 μM, CBP:0.02 μM, EP300:0.03 μM
In vitro	In biochemical assays, GNE-272 demonstrates high potency against CBP (IC50 = 0.02 μM) and EP300 (IC50 = 0.03 μM) with excellent selectivity over BRD4. In cell-based target engagement assays, the compound inhibits MYC expression in MV4-11 cells with an EC50 of 0.91 μM and shows a favorable safety profile in screenings against 35 kinases and 42 receptor off-targets [1]
In vivo	In pharmacological studies using mouse models, GNE-272 exhibited low clearance (1 mg/kg, i.v.) and good oral bioavailability at 100 mg/kg, reaching an unbound Cmax of 26 μM; systemically administered GNE-272 significantly modulated MYC expression in vivo, which correlated with potent anti-proliferative and anti-tumor activity in AML tumor xenograft models [1].

Chemical Properties

Molecular Weight	424.47
Formula	C₂₂H₂₅FN₆O₂
Cas No.	1936428-93-1
Smiles	N(C=1C2=C(N(N1)[C@H]3CCOC3)CCN(C(C)=O)C2)C4=C(F)C=C(C=C4)C5=CN(C)N=C5
Relative Density.	1.43 g/cm3 (Predicted)

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 80 mg/mL (188.47 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2.4 mg/mL (5.65 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	2.3559 mL	11.7794 mL	23.5588 mL	117.7940 mL
5 mM	0.4712 mL	2.3559 mL	4.7118 mL	23.5588 mL
10 mM	0.2356 mL	1.1779 mL	2.3559 mL	11.7794 mL
20 mM	0.1178 mL	0.5890 mL	1.1779 mL	5.8897 mL
50 mM	0.0471 mL	0.2356 mL	0.4712 mL	2.3559 mL
100 mM	0.0236 mL	0.1178 mL	0.2356 mL	1.1779 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

Keywords

GNE-272GNE272GNE 272EpigeneticReaderDomainEpigenetic Reader DomainEP300CBPBRD4