2. Immunology/Inflammation
  3. IFNAR STING
  4. Sim-9

Sim-9 is a covalent allosteric inhibitor of interferon regulatory factor 3 (IRF3). Sim-9 binds covalently to the Cys222 residue of IRF3, induces its conformational change, blocks its interactions with TRIF, MAVS and STING, and inhibits IRF3 homodimerization and type I interferon response. Sim-9 exhibits significant anti-inflammatory, organ-protective and survival benefits in mouse models of sepsis and acute pancreatitis. Sim-9 can be used for research related to inflammatory diseases.

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Sim-9

Sim-9 Chemical Structure

CAS No. : 3099101-40-0

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Sim-9 Related Antibodies

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Description

Sim-9 is a covalent allosteric inhibitor of interferon regulatory factor 3 (IRF3). Sim-9 binds covalently to the Cys222 residue of IRF3, induces its conformational change, blocks its interactions with TRIF, MAVS and STING, and inhibits IRF3 homodimerization and type I interferon response. Sim-9 exhibits significant anti-inflammatory, organ-protective and survival benefits in mouse models of sepsis and acute pancreatitis. Sim-9 can be used for research related to inflammatory diseases[1].

In Vitro

Sim-9 (2.5-10 μM) dose-dependently inhibits interferon responses induced by TLRs/RLRs/STING activation in murine RAW264.7 cells and human THP-1/HT-29/A549 cells[1].
Sim-9 (5 μM; 0.5-6 h) inhibits the phosphorylation of IRF3 in mouse RAW264.7 cells activated via the cGAS-STING, TLR3 or RIG-I pathways, without altering the phosphorylation of TBK1[1].
Sim-9 (5 μM) inhibits the homodimerization of IRF3 in mouse RAW264.7 cells activated via the cGAS-STING, TLR3 or RIG-I pathways[1].

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

Sim-9 Related Antibodies

Western Blot Analysis[1]

Cell Line: mouse RAW264.7 cells
Concentration: 5 μM
Incubation Time: 0.5, 1, 2, 4, 6 h
Result: Significantly reduced phosphorylated IRF3 levels starting at 1 h post-stimulation, with suppression sustained for up to 6 h.
Did not affect phosphorylated or total TBK1 protein levels.
In Vivo

Sim-9 (30-60 mg/kg; i.p.; single injection) exhibits protective and anti-inflammatory activities in a mouse sepsis model[1].
Sim-9 (30-60 mg/kg; i.p.; 1 injection/3 injections) improves pancreatic edema and the levels of inflammatory markers in a mouse model of acute pancreatitis[1].

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

Animal Model: C57BL/6J mice (8-week-old male, 0.022-0.024 kg, sepsis induced via cecal ligation and puncture)[1]
Dosage: 30 mg/kg; 60 mg/kg
Administration: i.p.; single injection 2 hours pre-surgery
Result: Reduced CLP-induced sepsis mortality to 60% and 80% respectively.
Significantly improved the survival rate.
Inhibited systemic inflammatory responses and ameliorated IRF3-mediated inflammatory injuries in kidney and lung tissues.
Animal Model: C57BL/6J mice (8-week-old male, 0.022-0.024 kg, acute pancreatitis induced by Caerulein (HY-A0190) )[1]
Dosage: 30 mg/kg; 60 mg/kg
Administration: i.p.; 1 injection 1 hour pre-first cerulein injection (acute phase); 3 total injections: 1 hour pre-first cerulein, 24 hours post-first cerulein, 48 hours post-first cerulein (recovery phase)
Result: Significantly reduced pancreatic edema, pancreatic weight, and serum amylase and lipase levels in acute phase with both doses.
Improved pancreatic histology (reduced acinar cell edema, necrosis, and immune cell infiltration) in acute phase with both doses.
Significantly reduced serum amylase and lipase levels in recovery phase with both doses.
Improved pancreatic histology (reduced acinar cell necrosis and acinar-to-ductal metaplasia) in recovery phase with both doses.
Reduced p-IRF3 staining in pancreatic tissues in recovery phase with both doses.
Reduced CD11b-IRF7 colocalization in pancreatic tissues in recovery phase with both doses.
Molecular Weight

567.55

Formula

C31H28F3NO6
CAS No.
SMILES

O=C(C1=CC=C(C2=CC=C(C=C2)C(F)(F)F)O1)OC3=C4[C@]56[C@@](C=C(C(C6)=O)OC)([H])[C@](N(CC5)C)([H])CC4=CC=C3OC
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Sim-9 Related Classifications

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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.

Keywords:

Sim-93099101-40-0Sim9Sim 9IFNARSTINGInterferon-α/β receptorInterferon-alpha/beta receptor Stimulator of Interferon GenesTMEM173MITAERISMPYSIFN responsesMAVSTRIFIRF3Cys222A549 cellssepsisRAW264.7 cellsInhibitorinhibitorinhibit

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