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  3. GSK1379725A

GSK1379725A 

Cat. No.: HY-112398 Purity: 98.06%
Handling Instructions

GSK1379725A is a selective BPTF ligand with a Kd of 2.8 uM, showing no binding activity for Brd4.

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 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

GSK1379725A is a selective BPTF ligand with a Kd of 2.8 uM, showing no binding activity for Brd4[1].

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].

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

Molecular Weight

450.47

Formula

C₂₃H₂₃FN₆O₃

CAS No.
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.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (221.99 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2199 mL 11.0995 mL 22.1990 mL
5 mM 0.4440 mL 2.2199 mL 4.4398 mL
10 mM 0.2220 mL 1.1100 mL 2.2199 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.55 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (5.55 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.55 mM); Clear solution

*All of the co-solvents are provided by MCE.
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

Purity: 98.06%

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Keywords:

GSK1379725AEpigenetic Reader DomainInhibitorinhibitorinhibit

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