2. Immunology/Inflammation MAPK/ERK Pathway NF-κB
  3. Toll-like Receptor (TLR) MyD88 p38 MAPK NF-κB JNK
  4. MyD88-IN-3

MyD88-IN-3 是一种具有口服活性的选择性 MyD88 抑制剂。MyD88-IN-3 特异性靶向 MyD88 的 TIR 结构域 (KD = 28.5 μM)，从而阻止 MyD88 自聚合及其与 TLR 的相互作用，从而抑制 MAPK 和 NF-κB 通路的激活。MyD88-IN-3 表现出显著的抗炎效果，并有效缓解 CLP (盲肠结扎和穿刺) 和脂多糖 (HY-D1056) (LPS) 诱导的急性肺损伤 (ALI) 中的症状。MyD88-IN-3 可用于 ALI 的研究。

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MyD88-IN-3

MyD88-IN-3 Chemical Structure

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MyD88-IN-3 相关抗体

Top Publications Citing Use of Products

查看 Toll-like Receptor (TLR) 亚型特异性产品:

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TLR3 TLR8 TLR9 TLR2 TLR4 TLR7 TLR1 TLR6

查看 p38 MAPK 亚型特异性产品:

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

查看 NF-κB 亚型特异性产品:

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

查看 JNK 亚型特异性产品:

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JNK1 JNK2 JNK3 JNK

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MyD88-IN-3 is an orally active, selective MyD88 Inhibitor. MyD88-IN-3 specifically targets the TIR domain of MyD88 (KD = 28.5 μM), thereby preventing MyD88 self-polymerization and interaction with TLRs, which suppresses the activation of MAPK and NF-κB pathways. MyD88-IN-3 demonstrates significant anti-inflammatory efficacy and effectively mitigates Acute Lung Injury (ALI) symptoms in CLP (cecal ligation and puncture) and Lipopolysaccharides (HY-D1056) (LPS)-induced ALI models. MyD88-IN-3 can be used for the study of ALI[1].

体外研究
(In Vitro)

MyD88-IN-3 (1.1-30 μM) 表现出强大的抗炎作用，显著抑制小鼠巨噬细胞 J774A.1 (IC50 = 1.32 μM) 和经 PMA 诱导分化而来的人巨噬细胞 THP-1 (IC50 = 0.75 μM) 中 IL-6 的分泌[1]。
MyD88-IN-3 (10 μM，预处理 2 小时，然后与 0.5 μg/mL LPS 共同处理 30 分钟) 可恢复 J774A.1 巨噬细胞中 LPS 诱导的 IκBα 表达水平的降低，显着降低 p38 的磷酸化，抑制 JNK 的磷酸化，抑制 p65 的磷酸化和核易位，并抑制 LPS 诱导的 MAPK 通路激活，导致细胞中 c-Jun 的核易位[1]。
MyD88-IN-3 (5 μM、10 μM) 可抑制 J774A.1 中 MyD88 的同源二聚化[1]。
MyD88-IN-3 (10 μM，2 小时) 可抑制 J774A.1 中 M yD88 与 TLR4 的相互作用[1]。
MyD88-IN-3 (10 μM，4 小时) 可提高 MyD88 的热稳定性，在64 ℃下可保留约 50% 的 MyD88[1]。
MyD88-IN-3 可有效结合 TIR 结构域 (KD = 28.5 μM) ，而对 DD 结构域不表现出结合亲和力 (KD = 1.32 M)[1]。

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

MyD88-IN-3 相关抗体:

Western Blot Analysis[1]

Cell Line: J774A.1 mouse macrophages
Concentration: Pretreatment for 2 h, followed by co-treatment with 0.5 μg/mL LPS for 30 minutes
Incubation Time: 2 h
Result: Restored LPS-induced IκBα degradation and inhibited p38 and JNK phosphorylation.
体内研究
(In Vivo)

MyD88-IN-3 (500 mg/kg，1000 mg/kg，灌胃，每日一次，连续 10 天) 在 SD 大鼠体内表现出良好的安全性[1]。
MyD88-IN-3 (20 mg/kg，灌胃，预处理 6 小时) 可减轻 C57BL/6 小鼠脓毒症诱发的急性肺损伤[1]。
MyD88-IN-3 (20 mg/kg，灌胃，预处理 30 分钟) 可减轻 C57BL/6 小鼠LPS诱发的急性肺损伤[1]。

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

Animal Model: SD rats[1]
Dosage: 500 mg/kg, 1000 mg/kg
Administration: Oral gavage, once daily for 10 days
Result: Induced a slight decrease in body weight in the first day, following which body weight progressively returned to levels akin to the control group, with no statistically significant differences noted.
Indicated no notable pathological alterations in the organs of mice.
Animal Model: Male C57BL/6 mice, weighing between 18 and 22 g, after the administration of anesthesia, an abdominal incision was performed to reveal the cecum. The cecum was ligated beneath the ileocecal valve with surgical thread and subsequently punctured once with a needle. The abdominal incision was subsequently sutured closed after repositioning[1]
Dosage: 20 mg/kg
Administration: Oral gavage, administer 6 hours before CLP surgery
Result: Markedly diminished the lung wet/dry weight ratio, demonstrating its effectiveness in alleviating sepsis-induced lung edema.
Obstructed this cellular influx into BALF, suggesting that MyD88-IN-3 alleviates sepsis-induced pulmonary edema.
led to a significant decrease in IL-6.
Alleviated lung tissue damage, interstitial edema, pulmonary congestion, inflammatory infiltration, and thickened alveolar septa.
Significantly diminished immune cell infiltration, thereby mitigating the inflammatory response.
Animal Model: LPS-Induced Male C57BL/6 mice, weighing between 18 and 22 g
Dosage: 20 mg/kg
Administration: Oral gavage, administer 30 min before LPS.
Result: Markedly diminished the lung wet/dry weight ratio, demonstrating its effectiveness in alleviating sepsis-induced lung edema.
Significantly suppressed the increase in total protein concentration and the discharge of immune cells into BALF.
Decreased spleen weight and mitigated inflammation.
Markedly reduced IL-6 levels in both bronchoalveolar lavage fluid and serum samples.
Mitigated augmented alveolar septal thickness, pulmonary congestion, inflammatory infiltration, and lung tissue degradation.
Reduced leukocyte infiltration into the alveoli.
分子量

508.55

Formula

C24H24N6O5S
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

MyD88-IN-3 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

MyD88-IN-3Toll-like Receptor (TLR)MyD88p38 MAPKNF-κBJNKNuclear factor-κBNuclear factor-kappaBc-Jun N-terminal kinaseAcute lung injuryALIAcute respiratory distress syndromeARDSMAPKInhibitorinhibitorinhibit

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