| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg | |||
| Other Sizes |
| Targets |
G150 targets human cyclic GMP-AMP synthase (cGAS), a cytosolic DNA sensor that catalyzes the synthesis of cGAMP from ATP and GTP. cGAMP activates the STING pathway, leading to type I interferon production. G150 inhibits h-cGAS with an IC50 of 10.2 nM. It is selective for human cGAS over mouse cGAS (IC50 = 25,000 nM).
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| ln Vitro |
G150 (0.1-100 μM; 1 hour) has an impact on primary human macrophages and human THP1 cells' production of CXCL10 and IFNB1 [1]. THP1 cells and primary human macrophages' dsDNA sensing is impacted by G150 (5–10 μM; 1 hour) [1]. G150 (0.1-100 μM; 1 hour) has an impact on THP1-Dual cell activation of the NF-κB pathway [1].
In vitro, G150 is a potent inhibitor of h-cGAS with an IC50 of 10.2 nM. It inhibits dsDNA-triggered interferon expression in THP1 cells with an intracellular IC50 of 1.96 µM. The compound is selective for human cGAS over mouse cGAS (IC50 = 25,000 nM). G150 can be used for research on inflammation. |
| ln Vivo |
In vivo activity data for G150 are not extensively detailed in the available sources. The compound is a research tool for studying cGAS-STING-driven inflammation. Specific in vivo efficacy data in animal models have not been reported. The compound may be used to explore therapeutic strategies targeting cGAS-STING pathway.
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| Enzyme Assay |
The in vitro enzyme assay for G150 involves measuring the inhibition of cGAS enzymatic activity. Recombinant human cGAS is incubated with DNA (e.g., herring testis DNA or ISD), ATP, and GTP in the presence of varying concentrations of the compound. cGAMP production is quantified by LC-MS/MS or using a cGAMP-specific ELISA. The IC50 value (10.2 nM) is determined from dose-response curves.
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| Cell Assay |
RT-PCR[1]
Cell Types: human THP1 cells and primary human macrophages Tested Concentrations: 0.1-100 μM Incubation Duration: 1 hour Experimental Results: Dose-dependent inhibition of IFNB1 and interferon-stimulated genes Monitoring CXCL10 expression, IC50 is 1.96 respectively and 7.57 μM in human THP1 cells, and inhibited the expression of IFNB1 and CXCL10 in primary human macrophages with IC50 of 0.62 and 0.87 μM, respectively. RT-PCR[1] Cell Types: human THP1 cells and primary human macrophages Tested Concentrations: 5 and 10 μM Incubation Duration: 1 hour Experimental Results: 10 μM in THP1 cells and 5 μM in primary cells , inhibits dsDNA sensing in human macrophages. RT-PCR[1] Cell Types: THP1-Dual cells Tested Concentrations: 0.1-100 μM Incubation Duration: 1 hour Experimental Results: Inhibits SEAP activity and luciferase activity in THP1-Dual cells, IC50 is 0.90 and 1.79 μM respectively. Cellular assays are performed using THP1 cells treated with G150 at varying concentrations. Cells are stimulated with dsDNA to activate the cGAS-STING pathway. Interferon expression is measured by RT-qPCR or by using an interferon-sensitive reporter assay. The intracellular IC50 of 1.96 µM is calculated from dose-response curves. |
| Animal Protocol |
In vivo animal studies for G150 are not detailed in the available sources. The compound is a research tool for studying cGAS-STING-driven inflammation. Specific animal models, dosing regimens, and efficacy data have not been reported.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for G150 are not available in the provided sources. The compound has a molecular weight of 391.25 g/mol and is soluble in DMSO (78 mg/mL). Powder formulations should be stored at -20°C for up to 3 years or 4°C for up to 2 years; solutions should be stored at -80°C for up to 6 months or -20°C for up to 1 month.
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| Toxicity/Toxicokinetics |
Toxicity data for G150 are not reported in the available sources. As a research compound, it is not intended for therapeutic use. Specific toxicological profiles have not been characterized. The compound is intended for research use only.
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| References | |
| Additional Infomation |
G150 is a research compound for studying the cGAS-STING pathway in inflammation. It is a potent and highly selective h-cGAS inhibitor. The compound is available from commercial suppliers for research use only. It can be used to explore therapeutic strategies targeting cGAS-STING-driven inflammation.
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| Molecular Formula |
C18H16CL2N4O2
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|---|---|
| Molecular Weight |
391.2512
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| Exact Mass |
390.065
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| CAS # |
2369751-30-2
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| PubChem CID |
138393372
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| Appearance |
White to off-white solid powder
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| Density |
1.545±0.06 g/cm3(Predicted)
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| Boiling Point |
694.0±55.0 °C(Predicted)
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| Flash Point |
373.5±31.5 °C
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| Vapour Pressure |
0.0±2.3 mmHg at 25°C
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| Index of Refraction |
1.736
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| LogP |
2.73
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
26
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| Complexity |
539
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CN(CC2=C1NC3=C2C(=CC(=C3Cl)Cl)C4=CN=C(C=C4)N)C(=O)CO
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| InChi Key |
VVUOUIPXYFIWLE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H16Cl2N4O2/c19-12-5-10(9-1-2-14(21)22-6-9)16-11-7-24(15(26)8-25)4-3-13(11)23-18(16)17(12)20/h1-2,5-6,23,25H,3-4,7-8H2,(H2,21,22)
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| Chemical Name |
1-[9-(6-aminopyridin-3-yl)-6,7-dichloro-1,3,4,5-tetrahydropyrido[4,3-b]indol-2-yl]-2-hydroxyethanone
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~319.49 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.32 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.32 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.32 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2556 mL | 1.2780 mL | 2.5559 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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