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GSK1379725A 

Cat. No.: HY-112398 Purity: >98.0%
Handling Instructions

GSK1379725A is an inhibitor of Brd4 and a selective BPTF ligand (Kd=2.8 μM).

For research use only. We do not sell to patients.

GSK1379725A Chemical Structure

GSK1379725A Chemical Structure

CAS No. : 1802251-00-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 396 In-stock
Estimated Time of Arrival: December 31
5 mg USD 360 In-stock
Estimated Time of Arrival: December 31
10 mg USD 660 Get quote
50 mg   Get quote  
100 mg   Get quote  

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Description

GSK1379725A is an inhibitor of Brd4 and a selective BPTF ligand (Kd=2.8 μM).

In Vitro

From the NMR titration of GSK1379725A, the bound and unbound resonances are separated by 171 Hz, providing an upper bound for the chemical exchange rate. Assuming an association rate of 1×108 M-1 s-1 as a high end for a range of protein-small molecule interactions, (e.g., chymotrypsin: proflavin k1=1.2×108 M-1 s-1), an upper Kd of 8 μM is estimated from this experiment. For a more accurate determination with a non-fluorinated protein, ITC is used as a complementary direct binding assay using unlabeled BPTF. A Kd of 2.8 μM is obtained, consistent with our intermediate exchange resonance broadening by PrOF NMR. Although GSK1379725A has been demonstrated to be selective over Brd4, a full selectivity panel against other bromodomains will be needed. A database search using ChEMBL only showed GSK1379725A to be active in five cellular assays with an EC50 of 500 nM carried out. Additionally, no kinase activity has been reported for GSK1379725A despite the growing screening use of the PKIS library[1].

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
References
Cell Assay
[1]

Cell viability assay of HEK 293 cells are performed using resazurine dye based CellTiter-Blue. HEK 293T cells are plated in 96 well plates and experiments conducted when cells are 80% confluent. Cells are treated with the 0, 1.0, 3.0 and 10.0 μM GSK1379725A (AU1) for 24 and 48 hours in 5% CO2 (n=5-6, per condition). 20 μL of CellTiter-Blue is added to the each well and incubated for 2.5 h at 37°C. As resazurin dye is reduced by viable cells to resorufin. Resorufin is fluorescent at 580 excitation and 590 emission. The data is normalized with the control (DMSO treated)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

450.47

Formula

C₂₃H₂₃FN₆O₃

CAS No.

1802251-00-8

SMILES

O=C(OC)C1=CC=CC(NC(NC2CN(C3=NC(NC4=CC=C(F)C=C4)=NC=C3)CC2)=O)=C1

Shipping

Room temperature in continental US; may vary elsewhere

Purity: >98.0%

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Product Name:
GSK1379725A
Cat. No.:
HY-112398
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GSK1379725A

Cat. No.: HY-112398