2. Epigenetics
  3. Epigenetic Reader Domain
  4. GSK1379725A

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

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GSK1379725A Chemical Structure

GSK1379725A Chemical Structure

CAS No. : 1802251-00-8

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Based on 1 publication(s) in Google Scholar

Other Forms of GSK1379725A:

GSK1379725A Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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].

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

GSK1379725A Related Antibodies
Molecular Weight

450.47

Formula

C23H23FN6O3
CAS No.
Appearance

Solid

Color

White to off-white

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (221.99 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.12%

SDS (252 KB)

COA (246 KB) RP-HPLC (245 KB)

Handling Instructions (2659 KB)
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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2199 mL 11.0995 mL 22.1990 mL 55.4976 mL
5 mM 0.4440 mL 2.2199 mL 4.4398 mL 11.0995 mL
10 mM 0.2220 mL 1.1100 mL 2.2199 mL 5.5498 mL
15 mM 0.1480 mL 0.7400 mL 1.4799 mL 3.6998 mL
20 mM 0.1110 mL 0.5550 mL 1.1100 mL 2.7749 mL
25 mM 0.0888 mL 0.4440 mL 0.8880 mL 2.2199 mL
30 mM 0.0740 mL 0.3700 mL 0.7400 mL 1.8499 mL
40 mM 0.0555 mL 0.2775 mL 0.5550 mL 1.3874 mL
50 mM 0.0444 mL 0.2220 mL 0.4440 mL 1.1100 mL
60 mM 0.0370 mL 0.1850 mL 0.3700 mL 0.9250 mL
80 mM 0.0277 mL 0.1387 mL 0.2775 mL 0.6937 mL
100 mM 0.0222 mL 0.1110 mL 0.2220 mL 0.5550 mL
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GSK1379725A Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSK1379725A1802251-00-8Epigenetic Reader DomainInhibitorinhibitorinhibit

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