2. Immunology/Inflammation NF-κB Cytoskeleton TGF-beta/Smad MAPK/ERK Pathway Metabolic Enzyme/Protease
  3. MyD88 Toll-like Receptor (TLR) NF-κB Collagen TGF-β Receptor p38 MAPK Reactive Oxygen Species (ROS)
  4. LM9

LM9 是一种强效、口服活性的 MyD88 抑制剂。LM9 阻断 TLR4/MyD88 结合、MyD88 同源二聚体形成以及 TLR4/MyD88/NF-κB 信号通路的激活。LM9 通过调节巨噬细胞中的炎症反应和氧化应激来预防动脉粥样硬化。LM9 能有效缓解肥胖诱发的心肌病中的炎症反应和纤维化。LM9 可用于纤维化和动脉粥样硬化的研究。

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LM9

LM9 Chemical Structure

CAS No. : 2249864-11-5

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LM9 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

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

查看 TGF-β Receptor 亚型特异性产品:

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ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LM9 is a potent, orally active MyD88 inhibitor. LM9 blocks TLR4/MyD88 binding, MyD88 homodimer formation, and TLR4/MyD88/NF-κB signaling pathway activation. LM9 prevents atherosclerosis by regulating inflammatory responses and oxidative stress in macrophages. LM9 efficiently mitigates inflammatory responses and fibrosis in obesity-induced cardiomyopathy. LM9 can be used for fibrosis and atherosclerosis research[1][2].

IC50 & Target[1][2]

NF-κB

 

TLR4

 

Collagen I

 

Collagen IV

 

体外研究
(In Vitro)

LM9 (5-10 μM; 1 小时预处理) 通过减少促炎细胞因子的产生和 ICAM-1 的表达，减弱棕榈酸 (PA)(HY-N0830) 在小鼠腹膜巨噬细胞中诱导的炎症 [1]。
LM9 (5-10 μM; 1 小时预处理) 抑制 PA 诱导的 H9C2 细胞炎症和 NF-κB 信号通路激活 [1]。
LM9 (5-10 μM) 抑制 PA 诱导的 TLR4/MyD88 结合及 MyD88 同源二聚体在 HEK293T 细胞中的形成 [1]。
LM9 (5-10 μM; 1 小时预处理) 减轻 PA 诱导的 H9C2 细胞脂质积累和纤维化，降低 胶原 1/4 和 TGF-β 表达 [1]。
LM9 (24 小时) 在高达 20 μM 的浓度下对小鼠原代腹膜巨噬细胞的存活率无影响 [2]。
LM9 (10-20 μM; 1 小时预处理) 通过抑制 TLR4-MyD88 复合物的形成、NF-κB 的活化以及 MAPK 的磷酸化，减轻了暴露于 ox-LDL (HY-NP013) 的小鼠原代腹膜巨噬细胞和 RAW264.7 细胞中的炎症反应 [2]。
LM9 (10-20 μM; 1 小时预处理) 抑制小鼠原代腹膜巨噬细胞中 ox-LDL 的摄取和泡沫细胞形成，这与 CD36 表达减少相关 [2]。
LM9 (10-20 μM; 1 小时预处理) 减少 ox-LDL 诱导的小鼠原代腹膜巨噬细胞中 ROS 的产生，且该效应由 MyD88 抑制介导 [2]。

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

LM9 相关抗体:

Real Time qPCR[1]

Cell Line: H9C2 cells
Concentration: 5; 10 μM
Incubation Time: 1 h pretreat + 12 h with PA
Result: Significantly reduced the mRNA levels of TNF-α, IL-6, ICAM-1, and BNP.
Markly decreased the protein levels of
collagen 1/4 and TGF-β.

ELISA Assay[1]

Cell Line: mouse peritoneal macrophages
Concentration: 5; 10 μM
Incubation Time: 1 h + 24 h with PA
Result: Reduced PA-induced TNF-α, IL-6, and IL-
1β in mouse peritoneal macrophages.
Exhibited a dose-dependent inhibitory effect on the mRNA levels of proinflammatory gene.

Western Blot Analysis[1]

Cell Line: H9C2 cells
Concentration: 5; 10 μM
Incubation Time: 1 h
Result: Markly inhibited the degradation and phosphorylation of IκB-α.
Decreased the accumulation of NF-κB p65 in the nucleus.
Markly decreased the protein levels of
collagen 1/4 and TGF-β.

Western Blot Analysis[2]

Cell Line: RAW264.7 cells; mouse primary peritoneal macrophages
Concentration: 10; 20 μM
Incubation Time: 1 h
Result: Inhibited ox-LDL-induced TLR4-MyD88 complex formation.
Inhibited oxLDL-induced activation of MAPKs.

Immunofluorescence[2]

Cell Line: RAW264.7 cells
Concentration: 10; 20 μM
Incubation Time: 1 h
Result: Decreased the accumulation of NF-κB p65 in the nucleus.
体内研究
(In Vivo)

LM9 (5 和 10 mg/kg；灌胃；每 2 天一次，持续 8 周) 被发现存在于高脂饮食 (HFD) 小鼠中，可减轻心肌炎症，改善纤维化，改善心脏功能，并使血脂谱恢复正常[1]。
LM9 (10 mg/kg; 灌胃; 每 2 天一次，持续 8 周) 被发现可减轻高脂饮食 (HFD) ApoE-/- 小鼠体内的动脉粥样硬化[2]。

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

Animal Model: Male C57BL/6J mice (18-22 g) fed with HFD for 16 weeks[1]
Dosage: 5, 10 mg/kg
Administration: i.g.; every 2 days; 8 weeks
Result: Dose-dependently decreased serum CK-MB, CK, triglyceride, total cholesterol, and LDL levels.
Increased HDL levels.
Improved cardiac function indicators (EF%, FS%).
Reduced myocardial TNF-α accumulation, neutrophil infiltration, and mRNA levels of proinflammatory genes (TNF-α, IL-6, ICAM-1).
Decreased collagen deposition and mRNA/protein levels of profibrotic genes (collagen I, collagen IV, TGF-β, BNP).
Inhibited HFD-induced IκB-α degradation.
Animal Model: Male ApoE-/- mice (8-week-old) fed with HFD for 16 weeks[2]
Dosage: 10 mg/kg
Administration: i.g.; every 2 days for 8 weeks
Result: Reduced whole aorta plaque area, aortic root lesion area, α-SMA-positive area, collagen deposition.
Reduced serum TNF-α and IL-6 levels, aortic mRNA levels of IL-1β, TNF-α, IL-6, ICAM, and VCAM, CD68-positive macrophage infiltration.
Reduced CD36 expression (mRNA and protein in aortas), and DHE-positive ROS levels in aortas.
Did not alter body weight or serum lipid levels (TG, TCH, LDL, HDL).
分子量

497.57

Formula

C24H27N5O5S
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

LM9 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:

LM92249864-11-5LM 9LM-9MyD88Toll-like Receptor (TLR)NF-κBCollagenTGF-β Receptorp38 MAPKReactive Oxygen Species (ROS)Nuclear factor-κBNuclear factor-kappaBTransforming growth factor beta receptorsMyD88 homodimer formationmacrophagesatherosclerosisox-LDLTLR4/MyD88/NF-κB signaling pathwayTLR4/MyD88 bindingobesity-induced cardiomyopathycardiac cellshigh-fat diet-fed miceInhibitorinhibitorinhibit

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