Home Tools
Log in
Cart

GSK1379725A

Catalog No. T15424   CAS 1802251-00-8

GSK1379725A is a selective BPTF ligand (Kd = 2.8 μM).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
GSK1379725A Chemical Structure
GSK1379725A, CAS 1802251-00-8
Pack Size Availability Price/USD Quantity
1 mg In stock $ 112.00
5 mg In stock $ 197.00
10 mg In stock $ 347.00
25 mg In stock $ 589.00
50 mg In stock $ 842.00
100 mg In stock $ 1,160.00
500 mg In stock $ 2,330.00
1 mL * 10 mM (in DMSO) In stock $ 226.00
Bulk Inquiry
Get quote
Select Batch  
Purity: 99.59%
Contact us for more batch information
Biological Description
Chemical Properties
Storage & Solubility Information
Description GSK1379725A is a selective BPTF ligand (Kd = 2.8 μM).
Targets&IC50 BPTF:2.8 μM(Kd)
In vitro GSK1379725A has proven to be selective towards Brd4, though comprehensive evaluation against other bromodomains is necessary. Searches in the ChEMBL database reveal its activity in only five cellular assays, indicating a potency (EC50) of 500 nM, with no kinase activity noted despite extensive screenings, especially with the PKIS library[1]. NMR titration data showed a separation of 171 Hz between bound and unbound resonances of GSK1379725A, suggesting a maximum chemical exchange rate. Based on an assumed high association rate (e.g., similar to chymotrypsin: proflavin at 1.2×108 M-1 s-1), the dissociation constant (Kd) is approximately 8 μM. For more precise Kd measurement, ITC was employed with unlabeled BPTF, yielding a Kd of 2.8 μM, aligning with the observed intermediate exchange resonance broadening detected by PrOF NMR, thus confirming the specificity and binding characteristics of GSK1379725A.
Molecular Weight 450.47
Formula C23H23FN6O3
CAS No. 1802251-00-8

Storage

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

Solubility Information

DMSO: 83.33 mg/mL (184.98 mM), sonification is recommended.

TargetMolReferences and Literature

1. Urick AK, et al. Dual Screening of BPTF and Brd4 Using Protein-Observed Fluorine NMR Uncovers New Bromodomain Probe Molecules. ACS Chem Biol. 2015 Oct 16;10(10):2246-56.

Related compound libraries

This product is contained In the following compound libraries:
Covalent Inhibitor Library Histone Modification Compound Library Epigenetics Compound Library Bioactive Compounds Library Max Bioactive Compound Library

Related Products

Related compounds with same targets
Menin-MLL inhibitor 27 I-BET762 carboxylic acid CBP/p300-IN-21 SMARCA-BD ligand 1 for Protac 653-47 hydrochloride BRD4-BD1-IN-2 FKBP12 PROTAC dTAG-13 MS31 trihydrochloride (2366264-12-0 free base)

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

GSK1379725A 1802251-00-8 Chromatin/Epigenetic Epigenetic Reader Domain inhibit Inhibitor GSK-1379725A inhibitor

 

TargetMol