2. Immunology/Inflammation
  3. NOD-like Receptor (NLR)
  4. GSK717

GSK717 is a potent, selective NOD2 (nucleotide-binding oligomerization domain 2) inhibitor. GSK717 inhibits muramyl dipeptide (MDP)-induced NOD2-mediated signaling, with an IC50 of 400 nM for MDP-stimulated IL-8 secretion in HEK293/hNOD2 cells.

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GSK717 Chemical Structure

GSK717 Chemical Structure

CAS No. : 1595278-21-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 110 In-stock
Solution
10 mM * 1 mL in DMSO USD 110 In-stock
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10 mg USD 160 In-stock
50 mg USD 470 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

GSK717 Related Antibodies

Top Publications Citing Use of Products

View All NOD-like Receptor (NLR) Isoform Specific Products:

View All Isoforms
NLRP3 NLRP1 NOD1 NOD2

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GSK717 is a potent, selective NOD2 (nucleotide-binding oligomerization domain 2) inhibitor. GSK717 inhibits muramyl dipeptide (MDP)-induced NOD2-mediated signaling, with an IC50 of 400 nM for MDP-stimulated IL-8 secretion in HEK293/hNOD2 cells[1].

Cellular Effect
Cell Line Type Value Description References
HEK-293T IC50
0.4 μM
Compound: 26, GSK717
Inhibition of NOD1 (unknown origin) expressed in HEK293T cells coexpressing NF-kappaB driven luciferase reporter gene by HTS primary assay
Inhibition of NOD1 (unknown origin) expressed in HEK293T cells coexpressing NF-kappaB driven luciferase reporter gene by HTS primary assay
[PMID: 24707857]
In Vitro

GSK717 blocks synergy between NOD2 and TLR2. GSK717 does not affect NOD1, TNFR1 and TLR2-mediated responses. GSK717 (5 μM) inhibits the release of IL-8, IL-6, TNFα and IL-1β in primary human monocytes stimulated with MDP[1].

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

GSK717 Related Antibodies
Molecular Weight

452.55

Formula

C28H28N4O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC=C2C(CCC2)=C1)CN3C4=CC=CC=C4N=C3CCN(C)C(C5=CC=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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (552.43 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 2.2097 mL 11.0485 mL 22.0970 mL
5 mM 0.4419 mL 2.2097 mL 4.4194 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: ≥ 2.08 mg/mL (4.60 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (4.60 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 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: 99.88%

SDS (393 KB)

COA (256 KB) LCMS (273 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 2.2097 mL 11.0485 mL 22.0970 mL 55.2425 mL
5 mM 0.4419 mL 2.2097 mL 4.4194 mL 11.0485 mL
10 mM 0.2210 mL 1.1049 mL 2.2097 mL 5.5243 mL
15 mM 0.1473 mL 0.7366 mL 1.4731 mL 3.6828 mL
20 mM 0.1105 mL 0.5524 mL 1.1049 mL 2.7621 mL
25 mM 0.0884 mL 0.4419 mL 0.8839 mL 2.2097 mL
30 mM 0.0737 mL 0.3683 mL 0.7366 mL 1.8414 mL
40 mM 0.0552 mL 0.2762 mL 0.5524 mL 1.3811 mL
50 mM 0.0442 mL 0.2210 mL 0.4419 mL 1.1049 mL
60 mM 0.0368 mL 0.1841 mL 0.3683 mL 0.9207 mL
80 mM 0.0276 mL 0.1381 mL 0.2762 mL 0.6905 mL
100 mM 0.0221 mL 0.1105 mL 0.2210 mL 0.5524 mL
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GSK717 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:

GSK7171595278-21-9GSK 717GSK-717NOD-like Receptor (NLR)pro-inflammatorycytokinesimmuneresponsesMDP-stimulatedNOD2-TLR2synergyInhibitorinhibitorinhibit

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