STING-IN-5 is a potent STING inhibitor that can suppress LSP-induced NO synthesis in macrophages with IC50 of 1.15 μM. STING-IN-5 inhibits inflammatory responses. STING-IN-5 may be utilized to study anti-inflammatory diseases and sepsis.

Physicochemical Properties

CAS #	2920064-17-9
Appearance	White to off-white solid powder
HS Tariff Code	2934.99.9001
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)

Biological Activity

ln Vitro	Compound 30 (STING-IN-5) (40 μM; 24 h) had minimal impact on the viability of RAW264.7 cells [1]. LPS-stimulated RAW264.7 cells produce less NO when exposed to STING-IN-5 (2.5 and 5 μM; 2 h). With an IC50 of 1.15, the inhibition rates are 69.28 ± 2.36% at 2.5 μM and 78.66 ± 2.73% at 5 μM. ± 0.15 μM [1]. STING-IN-5 (0.5-2 μM; 2 h) suppresses the activation of STING and TBK1/IRF3/NF-κB [1].
ln Vivo	In septic mice, STING-IN-5 (1.25–5 mg/kg; gavage; once daily for three days in a row) significantly reduces acute liver injury[1]. STING-IN-5's pharmacokinetic parameters in male Sprague-Dawley rats[1]. AUC0-t (ng/mL·h) AUC0-∞ (ng/mL·h) Tmax (h) Cmax (ng/mL) MRT0-t (h) MRT0-∞ (h) 1 66.52 81.08 135.7 1.11 0.99 2.02
Cell Assay	Cell Viability Assay[1] Cell Types: RAW264.7 Tested Concentrations: 40 μM Incubation Duration: 24 h Experimental Results: demonstrated less effect on RAW264.7 cell viability of 91.08 ± 1.09% Western Blot Analysis[1] Cell Types: RAW264.7 ( stimulated by LPS for 6 h) Tested Concentrations: 0.5, 1 and 2 μM Incubation Duration: 2 h Experimental Results: Dramatically inhibited the protein expression of STING and the phosphorylation of the downstream targets TBK1, IRF3, p65, and IκB in a concentration-dependent manner .
Animal Protocol	Animal/Disease Models: Male balb/c (Bagg ALBino) mouse (6-8 weeks; acute liver injury induced by injection of 10 mg/kg LPS)[1] Doses: 1.25, 2.5, 5 mg/kg Route of Administration: ig; one time/day; for 3 days Experimental Results: Dramatically improved pathological changes including disorderly arranged liver cells, blurred boundaries, congested hepatic sinusoids, swollen hepatocytes, a small number of hepatocytes were necrotic, and inflammatory cells infiltrated local areas. Dramatically decreased the levels of AST, ALT, and ALP (liver function specific indicators).
References	[1]. Discovery of fusidic acid derivatives as novel STING inhibitors for treatment of sepsis. Eur J Med Chem. 2022 Dec 15;244:114814.

Solubility Data

Solubility (In Vitro)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Solubility (In Vivo)

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples. Injection Formulations (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] *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. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.  (Please use freshly prepared in vivo formulations for optimal results.)