2. Immunology/Inflammation
  3. Cyclic GMP-AMP Synthase
  4. G150

G150 is a highly selective human cyclic GMP-AMP synthase (h-cGAS) inhibitor with an IC50 of 10.2 nM. G150 represses dsDNA-triggered interferon expression, and G150 can be used for the research of inflammatory.

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

G150 Chemical Structure

G150 Chemical Structure

CAS No. : 2369751-30-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 385 In-stock
Solution
10 mM * 1 mL in DMSO USD 385 In-stock
Solid
1 mg USD 166 In-stock
5 mg USD 350 In-stock
10 mg USD 550 In-stock
25 mg USD 940 In-stock
50 mg USD 1550 In-stock
100 mg USD 2250 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 4 publication(s) in Google Scholar

G150 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

G150 is a highly selective human cyclic GMP-AMP synthase (h-cGAS) inhibitor with an IC50 of 10.2 nM. G150 represses dsDNA-triggered interferon expression, and G150 can be used for the research of inflammatory[1].

IC50 & Target

IC50: 10.2 nM (h-cGAS)[1]
In Vitro

G150 (0.1-100 μM; 1 h) affects IFNB1 and CXCL10 expression in human THP1 cells and primary human macrophages[1].
G150 (5-10 μM; 1 h) affects dsDNA sensing in THP1 cells and primary human macrophages[1].
G150 (0.1-100 μM; 1 h) affects the NF-κB pathway activation in THP1-Dual cells[1].

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

G150 Related Antibodies

RT-PCR[1]

Cell Line: Human THP1 cells and primary human macrophages
Concentration: 0.1-100 μM
Incubation Time: 1 hour
Result: Dose-dependently inhibited IFNB1 and interferon-stimulated genes monitoring CXCL10 expression with IC50s of 1.96 and 7.57 μM respectively in human THP1 cells, and inhibited IFNB1 and CXCL10 expression with IC50s of 0.62 and 0.87 μM respectively in primary human macrophages.

RT-PCR[1]

Cell Line: Human THP1 cells and primary human macrophages
Concentration: 5 and 10 μM
Incubation Time: 1 hour
Result: Inhibited dsDNA sensing with a concentration of 10 μM in THP1 cells and with a concentration of 5 μM in primary human macrophages.

RT-PCR[1]

Cell Line: THP1-Dual cells
Concentration: 0.1-100 μM
Incubation Time: 1 hour
Result: Inhibited SEAP activity and luciferase activity with IC50s of 0.90 and 1.79 μM respectively in THP1-Dual cells.
Clinical Trial
Molecular Weight

391.25

Formula

C18H16Cl2N4O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NC1=CC=C(C2=C3C(NC4=C3CN(C(CO)=O)CC4)=C(Cl)C(Cl)=C2)C=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 : 125 mg/mL (319.49 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 2.5559 mL 12.7796 mL 25.5591 mL
5 mM 0.5112 mL 2.5559 mL 5.1118 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: ≥ 2.08 mg/mL (5.32 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 (5.32 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: 98.61%

COA (257 KB) LCMS (268 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 2.5559 mL 12.7796 mL 25.5591 mL 63.8978 mL
5 mM 0.5112 mL 2.5559 mL 5.1118 mL 12.7796 mL
10 mM 0.2556 mL 1.2780 mL 2.5559 mL 6.3898 mL
15 mM 0.1704 mL 0.8520 mL 1.7039 mL 4.2599 mL
20 mM 0.1278 mL 0.6390 mL 1.2780 mL 3.1949 mL
25 mM 0.1022 mL 0.5112 mL 1.0224 mL 2.5559 mL
30 mM 0.0852 mL 0.4260 mL 0.8520 mL 2.1299 mL
40 mM 0.0639 mL 0.3195 mL 0.6390 mL 1.5974 mL
50 mM 0.0511 mL 0.2556 mL 0.5112 mL 1.2780 mL
60 mM 0.0426 mL 0.2130 mL 0.4260 mL 1.0650 mL
80 mM 0.0319 mL 0.1597 mL 0.3195 mL 0.7987 mL
100 mM 0.0256 mL 0.1278 mL 0.2556 mL 0.6390 mL
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G150 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:

G1502369751-30-2G 150G-150Cyclic GMP-AMP SynthasecGASTHP1macrophagedsDNAanti-inflammatoryhigh-throughput screeninghuman myeloid cellInhibitorinhibitorinhibit

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