2. Epigenetics
  3. Epigenetic Reader Domain
  4. GSK761

GSK761 is a selective inhibitor of speckled 140 kDa (SP140) with an IC50 value of 77.79 nM. GSK761 reduces monocyte-to-inflammatory macrophage differentiation and lipopolysaccharide (LPS)-induced inflammatory activation. GSK761 induces the production of CD206+ regulatory macrophages by inhibiting SP140.

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GSK761 Chemical Structure

GSK761 Chemical Structure

Size Price Stock Quantity
5 mg USD 380 In-stock
10 mg USD 600 In-stock
25 mg USD 1150 In-stock
50 mg USD 1800 In-stock
100 mg USD 2850 In-stock
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Based on 1 publication(s) in Google Scholar

GSK761 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

GSK761 is a selective inhibitor of speckled 140 kDa (SP140) with an IC50 value of 77.79 nM. GSK761 reduces monocyte-to-inflammatory macrophage differentiation and lipopolysaccharide (LPS)-induced inflammatory activation. GSK761 induces the production of CD206+ regulatory macrophages by inhibiting SP140[1].

IC50 & Target

IC50: 77.79 nM (Speckled 140 kDa, SP140)[1]
In Vitro

GSK761 combines with SP140 in HuT78 cells and HEK293 cells transfected with Halo-tagged SP140[1].
GSK761 (0.01-1.11 µM; 1 h) reduces the inflammatory activation and down-regulates the expression of TNF, IL-6, IL-12p70, IL-1β, IL-8, IL-10 pro-inflammatory cytokines in M1 polarized macrophages[1].
GSK761 (0.04 µM; 4 h) significantly decreases the expression of TNF, IL6 and IL10 in CD14+ mucosal macrophages[1].

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

GSK761 Related Antibodies
Molecular Weight

646.82

Formula

C40H46N4O4
Unlabeled CAS

Appearance

Solid

Color

White to off-white

SMILES

CN1C2=CC=C(C=C2N=C1C3=CC=C(C=C3)C(NC4=CC(CCOC(C)(C)C)=CC=C4)=O)C(NC5=CC(CCOC(C)(C)C)=CC=C5)=O
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 : 125 mg/mL (193.25 mM; ultrasonic and warming and heat to 60°C; 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 1.5460 mL 7.7301 mL 15.4603 mL
5 mM 0.3092 mL 1.5460 mL 3.0921 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 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

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Volume (start)

V1

=
Concentration (final)

C2

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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: ≥ 2.08 mg/mL (3.22 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% Corn Oil

    Solubility: ≥ 2.08 mg/mL (3.22 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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: 99.64%

COA (243 KB) HNMR (287 KB) LCMS (111 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5460 mL 7.7301 mL 15.4603 mL 38.6506 mL
5 mM 0.3092 mL 1.5460 mL 3.0921 mL 7.7301 mL
10 mM 0.1546 mL 0.7730 mL 1.5460 mL 3.8651 mL
15 mM 0.1031 mL 0.5153 mL 1.0307 mL 2.5767 mL
20 mM 0.0773 mL 0.3865 mL 0.7730 mL 1.9325 mL
25 mM 0.0618 mL 0.3092 mL 0.6184 mL 1.5460 mL
30 mM 0.0515 mL 0.2577 mL 0.5153 mL 1.2884 mL
40 mM 0.0387 mL 0.1933 mL 0.3865 mL 0.9663 mL
50 mM 0.0309 mL 0.1546 mL 0.3092 mL 0.7730 mL
60 mM 0.0258 mL 0.1288 mL 0.2577 mL 0.6442 mL
80 mM 0.0193 mL 0.0966 mL 0.1933 mL 0.4831 mL
100 mM 0.0155 mL 0.0773 mL 0.1546 mL 0.3865 mL
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GSK761 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:

GSK761GSK 761GSK-761Epigenetic Reader DomainHuT78HEK293MacrophagesInhibitorinhibitorinhibit

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