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GSK046

Name: GSK046
Brand: TargetMol
SKU: T8932
Price: 55 USD
Availability: InStock
Rating: 5 (10 reviews)

🥰Excellent

Catalog No. T8932Cas No. 2474876-09-8

Alias iBET-BD2

GSK046 (iBET-BD2) is a potent, selective, and orally active BD2 bromodomain inhibitor of the BET proteins, with IC50 values of 264 nM [BRD2 BD2], 98 nM [BRD3 BD2], 49 nM [BRD4 BD2], and 214 nM [BRDT BD2], respectively. It exhibits immunomodulatory activity.

GSK046

🥰Excellent

Purity: 99.97%

Catalog No. T8932Alias iBET-BD2Cas No. 2474876-09-8

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$55	In Stock	In Stock
5 mg	$129	In Stock	In Stock
10 mg	$223	In Stock	In Stock
25 mg	$496	In Stock	In Stock
50 mg	$795	-	In Stock
100 mg	$1,230	-	In Stock
200 mg	$1,650	-	In Stock
1 mL x 10 mM (in DMSO)	$143	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:99.97%

Resource Download

COA HNMR LCMS

Product Introduction

Bioactivity

Description	GSK046 (iBET-BD2) is a potent, selective, and orally active BD2 bromodomain inhibitor of the BET proteins, with IC50 values of 264 nM [BRD2 BD2], 98 nM [BRD3 BD2], 49 nM [BRD4 BD2], and 214 nM [BRDT BD2], respectively. It exhibits immunomodulatory activity.
Targets&IC50	BRD3 BD2:98 nM (IC50), BRD2 BD2:264 nM (IC50), BRDT BD2:214 nM (IC50), BRD4 BD2:49 nM (IC50)
In vivo	GSK046 (40 mg/kg/QD;?s.c. for 14 days) has immunomodulatory activity.?GSK046 exhibits Cmax (C57BL6 1589, C57B16 2993 ng/mL) and terminal elimination half-lives (C57BL6 1.8, C57B16 1.9 h) following oral administration (C57BL6 10, C57B16 40 mg/kg).?GSK046 exhibits Cmax (mouse 1589, rat 202 ng/mL) and terminal elimination half-lives (mouse 1.8, rat 1.4 h) following oral administration (mouse 10, rat 10 mg/kg)[1].
Synonyms	iBET-BD2

Chemical Properties

Molecular Weight	414.47
Formula	C₂₃H₂₇FN₂O₄
Cas No.	2474876-09-8
Smiles	C[C@H](Oc1cc(cc(F)c1NC(C)=O)C(=O)N[C@H]1CC[C@H](O)CC1)c1ccccc1
Relative Density.	1.26 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: 83.33 mg/mL (201.05 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (7.96 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	2.4127 mL	12.0636 mL	24.1272 mL	120.6360 mL
5 mM	0.4825 mL	2.4127 mL	4.8254 mL	24.1272 mL
10 mM	0.2413 mL	1.2064 mL	2.4127 mL	12.0636 mL
20 mM	0.1206 mL	0.6032 mL	1.2064 mL	6.0318 mL
50 mM	0.0483 mL	0.2413 mL	0.4825 mL	2.4127 mL
100 mM	0.0241 mL	0.1206 mL	0.2413 mL	1.2064 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 mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

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