1. Immunology/Inflammation
  2. STING
  3. STING-IN-5

STING-IN-5 is a potent STING inhibitor, inhibiting LPS-induced NO synthesis in macrophages with an IC50 value of 1.15 μM. STING-IN-5 inhibits the inflammatory response. STING-IN-5 can be used to research anti-inflammatory diseases and sepsis.

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

STING-IN-5 Chemical Structure

STING-IN-5 Chemical Structure

CAS No. : 2920064-17-9

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Description

STING-IN-5 is a potent STING inhibitor, inhibiting LPS-induced NO synthesis in macrophages with an IC50 value of 1.15 μM. STING-IN-5 inhibits the inflammatory response. STING-IN-5 can be used to research anti-inflammatory diseases and sepsis[1].

In Vitro

STING-IN-5 (compound 30) (40 μM; 24 h) exhibits less effect on RAW264.7 cell viability[1].
STING-IN-5 (2.5 and 5 μM; 2 h) inhibits NO production in LPS-stimulated RAW264.7 with inhibition rate of 69.28 ± 2.36 and 78.66 ± 2.73 at 2.5 and 5 μM, respectively, and exhibits IC50 of 1.15 ± 0.15 μM[1].
STING-IN-5 (0.5-2 μM; 2 h) suppresses STING, as well as TBK1/IRF3/NF-κB activation[1].

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

Cell Viability Assay[1]

Cell Line: RAW264.7
Concentration: 40 μM
Incubation Time: 24 h
Result: Exhibited less effect on RAW264.7 cell viability of 91.08 ± 1.09%

Western Blot Analysis[1]

Cell Line: RAW264.7 (stimulated by LPS for 6 h)
Concentration: 0.5, 1 and 2 μM
Incubation Time: 2 h
Result: Significantly inhibited the protein expression of STING and the phosphorylation of the downstream targets TBK1, IRF3, p65, and IκB in a concentration-dependent manner.
In Vivo

STING-IN-5 (1.25-5 mg/kg; i.g.; once daily; for 3 days) have an obvious protective effect on acute liver injury in septic mice[1].
Pharmacokinetic Parameters of STING-IN-5 in male Sprague-Dawley rats[1].

Tmax (h) Cmax (ng/mL) AUC0-t (ng/mL·h) AUC0-∞ (ng/mL·h) T1/2 (h) MRT0-t (h) MRT0-∞ (h)
1 66.52 81.08 135.7 1.11 0.99 2.02

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

Animal Model: Male BALB/c mice (6-8 weeks; acute liver injury induced by injection of 10 mg/kg LPS)[1]
Dosage: 1.25, 2.5, 5 mg/kg
Administration: i.g.; once daily; for 3 days
Result: Significantly 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.
Significantly reduced the levels of AST, ALT, and ALP (liver function specific indicators).
Molecular Weight

854.17

Formula

C47H67NO9S2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@H]([C@H](OC(CCSSCCC(NOCC=C)=O)=O)CC[C@@]1([C@@]2([C@@H](C[C@]3(/C4=C(CC/C=C(C)/C)\C(OCC5=CC=CC=C5)=O)[H])O)[H])C)[C@@]1(CC[C@]2(C)[C@@]3(C)C[C@@H]4OC(C)=O)[H]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (117.07 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 1.1707 mL 5.8536 mL 11.7073 mL
5 mM 0.2341 mL 1.1707 mL 2.3415 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
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 (stored under nitrogen). 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 1.1707 mL 5.8536 mL 11.7073 mL 29.2682 mL
5 mM 0.2341 mL 1.1707 mL 2.3415 mL 5.8536 mL
10 mM 0.1171 mL 0.5854 mL 1.1707 mL 2.9268 mL
15 mM 0.0780 mL 0.3902 mL 0.7805 mL 1.9512 mL
20 mM 0.0585 mL 0.2927 mL 0.5854 mL 1.4634 mL
25 mM 0.0468 mL 0.2341 mL 0.4683 mL 1.1707 mL
30 mM 0.0390 mL 0.1951 mL 0.3902 mL 0.9756 mL
40 mM 0.0293 mL 0.1463 mL 0.2927 mL 0.7317 mL
50 mM 0.0234 mL 0.1171 mL 0.2341 mL 0.5854 mL
60 mM 0.0195 mL 0.0976 mL 0.1951 mL 0.4878 mL
80 mM 0.0146 mL 0.0732 mL 0.1463 mL 0.3659 mL
100 mM 0.0117 mL 0.0585 mL 0.1171 mL 0.2927 mL
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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.

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STING-IN-5
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