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

Sim-9 是一种干扰素调节因子 3 (IRF3) 共价变构抑制剂。Sim-9 可与 IRF3 的 Cys222 残基共价结合，诱导其构象变化，阻断其与 TRIF、MAVS、STING 的相互作用，抑制 IRF3 同源二聚化和 I 型干扰素应答。Sim-9 在小鼠脓毒症和急性胰腺炎模型中展现出显著的抗炎、器官保护及生存获益效果。Sim-9 可用于炎症性疾病相关研究。

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Sim-9

Sim-9 Chemical Structure

CAS No. : 3099101-40-0

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Sim-9 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

Sim-9 (2.5-10 μM) 在小鼠 RAW264.7 细胞和人 THP-1/HT-29/A549 细胞中剂量依赖性抑制 TLRs/RLRs/STING 激活引发的干扰素反应[1]。
Sim-9 (5 μM; 0.5-6 h) 可抑制经 cGAS-STING、TLR3 或 RIG-I 通路激活的小鼠 RAW264.7 细胞中 IRF3 的磷酸化，且不会改变 TBK1 的磷酸化[1]。
Sim-9 (5 μM) 可抑制经 cGAS-STING、TLR3 或 RIG-I 通路激活的小鼠 RAW264.7 细胞中 IRF3 的同源二聚化[1]。

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

Sim-9 相关抗体:

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.
体内研究
(In Vivo)

Sim-9 (30-60 mg/kg; i.p.; single injection) 在小鼠脓毒症模型中具有保护和抗炎活性[1]。
Sim-9 (30-60 mg/kg; i.p.; 1 injection/3 injections) 在急性胰腺炎小鼠模型中能改善胰腺水肿及炎症标志物水平[1]。

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.
分子量

567.55

Formula

C31H28F3NO6
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Sim-9 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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