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  4. GSK 525768A

GSK 525768A is the inactive enantiomer of GSK525762A. GSK 525768A has no activity towards BET.

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

GSK 525768A Chemical Structure

GSK 525768A Chemical Structure

CAS No. : 1260530-25-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 462 In-stock
Solution
10 mM * 1 mL in DMSO USD 462 In-stock
Solid
5 mg USD 420 In-stock
10 mg USD 678 In-stock
50 mg USD 1850 In-stock
100 mg USD 2520 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of GSK 525768A:

GSK 525768A Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE GSK 525768A

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GSK 525768A is the inactive enantiomer of GSK525762A. GSK 525768A has no activity towards BET.

In Vitro

GSK 525768A has no activity towards BET[1]. GSK 525768A (GSK525768A) is the (R)-enantiomer of GSK525762A. GSK525762A is shown to regulate levels of the high-density lipid protein apolipoprotein A1 (APOA1) in assays monitoring APOA1 release in liver cells, whereas the (R)-enantiomer (GSK 525768A) has no effect. GSK 525768A directly engages the protein module by forming hydrogen bonds with the conserved asparagine residue in a way that mimics the binding mode of acetylated lysine; this usually results in the binding of the inhibitor deeper within the acetylated lysine binding site but without displacing the conserved water molecules that are present at the bottom of the acetyl-lysine binding cavity[2].

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

GSK 525768A Related Antibodies
Molecular Weight

423.90

Formula

C22H22ClN5O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NCC)C[C@@H]1C2=NN=C(C)N2C3=CC=C(OC)C=C3C(C4=CC=C(Cl)C=C4)=N1
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 (235.90 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3590 mL 11.7952 mL 23.5905 mL
5 mM 0.4718 mL 2.3590 mL 4.7181 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
×
Volume
×
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 (5.90 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 (5.90 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 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: 99.62%

COA (255 KB) LCMS (255 KB)

Handling Instructions (2659 KB)
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 2.3590 mL 11.7952 mL 23.5905 mL 58.9762 mL
5 mM 0.4718 mL 2.3590 mL 4.7181 mL 11.7952 mL
10 mM 0.2359 mL 1.1795 mL 2.3590 mL 5.8976 mL
15 mM 0.1573 mL 0.7863 mL 1.5727 mL 3.9317 mL
20 mM 0.1180 mL 0.5898 mL 1.1795 mL 2.9488 mL
25 mM 0.0944 mL 0.4718 mL 0.9436 mL 2.3590 mL
30 mM 0.0786 mL 0.3932 mL 0.7863 mL 1.9659 mL
40 mM 0.0590 mL 0.2949 mL 0.5898 mL 1.4744 mL
50 mM 0.0472 mL 0.2359 mL 0.4718 mL 1.1795 mL
60 mM 0.0393 mL 0.1966 mL 0.3932 mL 0.9829 mL
80 mM 0.0295 mL 0.1474 mL 0.2949 mL 0.7372 mL
100 mM 0.0236 mL 0.1180 mL 0.2359 mL 0.5898 mL
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GSK 525768A 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:

GSK 525768A1260530-25-3OthersInhibitorinhibitorinhibit

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